Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10934575 202771 0 None 3 5 Human 10.0 pEC50 = 10.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72441 202771 0 None 3 5 Human 10.0 pEC50 = 10.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
44362146 164371 1 None 50 3 Human 9.6 pEC50 = 9.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1ccc(-c2ccsc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL422477 164371 1 None 50 3 Human 9.6 pEC50 = 9.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1ccc(-c2ccsc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44574074 188869 0 None 977 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 2 0 4 2.7 c1ccc([C@@H]2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL513691 188869 0 None 977 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 2 0 4 2.7 c1ccc([C@@H]2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
11109088 202470 0 None 1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70751 202470 0 None 1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
22493318 44489 0 None 13 3 Human 9.3 pEC50 = 9.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 241 4 2 4 2.4 c1coc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL152155 44489 0 None 13 3 Human 9.3 pEC50 = 9.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 241 4 2 4 2.4 c1coc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44362194 34144 1 None 10 3 Human 9.3 pEC50 = 9.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1ccc(-c2ccoc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142784 34144 1 None 10 3 Human 9.3 pEC50 = 9.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1ccc(-c2ccoc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493352 47995 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ncco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL155326 47995 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ncco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
22493236 60062 0 None 5 3 Human 9.1 pEC50 = 9.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 242 4 3 5 0.9 c1ccc(-c2nc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
CHEMBL17491 60062 0 None 5 3 Human 9.1 pEC50 = 9.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 242 4 3 5 0.9 c1ccc(-c2nc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
44271661 161235 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL414185 161235 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44271661 161235 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
Effective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determinedEffective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determined
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL414185 161235 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
Effective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determinedEffective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determined
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
22493280 47996 0 None 1 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ccno2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL155327 47996 0 None 1 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ccno2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44271661 161235 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL414185 161235 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44369431 45084 0 None 57 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccsc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL152693 45084 0 None 57 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccsc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44362208 35190 1 None 3 3 Human 9.0 pEC50 = 9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1csc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL143801 35190 1 None 3 3 Human 9.0 pEC50 = 9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1csc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493258 98198 0 None 5 3 Human 9.0 pEC50 = 9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
CHEMBL277375 98198 0 None 5 3 Human 9.0 pEC50 = 9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
44574078 178174 0 None 120 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 0 3 3.3 c1cncc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL468711 178174 0 None 120 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 0 3 3.3 c1cncc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44219718 188249 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(-c2cncnc2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL506744 188249 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(-c2cncnc2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44362286 98416 1 None 7 2 Human 8.9 pEC50 = 8.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1coc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL279136 98416 1 None 7 2 Human 8.9 pEC50 = 8.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1coc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44362195 120563 0 None 2 3 Human 8.9 pEC50 = 8.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 241 4 2 3 2.1 c1c[nH]c(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL357129 120563 0 None 2 3 Human 8.9 pEC50 = 8.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 241 4 2 3 2.1 c1c[nH]c(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493263 97620 0 None 50 3 Human 8.9 pEC50 = 8.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 5 2 6 1.4 CCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL273316 97620 0 None 50 3 Human 8.9 pEC50 = 8.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 5 2 6 1.4 CCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
22493365 97999 0 None 15 3 Human 8.9 pEC50 = 8.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cn[nH]c2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
CHEMBL275844 97999 0 None 15 3 Human 8.9 pEC50 = 8.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cn[nH]c2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
44329788 206352 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 2.1 CCC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL97859 206352 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 2.1 CCC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
11098175 202460 0 None 2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL70691 202460 0 None 2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
10221005 202609 0 None 72 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71479 202609 0 None 72 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
44362185 120503 0 None 19 3 Human 8.7 pEC50 = 8.7 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1cncc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL356605 120503 0 None 19 3 Human 8.7 pEC50 = 8.7 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1cncc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493343 63625 0 None 19 3 Human 8.7 pEC50 = 8.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 2 6 0.9 Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL18069 63625 0 None 19 3 Human 8.7 pEC50 = 8.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 2 6 0.9 Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44343410 11435 2 None -1 3 Human 8.0 pEC50 = 8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 219 4 2 3 2.7 CSc1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL118055 11435 2 None -1 3 Human 8.0 pEC50 = 8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 219 4 2 3 2.7 CSc1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
9837963 62627 0 None 8 3 Human 8.0 pEC50 = 8 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17851 62627 0 None 8 3 Human 8.0 pEC50 = 8 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44329796 206628 0 None 1 3 Human 8.0 pEC50 = 8 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 7 2 5 2.1 CCCCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL99559 206628 0 None 1 3 Human 8.0 pEC50 = 8 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 7 2 5 2.1 CCCCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493289 49405 0 None 4 3 Human 8.0 pEC50 = 8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1cnc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
CHEMBL156661 49405 0 None 4 3 Human 8.0 pEC50 = 8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1cnc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
11034737 202813 0 None -1 4 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72724 202813 0 None -1 4 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
44362145 34245 3 None - 1 Human 7.0 pEC50 = 7 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2ncc[nH]2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142864 34245 3 None - 1 Human 7.0 pEC50 = 7 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2ncc[nH]2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493401 206498 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 288 7 2 4 2.0 CCCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL98769 206498 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 288 7 2 4 2.0 CCCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493225 62168 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 4 2 6 1.2 Cc1nc(-c2ccccc2NCC2=NCCN2)n(C)n1 10.1016/s0960-894x(03)00050-7
CHEMBL17819 62168 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 4 2 6 1.2 Cc1nc(-c2ccccc2NCC2=NCCN2)n(C)n1 10.1016/s0960-894x(03)00050-7
44574878 177962 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
CHEMBL466916 177962 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
22493372 119720 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
CHEMBL352225 119720 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
11059195 101689 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 321 4 2 5 1.5 CS(=O)(=O)c1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL302698 101689 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 321 4 2 5 1.5 CS(=O)(=O)c1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
44574987 178091 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 3 0 3 2.8 FC(F)Oc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL467915 178091 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 3 0 3 2.8 FC(F)Oc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
76632 99575 48 None -5 2 Human 5.0 pEC50 = 5.0 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 181 4 1 3 1.2 COc1ccc(OC)c(CCN)c1 10.1021/jm00144a012
CHEMBL287047 99575 48 None -5 2 Human 5.0 pEC50 = 5.0 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 181 4 1 3 1.2 COc1ccc(OC)c(CCN)c1 10.1021/jm00144a012
44449657 95607 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 265 2 1 3 3.5 Cc1oncc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL260009 95607 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 265 2 1 3 3.5 Cc1oncc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44571891 169438 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 280 3 1 4 2.8 Cc1noc(Cc2cccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
CHEMBL444252 169438 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 280 3 1 4 2.8 Cc1noc(Cc2cccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
2435 713 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
395 713 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
520 713 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
5386 713 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
CHEMBL844 713 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
DB00484 713 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
44449690 95701 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1ccc(-c2cccc3c2CCC3c2ncc[nH]2)nc1 10.1016/j.bmcl.2008.03.070
CHEMBL260575 95701 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1ccc(-c2cccc3c2CCC3c2ncc[nH]2)nc1 10.1016/j.bmcl.2008.03.070
1960 2805 64 None -199 13 Rat 5.9 pEC50 = 5.9 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
439260 2805 64 None -199 13 Rat 5.9 pEC50 = 5.9 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
505 2805 64 None -199 13 Rat 5.9 pEC50 = 5.9 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
CHEMBL1437 2805 64 None -199 13 Rat 5.9 pEC50 = 5.9 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
DB00368 2805 64 None -199 13 Rat 5.9 pEC50 = 5.9 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
44574105 178220 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 1 4 1.3 CNS(=O)(=O)CCc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
CHEMBL469127 178220 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 1 4 1.3 CNS(=O)(=O)CCc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
44574045 188687 0 None 60 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 260 2 0 2 3.9 c1ccc(-c2ccccc2[C@@H]2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.166
CHEMBL512062 188687 0 None 60 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 260 2 0 2 3.9 c1ccc(-c2ccccc2[C@@H]2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.166
2765 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
515 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
CHEMBL13852 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
DB09202 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
22493274 10920 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 4 2 4 2.1 c1ccc(N2CCCCC2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL117581 10920 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 4 2 4 2.1 c1ccc(N2CCCCC2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
10015132 163306 1 None 29 3 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(02)00753-9
CHEMBL420683 163306 1 None 29 3 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(02)00753-9
9817256 202527 0 None 251 2 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL71001 202527 0 None 251 2 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
2765 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
515 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
CHEMBL13852 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
DB09202 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
10038958 118207 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cnsc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL341747 118207 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cnsc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
10015132 163306 1 None 29 3 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
CHEMBL420683 163306 1 None 29 3 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
22493265 61790 0 None 19 3 Human 7.9 pEC50 = 7.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 6 2 6 1.8 CCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17776 61790 0 None 19 3 Human 7.9 pEC50 = 7.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 6 2 6 1.8 CCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
2765 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
515 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
CHEMBL13852 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
DB09202 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
44329790 112041 0 None 5 3 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 247 5 2 5 1.3 CCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL329928 112041 0 None 5 3 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 247 5 2 5 1.3 CCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493224 206594 4 None 6 3 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 5 3 4 0.9 CCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL99362 206594 4 None 6 3 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 5 3 4 0.9 CCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
2765 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
515 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
CHEMBL13852 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
DB09202 928 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
12924821 102411 5 None - 1 Human 6.9 pEC50 = 6.9 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 207 2 1 3 1.5 COc1ccc(OC)c2c1CCC(N)C2 10.1021/jm00144a012
CHEMBL30596 102411 5 None - 1 Human 6.9 pEC50 = 6.9 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 207 2 1 3 1.5 COc1ccc(OC)c2c1CCC(N)C2 10.1021/jm00144a012
44593577 177879 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466296 177879 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
44343251 10405 2 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 251 4 2 4 1.4 CS(=O)(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL116843 10405 2 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 251 4 2 4 1.4 CS(=O)(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
44362510 118415 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 267 4 1 4 2.4 Cc1cccc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
CHEMBL342324 118415 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 267 4 1 4 2.4 Cc1cccc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
22493257 205902 3 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 272 4 2 4 1.3 O=C(c1ccccc1NCC1=NCCN1)N1CCCC1 10.1016/s0960-894x(01)00569-8
CHEMBL95245 205902 3 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 272 4 2 4 1.3 O=C(c1ccccc1NCC1=NCCN1)N1CCCC1 10.1016/s0960-894x(01)00569-8
44362289 121170 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1cnc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
CHEMBL358802 121170 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1cnc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
44449306 95149 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 2 3 2.6 CCCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257801 95149 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 2 3 2.6 CCCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449730 155555 0 None 22 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2cn[nH]c2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL406316 155555 0 None 22 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2cn[nH]c2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
9817256 202527 0 None 251 2 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71001 202527 0 None 251 2 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
44449278 95195 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257977 95195 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44574877 177956 0 None 23 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL466869 177956 0 None 23 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
44574135 188579 0 None 18 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2ccn[nH]2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL511211 188579 0 None 18 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2ccn[nH]2)c1 10.1016/j.bmcl.2009.03.166
22493269 46548 0 None 6 3 Human 7.8 pEC50 = 7.8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncoc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL154023 46548 0 None 6 3 Human 7.8 pEC50 = 7.8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncoc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44343257 10385 0 None 13 3 Human 7.8 pEC50 = 7.8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 250 4 1 2 3.7 c1ccc(-c2ccccc2OCc2c[nH]cn2)cc1 10.1016/s0960-894x(02)00753-9
CHEMBL116700 10385 0 None 13 3 Human 7.8 pEC50 = 7.8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 250 4 1 2 3.7 c1ccc(-c2ccccc2OCc2c[nH]cn2)cc1 10.1016/s0960-894x(02)00753-9
10199052 206205 0 None 5 3 Human 7.8 pEC50 = 7.8 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 258 5 3 4 1.0 O=C(NC1CC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL97044 206205 0 None 5 3 Human 7.8 pEC50 = 7.8 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 258 5 3 4 1.0 O=C(NC1CC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
619552 102212 2 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 250 2 0 3 2.5 Cn1nc(Cc2ccccc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
CHEMBL304747 102212 2 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 250 2 0 3 2.5 Cn1nc(Cc2ccccc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
45280075 121835 0 None -91 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 430 10 4 6 2.5 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3600395 121835 0 None -91 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 430 10 4 6 2.5 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
44343235 10087 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 4 1 4 2.6 c1ccc(-c2ccno2)c(OCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL115977 10087 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 4 1 4 2.6 c1ccc(-c2ccno2)c(OCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
44362013 35141 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cc(-c2ccccc2OCC2=NCCN2)sn1 10.1016/s0960-894x(01)00764-8
CHEMBL143766 35141 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cc(-c2ccccc2OCC2=NCCN2)sn1 10.1016/s0960-894x(01)00764-8
481 2836 5 None 8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
9838763 2836 5 None 8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
CHEMBL72958 2836 5 None 8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
10199335 203029 0 None 120 2 Human 7.8 pEC50 = 7.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74467 203029 0 None 120 2 Human 7.8 pEC50 = 7.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
44574834 172042 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.3 c1ccc2c(c1)CC(c1ncc[nH]1)C2 10.1016/j.bmcl.2009.03.162
CHEMBL449279 172042 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.3 c1ccc2c(c1)CC(c1ncc[nH]1)C2 10.1016/j.bmcl.2009.03.162
2146 3039 63 None -281 10 Rat 5.8 pEC50 = 5.8 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
485 3039 63 None -281 10 Rat 5.8 pEC50 = 5.8 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
6041 3039 63 None -281 10 Rat 5.8 pEC50 = 5.8 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
CHEMBL1215 3039 63 None -281 10 Rat 5.8 pEC50 = 5.8 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
DB00388 3039 63 None -281 10 Rat 5.8 pEC50 = 5.8 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
44449247 94957 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.8 COc1c(C)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL256984 94957 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.8 COc1c(C)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44571843 178731 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 2.7 COCCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL473425 178731 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 2.7 COCCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44571937 188949 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 282 3 1 3 2.9 Fc1ccn(Cc2cccc3c2CCC3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
CHEMBL514333 188949 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 282 3 1 3 2.9 Fc1ccn(Cc2cccc3c2CCC3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
9794803 10888 2 None 4 3 Human 7.8 pEC50 = 7.8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL117381 10888 2 None 4 3 Human 7.8 pEC50 = 7.8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44449692 156431 0 None 8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 1 3 3.1 c1cc(-c2ncco2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL407308 156431 0 None 8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 1 3 3.1 c1cc(-c2ncco2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
44281493 99521 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@H]1NCCCC21 10.1021/jm00144a012
CHEMBL286702 99521 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@H]1NCCCC21 10.1021/jm00144a012
44574106 177841 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 3 1 3 3.3 CNC(=O)c1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL466012 177841 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 3 1 3 3.3 CNC(=O)c1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44574107 188164 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL505414 188164 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
44574935 172043 0 None 19 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL449284 172043 0 None 19 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
9794803 10888 2 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL117381 10888 2 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
9859855 60063 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 254 4 2 4 2.1 Cn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17492 60063 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 254 4 2 4 2.1 Cn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
124 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
2032 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
4636 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
CHEMBL762 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
DB00935 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
22493320 4125 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 4 2 4 0.8 CN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL100198 4125 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 4 2 4 0.8 CN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44329481 4153 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 289 7 2 5 2.4 CCC(CC)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL100383 4153 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 289 7 2 5 2.4 CCC(CC)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
10378649 108093 0 None 15 3 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 7 3 4 1.6 CCCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL320419 108093 0 None 15 3 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 7 3 4 1.6 CCCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
124 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
2032 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
4636 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
CHEMBL762 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
DB00935 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
11811395 202985 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 281 5 2 5 1.3 CC(C)S(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74071 202985 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 281 5 2 5 1.3 CC(C)S(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44571844 171977 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 295 4 2 2 3.1 FC(F)(F)CNCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL448510 171977 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 295 4 2 2 3.1 FC(F)(F)CNCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
22493367 65839 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 298 7 2 6 2.2 CCCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL18436 65839 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 298 7 2 6 2.2 CCCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44574075 171998 0 None 72 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 0 4 2.9 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL448802 171998 0 None 72 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 0 4 2.9 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
44369351 119084 0 None 2 3 Human 8.7 pEC50 = 8.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 4 2.8 c1csc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL346380 119084 0 None 2 3 Human 8.7 pEC50 = 8.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 4 2.8 c1csc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
11140347 202818 0 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72768 202818 0 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
44362196 34250 1 None 7 3 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2nccs2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142871 34250 1 None 7 3 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2nccs2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44362288 35386 1 None 251 2 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1ccc(-c2cnccn2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL143973 35386 1 None 251 2 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1ccc(-c2cnccn2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
9881853 98009 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 5 2 4 2.6 CCn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL275902 98009 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 5 2 4 2.6 CCn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
10198532 205952 0 None 1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 232 4 3 4 0.5 CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL95523 205952 0 None 1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 232 4 3 4 0.5 CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44369434 45110 0 None 17 2 Human 8.6 pEC50 = 8.6 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 255 4 2 4 2.7 Cc1ccc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
CHEMBL152725 45110 0 None 17 2 Human 8.6 pEC50 = 8.6 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 255 4 2 4 2.7 Cc1ccc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
9947861 202452 0 None 21 3 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70634 202452 0 None 21 3 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
124 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
2032 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
4636 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
CHEMBL762 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
DB00935 2921 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
10422033 120449 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 246 5 2 5 1.5 CO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL356195 120449 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 246 5 2 5 1.5 CO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44281250 114295 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@@H]1NCCCC21 10.1021/jm00144a012
CHEMBL33405 114295 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@@H]1NCCCC21 10.1021/jm00144a012
44449691 95702 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1cncc(-c2cccc3c2CCC3c2ncc[nH]2)c1 10.1016/j.bmcl.2008.03.070
CHEMBL260576 95702 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1cncc(-c2cccc3c2CCC3c2ncc[nH]2)c1 10.1016/j.bmcl.2008.03.070
4038180 202 11 None -2 5 Human 7.7 pEC50 = 7.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
480 202 11 None -2 5 Human 7.7 pEC50 = 7.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
CHEMBL109783 202 11 None -2 5 Human 7.7 pEC50 = 7.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
44449278 95195 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257977 95195 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
1960 2805 64 None -23 13 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
439260 2805 64 None -23 13 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
505 2805 64 None -23 13 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
CHEMBL1437 2805 64 None -23 13 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
DB00368 2805 64 None -23 13 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
10135864 121990 0 None -10 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601200 121990 0 None -10 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
44574937 178075 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL467688 178075 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
44449276 95194 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 241 2 2 2 1.8 CNC(=O)c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257976 95194 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 241 2 2 2 1.8 CNC(=O)c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
11090351 162827 0 None 20 2 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL419448 162827 0 None 20 2 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
44449278 95195 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257977 95195 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44593577 177879 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466296 177879 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
10221004 202521 0 None 20 2 Human 6.6 pEC50 = 6.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70973 202521 0 None 20 2 Human 6.6 pEC50 = 6.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
22493356 46732 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 266 4 2 4 2.5 Cc1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL154170 46732 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 266 4 2 4 2.5 Cc1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
10804826 23397 1 None 1 2 Human 4.6 pEC50 = 4.6 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL133451 23397 1 None 1 2 Human 4.6 pEC50 = 4.6 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
216249 1273 44 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 10.1016/j.bmcl.2008.03.070
3469 1273 44 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 10.1016/j.bmcl.2008.03.070
CHEMBL257978 1273 44 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 10.1016/j.bmcl.2008.03.070
10423384 34358 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 272 4 1 4 3.1 Cc1ccc(-c2ccccc2OCC2=NCCN2)s1 10.1016/s0960-894x(01)00764-8
CHEMBL142958 34358 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 272 4 1 4 3.1 Cc1ccc(-c2ccccc2OCC2=NCCN2)s1 10.1016/s0960-894x(01)00764-8
10084685 118918 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1csc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
CHEMBL344957 118918 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1csc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
10221066 162600 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
CHEMBL417999 162600 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
44271931 97928 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 283 6 2 5 2.4 CCCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL275386 97928 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 283 6 2 5 2.4 CCCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
10180440 121991 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 4 7 1.6 COc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601201 121991 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 4 7 1.6 COc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
2683 3762 57 None -1 3 Bovine 6.6 pEC50 = 6.6 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
5487 3762 57 None -1 3 Bovine 6.6 pEC50 = 6.6 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
7308 3762 57 None -1 3 Bovine 6.6 pEC50 = 6.6 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
CHEMBL1079 3762 57 None -1 3 Bovine 6.6 pEC50 = 6.6 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
DB00697 3762 57 None -1 3 Bovine 6.6 pEC50 = 6.6 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
44574138 177920 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(C2Cc3nccn3C2)c(-n2cccn2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL466635 177920 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(C2Cc3nccn3C2)c(-n2cccn2)c1 10.1016/j.bmcl.2009.03.166
44593557 183326 7 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
CHEMBL481322 183326 7 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
44574874 177808 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL465599 177808 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
122184771 121992 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 434 11 4 7 2.0 CCOc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601202 121992 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 434 11 4 7 2.0 CCOc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
44449723 155581 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 1 3 2.9 Cn1nccc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL406348 155581 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 1 3 2.9 Cn1nccc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
124 2921 44 None -52 21 Rat 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
2032 2921 44 None -52 21 Rat 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
4636 2921 44 None -52 21 Rat 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
CHEMBL762 2921 44 None -52 21 Rat 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
DB00935 2921 44 None -52 21 Rat 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
2146 3039 63 None -35 10 Human 5.5 pEC50 = 5.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
485 3039 63 None -35 10 Human 5.5 pEC50 = 5.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
6041 3039 63 None -35 10 Human 5.5 pEC50 = 5.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
CHEMBL1215 3039 63 None -35 10 Human 5.5 pEC50 = 5.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
DB00388 3039 63 None -35 10 Human 5.5 pEC50 = 5.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
44574134 177919 0 None 91 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(-c2ncco2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL466634 177919 0 None 91 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(-c2ncco2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44574077 178173 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 0 4 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2nccs2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL468710 178173 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 0 4 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2nccs2)c1 10.1016/j.bmcl.2009.03.166
44574136 188444 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(-c2ccn[nH]2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL509350 188444 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(-c2ccn[nH]2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44449725 95730 0 None 208 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 2 2 3.2 Cc1n[nH]cc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL260720 95730 0 None 208 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 2 2 3.2 Cc1n[nH]cc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44269124 28590 1 None 23 3 Human 8.5 pEC50 = 8.5 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(02)00753-9
CHEMBL13789 28590 1 None 23 3 Human 8.5 pEC50 = 8.5 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(02)00753-9
44269124 28590 1 None 23 3 Human 8.5 pEC50 = 8.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
CHEMBL13789 28590 1 None 23 3 Human 8.5 pEC50 = 8.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
10060965 34993 1 None 39 3 Human 8.5 pEC50 = 8.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 4 2.6 Cc1ccoc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL143562 34993 1 None 39 3 Human 8.5 pEC50 = 8.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 4 2.6 Cc1ccoc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
9816515 62634 0 None 5 3 Human 8.5 pEC50 = 8.5 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
CHEMBL17856 62634 0 None 5 3 Human 8.5 pEC50 = 8.5 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
44329797 107607 0 None 67 3 Human 8.5 pEC50 = 8.5 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 261 5 2 5 1.7 CC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL319553 107607 0 None 67 3 Human 8.5 pEC50 = 8.5 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 261 5 2 5 1.7 CC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
10244367 49758 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CC/C(=N\OC)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL156950 49758 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CC/C(=N\OC)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
11000184 12926 0 None 4 5 Human 8.5 pEC50 = 8.5 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1190038 12926 0 None 4 5 Human 8.5 pEC50 = 8.5 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540035 12926 0 None 4 5 Human 8.5 pEC50 = 8.5 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
44343247 110133 0 None 15 3 Human 8.4 pEC50 = 8.4 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 6 3 3 2.2 CCCNC(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL325745 110133 0 None 15 3 Human 8.4 pEC50 = 8.4 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 6 3 3 2.2 CCCNC(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
15959112 201829 0 None -1 2 Rat 5.5 pEC50 = 5.5 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 280 2 1 5 2.7 Oc1nnc(Cc2ccc3c(c2)OCO3)c2ccccc12 10.1016/j.bmcl.2006.02.003
CHEMBL66433 201829 0 None -1 2 Rat 5.5 pEC50 = 5.5 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 280 2 1 5 2.7 Oc1nnc(Cc2ccc3c(c2)OCO3)c2ccccc12 10.1016/j.bmcl.2006.02.003
11264016 99172 2 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 193 2 1 3 1.1 COc1ccc(OC)c2c1CC(N)C2 10.1021/jm00144a012
CHEMBL284307 99172 2 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 193 2 1 3 1.1 COc1ccc(OC)c2c1CC(N)C2 10.1021/jm00144a012
44281507 99452 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@@H](N)C1 10.1021/jm00144a012
CHEMBL286226 99452 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@@H](N)C1 10.1021/jm00144a012
44280965 99508 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@H](N)C1 10.1021/jm00144a012
CHEMBL286609 99508 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@H](N)C1 10.1021/jm00144a012
10804826 23397 1 None -1 2 Rat 4.5 pEC50 = 4.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL133451 23397 1 None -1 2 Rat 4.5 pEC50 = 4.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
44593557 183326 7 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.166
CHEMBL481322 183326 7 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.166
44593557 183326 7 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL481322 183326 7 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
9816986 163576 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL421011 163576 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
9816986 163576 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL421011 163576 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00764-8
9816986 163576 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL421011 163576 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44593577 177879 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466296 177879 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
481 2836 5 None 8 2 Human 6.5 pEC50 = 6.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1016/s0960-894x(01)00764-8
9838763 2836 5 None 8 2 Human 6.5 pEC50 = 6.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1016/s0960-894x(01)00764-8
CHEMBL72958 2836 5 None 8 2 Human 6.5 pEC50 = 6.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1016/s0960-894x(01)00764-8
22493344 98196 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 323 5 2 5 2.5 FC(F)(F)Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL277361 98196 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 323 5 2 5 2.5 FC(F)(F)Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44449277 154632 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 1 2 2.5 COc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL402388 154632 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 1 2 2.5 COc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449305 155058 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL404566 155058 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44571889 183437 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 264 3 1 3 2.7 c1cc(Cn2cccn2)c2c(c1)[C@H](c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.10.066
CHEMBL482148 183437 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 264 3 1 3 2.7 c1cc(Cn2cccn2)c2c(c1)[C@H](c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.10.066
44449337 154565 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1ccn[nH]1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL402003 154565 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1ccn[nH]1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
22493272 44487 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1nc(-c2ccccc2NCC2=NCCN2)co1 10.1016/s0960-894x(01)00822-8
CHEMBL152154 44487 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1nc(-c2ccccc2NCC2=NCCN2)co1 10.1016/s0960-894x(01)00822-8
44574133 187782 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(C2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL501404 187782 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(C2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
122184835 122013 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 5 7 1.1 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(CO)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601310 122013 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 5 7 1.1 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(CO)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
44449249 94741 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 Cc1ccc2c(c1NS(C)(=O)=O)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL255938 94741 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 Cc1ccc2c(c1NS(C)(=O)=O)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
10420352 168164 10 None -83 2 Human 5.5 pEC50 = 5.5 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
CHEMBL43711 168164 10 None -83 2 Human 5.5 pEC50 = 5.5 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
44280982 99290 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 205 2 1 3 1.3 COc1ccc(OC)c2c1CC1C2[C@@H]1N 10.1021/jm00144a012
CHEMBL285082 99290 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 205 2 1 3 1.3 COc1ccc(OC)c2c1CC1C2[C@@H]1N 10.1021/jm00144a012
124 2921 44 None -26 21 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
2032 2921 44 None -26 21 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
4636 2921 44 None -26 21 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
CHEMBL762 2921 44 None -26 21 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
DB00935 2921 44 None -26 21 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
44574936 178044 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL467495 178044 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
44369646 119645 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccc(-c2ccccc2NCC2=NCCN2)s1 10.1016/s0960-894x(01)00822-8
CHEMBL351543 119645 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccc(-c2ccccc2NCC2=NCCN2)s1 10.1016/s0960-894x(01)00822-8
44571841 178730 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 228 3 1 2 2.6 COCc1cccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL473424 178730 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 228 3 1 2 2.6 COCc1cccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44574988 188630 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 227 2 1 3 1.3 NC(=O)c1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL511576 188630 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 227 2 1 3 1.3 NC(=O)c1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
521 1372 64 None -104 4 Bovine 6.4 pEC50 = 6.4 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
5311068 1372 64 None -104 4 Bovine 6.4 pEC50 = 6.4 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
835 1372 64 None -104 4 Bovine 6.4 pEC50 = 6.4 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
CHEMBL778 1372 64 None -104 4 Bovine 6.4 pEC50 = 6.4 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
DB00633 1372 64 None -104 4 Bovine 6.4 pEC50 = 6.4 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
22493349 119169 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1cc(-c2ccccc2NCC2=NCCN2)on1 10.1016/s0960-894x(01)00822-8
CHEMBL347268 119169 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1cc(-c2ccccc2NCC2=NCCN2)on1 10.1016/s0960-894x(01)00822-8
17804479 95203 16 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.9 c1ccc2c(c1)CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL258007 95203 16 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.9 c1ccc2c(c1)CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
10083742 34368 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 5 1.5 Cn1nccc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL142967 34368 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 5 1.5 Cn1nccc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
44329739 111819 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 287 5 2 5 2.2 O=C(OC1CCCC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL329272 111819 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 287 5 2 5 2.2 O=C(OC1CCCC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
104452 201403 66 None -4 2 Rat 5.4 pEC50 = 5.4 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 270 2 1 3 3.6 Oc1nnc(Cc2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.02.003
CHEMBL63976 201403 66 None -4 2 Rat 5.4 pEC50 = 5.4 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 270 2 1 3 3.6 Oc1nnc(Cc2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.02.003
22493381 97618 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1cc(-c2ccccc2NCC2=NCCN2)cn1 10.1016/s0960-894x(03)00050-7
CHEMBL273312 97618 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1cc(-c2ccccc2NCC2=NCCN2)cn1 10.1016/s0960-894x(03)00050-7
22493231 205921 0 None -5 3 Human 6.4 pEC50 = 6.4 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 286 4 2 4 1.7 O=C(c1ccccc1NCC1=NCCN1)N1CCCCC1 10.1016/s0960-894x(01)00569-8
CHEMBL95333 205921 0 None -5 3 Human 6.4 pEC50 = 6.4 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 286 4 2 4 1.7 O=C(c1ccccc1NCC1=NCCN1)N1CCCCC1 10.1016/s0960-894x(01)00569-8
44574104 188889 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 353 4 1 4 3.3 CS(=O)(=O)Nc1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL513871 188889 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 353 4 1 4 3.3 CS(=O)(=O)Nc1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
9838376 167726 0 None 15 2 Human 8.4 pEC50 = 8.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 272 4 2 5 2.5 Cc1nc(-c2ccccc2NCC2=NCCN2)cs1 10.1016/s0960-894x(01)00822-8
CHEMBL434074 167726 0 None 15 2 Human 8.4 pEC50 = 8.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 272 4 2 5 2.5 Cc1nc(-c2ccccc2NCC2=NCCN2)cs1 10.1016/s0960-894x(01)00822-8
11108001 10756 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117248 10756 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540542 10756 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
9816460 119375 0 None 39 3 Human 8.3 pEC50 = 8.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1ccc(-c2cnccn2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL349082 119375 0 None 39 3 Human 8.3 pEC50 = 8.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1ccc(-c2cnccn2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
1028 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
139148732 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
479 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
5816 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
CHEMBL679 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
DB00668 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
11058166 202989 0 None 10 2 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74114 202989 0 None 10 2 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
44574986 188611 0 None 7 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 202 1 0 2 2.4 Fc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL511411 188611 0 None 7 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 202 1 0 2 2.4 Fc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
22493415 49688 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 268 4 3 6 1.1 Nc1nccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
CHEMBL156893 49688 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 268 4 3 6 1.1 Nc1nccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
44449686 95625 0 None 7 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 1 3 3.6 c1cc(-c2nccs2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL260116 95625 0 None 7 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 1 3 3.6 c1cc(-c2nccs2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
25066019 94955 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL256982 94955 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
25066019 94955 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
CHEMBL256982 94955 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
25066019 94955 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL256982 94955 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
11079593 202406 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70326 202406 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
15959119 76688 0 None -1 2 Rat 5.4 pEC50 = 5.4 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 310 4 0 3 3.8 C=CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
CHEMBL207277 76688 0 None -1 2 Rat 5.4 pEC50 = 5.4 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 310 4 0 3 3.8 C=CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
44369647 46928 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnoc2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL154346 46928 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnoc2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44449248 94740 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 248 2 1 2 3.2 COc1c(Cl)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL255937 94740 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 248 2 1 2 3.2 COc1c(Cl)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449338 95234 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL258178 95234 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449338 95234 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
CHEMBL258178 95234 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
44593580 177957 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL466876 177957 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
11747739 13109 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1191324 13109 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL542402 13109 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44574103 172009 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 0 4 2.4 c1ccc(-n2cccn2)c([C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL448908 172009 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 0 4 2.4 c1ccc(-n2cccn2)c([C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44574137 188491 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(-n2cccn2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL510023 188491 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(-n2cccn2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
11108001 10756 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL117248 10756 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL540542 10756 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
44362149 33695 0 None 2 3 Human 8.3 pEC50 = 8.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2ccns2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142387 33695 0 None 2 3 Human 8.3 pEC50 = 8.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2ccns2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44362150 118872 0 None 15 2 Human 8.3 pEC50 = 8.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2cc[nH]n2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL344551 118872 0 None 15 2 Human 8.3 pEC50 = 8.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2cc[nH]n2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
10859076 13555 0 None 5 4 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1194763 13555 0 None 5 4 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL553276 13555 0 None 5 4 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
6604803 116005 2 None 1 4 Rat 8.3 pEC50 = 8.3 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL336161 116005 2 None 1 4 Rat 8.3 pEC50 = 8.3 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
6604803 116005 2 None -1 4 Human 8.3 pEC50 = 8.3 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL336161 116005 2 None -1 4 Human 8.3 pEC50 = 8.3 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
4038180 202 11 None 1 5 Rat 8.2 pEC50 = 8.2 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
480 202 11 None 1 5 Rat 8.2 pEC50 = 8.2 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
CHEMBL109783 202 11 None 1 5 Rat 8.2 pEC50 = 8.2 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
9816461 10604 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL117094 10604 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL544290 10604 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
44343245 110113 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 256 4 2 3 3.0 c1ccc(N2CCCCC2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL325648 110113 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 256 4 2 3 3.0 c1ccc(N2CCCCC2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
44343275 110272 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 240 4 2 4 2.7 c1ccc(-c2cnco2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL326067 110272 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 240 4 2 4 2.7 c1ccc(-c2cnco2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
22493233 168710 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 4 2 4 2.4 Cc1ccc(-c2ccccc2NCC2=NCCN2)n1C 10.1016/s0960-894x(03)00050-7
CHEMBL441412 168710 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 4 2 4 2.4 Cc1ccc(-c2ccccc2NCC2=NCCN2)n1C 10.1016/s0960-894x(03)00050-7
9903313 172099 0 None 5 3 Human 7.3 pEC50 = 7.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 2 4 1.2 CCN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL450018 172099 0 None 5 3 Human 7.3 pEC50 = 7.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 2 4 1.2 CCN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493379 206375 0 None 2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 3 4 1.2 CC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL98016 206375 0 None 2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 3 4 1.2 CC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493411 167456 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.6 CCC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL432192 167456 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.6 CCC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44329701 205934 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 1.9 CC(C)COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL95398 205934 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 1.9 CC(C)COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44574044 177846 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
CHEMBL466046 177846 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
44219719 178092 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL467916 178092 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
10399043 119644 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 232 5 2 5 1.1 CO/N=C/c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL351542 119644 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 232 5 2 5 1.1 CO/N=C/c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
10916464 202443 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1cc(Cl)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70563 202443 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1cc(Cl)ccc1NCC1=NCCN1 10.1021/jm000542r
44574875 188048 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
CHEMBL503269 188048 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
44449245 94956 0 None 6 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2ccn[nH]2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL256983 94956 0 None 6 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2ccn[nH]2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
22493347 119094 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CCO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL346465 119094 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CCO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44281057 99201 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 221 2 1 3 1.9 COc1ccc(OC)c2c1CCCC(N)C2 10.1021/jm00144a012
CHEMBL284486 99201 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 221 2 1 3 1.9 COc1ccc(OC)c2c1CCCC(N)C2 10.1021/jm00144a012
9816461 10604 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117094 10604 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL544290 10604 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44574938 188317 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1cccc(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.162
CHEMBL507755 188317 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1cccc(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.162
44571888 183325 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1cc(F)cc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL481321 183325 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1cc(F)cc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44343244 9843 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 3 3 4 2.0 Oc1ccc2cccc(NCC3=NCCN3)c2c1 10.1016/s0960-894x(02)00753-9
CHEMBL114669 9843 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 3 3 4 2.0 Oc1ccc2cccc(NCC3=NCCN3)c2c1 10.1016/s0960-894x(02)00753-9
44343236 110863 0 None 15 3 Human 8.2 pEC50 = 8.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 243 4 1 5 1.7 c1ccc(-c2ccno2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL327005 110863 0 None 15 3 Human 8.2 pEC50 = 8.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 243 4 1 5 1.7 c1ccc(-c2ccno2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
9903932 59183 0 None 501 2 Human 8.2 pEC50 = 8.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 5 2 6 1.9 CC(C)n1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17151 59183 0 None 501 2 Human 8.2 pEC50 = 8.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 5 2 6 1.9 CC(C)n1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44271932 64865 0 None 6 3 Human 8.2 pEC50 = 8.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL18256 64865 0 None 6 3 Human 8.2 pEC50 = 8.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
22493392 46876 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 252 4 2 4 2.2 c1ccc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
CHEMBL154298 46876 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 252 4 2 4 2.2 c1ccc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
9838192 110811 13 None -2 3 Rabbit 7.2 pEC50 = 7.2 Functional
Agonist activity at rabbit urethra adrenergic alpha1A receptorAgonist activity at rabbit urethra adrenergic alpha1A receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmc.2008.02.091
CHEMBL326702 110811 13 None -2 3 Rabbit 7.2 pEC50 = 7.2 Functional
Agonist activity at rabbit urethra adrenergic alpha1A receptorAgonist activity at rabbit urethra adrenergic alpha1A receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmc.2008.02.091
122184772 121993 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 424 9 4 6 2.3 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(Cl)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601203 121993 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 424 9 4 6 2.3 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(Cl)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
44574132 178004 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1cccc(-c2cncnc2)c1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
CHEMBL467259 178004 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1cccc(-c2cncnc2)c1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
44571842 178682 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 3.0 CCOCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL473043 178682 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 3.0 CCOCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44571887 187822 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1c(F)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL502078 187822 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1c(F)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44343243 9737 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 239 3 3 3 2.9 Oc1ccc2cccc(NCc3c[nH]cn3)c2c1 10.1016/s0960-894x(02)00753-9
CHEMBL114054 9737 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 239 3 3 3 2.9 Oc1ccc2cccc(NCc3c[nH]cn3)c2c1 10.1016/s0960-894x(02)00753-9
44343173 10903 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 272 6 2 3 2.5 CCN(CC)C(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL117482 10903 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 272 6 2 3 2.5 CCN(CC)C(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
9838294 59346 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17221 59346 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
11079 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
3369 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
4436 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
5509 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
CHEMBL761 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
DB06711 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
11079 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
3369 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
4436 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
5509 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
CHEMBL761 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
DB06711 2683 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
25154770 183060 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1ccc(F)c2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL480272 183060 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1ccc(F)c2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
22493325 119244 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1noc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
CHEMBL347920 119244 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1noc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
22493287 119575 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 320 4 2 4 3.2 FC(F)(F)c1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL350906 119575 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 320 4 2 4 3.2 FC(F)(F)c1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
11097789 102511 0 None -1 5 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL306792 102511 0 None -1 5 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
11140345 202461 0 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70692 202461 0 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
9795167 106995 0 None 6 3 Human 8.1 pEC50 = 8.1 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL318544 106995 0 None 6 3 Human 8.1 pEC50 = 8.1 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
44352155 116295 0 None 7 5 Human 8.1 pEC50 = 8.1 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 251 4 2 3 2.8 c1ccc(-c2ccccc2NCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
CHEMBL337862 116295 0 None 7 5 Human 8.1 pEC50 = 8.1 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 251 4 2 3 2.8 c1ccc(-c2ccccc2NCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
9795167 106995 0 None 6 3 Human 8.1 pEC50 = 8.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL318544 106995 0 None 6 3 Human 8.1 pEC50 = 8.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44329703 206411 0 None 7 2 Human 8.1 pEC50 = 8.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 4 2 5 2.1 CC(C)(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL98243 206411 0 None 7 2 Human 8.1 pEC50 = 8.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 4 2 5 2.1 CC(C)(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44449304 95148 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 277 3 2 3 1.9 CS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257800 95148 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 277 3 2 3 1.9 CS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
12764879 177838 0 None 100 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL465963 177838 0 None 100 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
172745 99648 7 None -234 2 Human 4.2 pEC50 = 4.2 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
CHEMBL287587 99648 7 None -234 2 Human 4.2 pEC50 = 4.2 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
1753 2458 26 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
483 2458 26 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
6082 2458 26 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
CHEMBL524 2458 26 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
DB00723 2458 26 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
12764880 177961 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 0 2 2.6 c1ccc(C2CCc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466914 177961 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 0 2 2.6 c1ccc(C2CCc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
22493359 121161 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1nc(-c2ccccc2NCC2=NCCN2)no1 10.1016/s0960-894x(01)00822-8
CHEMBL358685 121161 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1nc(-c2ccccc2NCC2=NCCN2)no1 10.1016/s0960-894x(01)00822-8
12764879 177838 0 None 100 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL465963 177838 0 None 100 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
44593580 177957 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL466876 177957 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
44449303 95147 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257799 95147 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449303 95147 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL257799 95147 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
9840212 61777 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 324 5 2 6 1.9 FC(F)(F)Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17764 61777 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 324 5 2 6 1.9 FC(F)(F)Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44329133 205957 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.5 CC(C)CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL95565 205957 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.5 CC(C)CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493408 60856 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 3 5 1.2 Cc1n[nH]c(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
CHEMBL17657 60856 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 3 5 1.2 Cc1n[nH]c(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
541604 164776 10 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm00118a019
CHEMBL42359 164776 10 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm00118a019
44574079 188710 0 None 8 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 0 3 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ccncc2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL512289 188710 0 None 8 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 0 3 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ccncc2)c1 10.1016/j.bmcl.2009.03.166
11522042 201975 1 None -1 2 Rat 6.1 pEC50 = 6.1 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 284 2 0 3 3.2 Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
CHEMBL67457 201975 1 None -1 2 Rat 6.1 pEC50 = 6.1 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 284 2 0 3 3.2 Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
45381933 122011 0 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 458 9 4 6 2.7 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C(F)(F)F)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601308 122011 0 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 458 9 4 6 2.7 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C(F)(F)F)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
44574989 188631 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 3 0 3 2.4 COCc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL511577 188631 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 3 0 3 2.4 COCc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
12764879 177838 0 None 100 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL465963 177838 0 None 100 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
44571840 187621 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 276 3 1 3 2.0 CS(=O)(=O)Cc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL499180 187621 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 276 3 1 3 2.0 CS(=O)(=O)Cc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
45381852 121994 0 None -60 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 418 10 4 6 2.2 CCc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601204 121994 0 None -60 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 418 10 4 6 2.2 CCc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
22493254 168511 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CC/C(=N/OC)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL439822 168511 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CC/C(=N/OC)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44571845 188535 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 289 3 1 2 2.9 FC1(F)CN(Cc2cccc3c2CCC3c2ncc[nH]2)C1 10.1016/j.bmcl.2008.10.066
CHEMBL510613 188535 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 289 3 1 2 2.9 FC1(F)CN(Cc2cccc3c2CCC3c2ncc[nH]2)C1 10.1016/j.bmcl.2008.10.066
2803 939 53 None -6 11 Bovine 7.1 pEC50 = 7.1 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
516 939 53 None -6 11 Bovine 7.1 pEC50 = 7.1 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
704 939 53 None -6 11 Bovine 7.1 pEC50 = 7.1 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
CHEMBL134 939 53 None -6 11 Bovine 7.1 pEC50 = 7.1 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
DB00575 939 53 None -6 11 Bovine 7.1 pEC50 = 7.1 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
2146 3039 63 None -1 10 Bovine 8.1 pEC50 = 8.1 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
485 3039 63 None -1 10 Bovine 8.1 pEC50 = 8.1 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
6041 3039 63 None -1 10 Bovine 8.1 pEC50 = 8.1 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
CHEMBL1215 3039 63 None -1 10 Bovine 8.1 pEC50 = 8.1 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
DB00388 3039 63 None -1 10 Bovine 8.1 pEC50 = 8.1 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
44574080 188349 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 0 4 2.6 Cn1cc(-c2ccccc2[C@@H]2Cc3nccn3C2)cn1 10.1016/j.bmcl.2009.03.166
CHEMBL508084 188349 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 0 4 2.6 Cn1cc(-c2ccccc2[C@@H]2Cc3nccn3C2)cn1 10.1016/j.bmcl.2009.03.166
9838192 110811 13 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmcl.2008.03.070
CHEMBL326702 110811 13 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmcl.2008.03.070
44571938 179483 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 300 3 1 3 3.0 Fc1ccn(Cc2c(F)ccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
CHEMBL474796 179483 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 300 3 1 3 3.0 Fc1ccn(Cc2c(F)ccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
1960 2805 64 None -23 13 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jmedchem.5b00638
439260 2805 64 None -23 13 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jmedchem.5b00638
505 2805 64 None -23 13 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jmedchem.5b00638
CHEMBL1437 2805 64 None -23 13 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jmedchem.5b00638
DB00368 2805 64 None -23 13 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jmedchem.5b00638
44571890 191369 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 265 3 1 4 2.1 c1cc(Cn2ccnn2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.10.066
CHEMBL520117 191369 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 265 3 1 4 2.1 c1cc(Cn2ccnn2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.10.066
44574076 171884 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 0 4 2.9 c1ccc([C@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL448147 171884 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 0 4 2.9 c1ccc([C@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
44574985 187813 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL501920 187813 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
123562321 139968 0 None 1 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 443 12 3 6 2.9 COc1ccc(F)cc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3810110 139968 0 None 1 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 443 12 3 6 2.9 COc1ccc(F)cc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
129211 3680 75 None 1 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2020.112616
2562 3680 75 None 1 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2020.112616
488 3680 75 None 1 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2020.112616
CHEMBL836 3680 75 None 1 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2020.112616
DB00706 3680 75 None 1 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2020.112616
499 4002 15 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levelsAntagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levels
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.ejmech.2014.12.045
5685 4002 15 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levelsAntagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levels
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.ejmech.2014.12.045
CHEMBL25554 4002 15 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levelsAntagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levels
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.ejmech.2014.12.045
499 4002 15 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ release
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm401895u
5685 4002 15 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ release
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm401895u
CHEMBL25554 4002 15 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ release
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm401895u
123854385 139973 0 None 72 3 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 527 13 3 6 4.3 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3810145 139973 0 None 72 3 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 527 13 3 6 4.3 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
4151 3537 85 None 1 5 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
493 3537 85 None 1 5 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
5312125 3537 85 None 1 5 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
CHEMBL24778 3537 85 None 1 5 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
DB06207 3537 85 None 1 5 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
4151 3537 85 None 1 5 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.5b02023
493 3537 85 None 1 5 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.5b02023
5312125 3537 85 None 1 5 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.5b02023
CHEMBL24778 3537 85 None 1 5 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.5b02023
DB06207 3537 85 None 1 5 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.5b02023
9913616 139840 4 None 8 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 493 13 3 6 3.7 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3808572 139840 4 None 8 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 493 13 3 6 3.7 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
10160408 139897 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 13 3 6 3.1 CCOc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809248 139897 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 13 3 6 3.1 CCOc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
86344174 139925 0 None 251 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCN[C@H](C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809490 139925 0 None 251 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCN[C@H](C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
2389 3267 114 None -10 23 Human 8.0 pIC50 = 8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
5073 3267 114 None -10 23 Human 8.0 pIC50 = 8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
96 3267 114 None -10 23 Human 8.0 pIC50 = 8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
CHEMBL85 3267 114 None -10 23 Human 8.0 pIC50 = 8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
DB00734 3267 114 None -10 23 Human 8.0 pIC50 = 8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
2389 3267 114 None -10 23 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
5073 3267 114 None -10 23 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
96 3267 114 None -10 23 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
CHEMBL85 3267 114 None -10 23 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
DB00734 3267 114 None -10 23 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
145946682 167002 0 None -10 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 444 7 0 3 5.6 Fc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4225239 167002 0 None -10 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 444 7 0 3 5.6 Fc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4300633 167002 0 None -10 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 444 7 0 3 5.6 Fc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
145964299 163569 0 None -1 6 Human 8.0 pIC50 = 8.0 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 426 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4210030 163569 0 None -1 6 Human 8.0 pIC50 = 8.0 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 426 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
76071739 142253 0 None -25 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@H]1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3892879 142253 0 None -25 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@H]1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
145946986 167033 0 None -4 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 460 7 0 3 6.2 Clc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
CHEMBL4227241 167033 0 None -4 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 460 7 0 3 6.2 Clc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
CHEMBL4300995 167033 0 None -4 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 460 7 0 3 6.2 Clc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
145990794 166236 0 None -19 6 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4284346 166236 0 None -19 6 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
131978695 150316 0 None 5 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 440 5 1 4 5.4 COc1ccc2[nH]c3c(c2c1)CC1c2cc(OCc4ccccc4)c(OC)cc2CCN1C3 10.1021/acs.jmedchem.6b01217
CHEMBL3957222 150316 0 None 5 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 440 5 1 4 5.4 COc1ccc2[nH]c3c(c2c1)CC1c2cc(OCc4ccccc4)c(OC)cc2CCN1C3 10.1021/acs.jmedchem.6b01217
134138882 147183 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 0 1 3 3.6 c1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3932187 147183 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 0 1 3 3.6 c1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
44575544 173416 0 None -3 4 Human 7.9 pIC50 = 7.9 Functional
Inhibition of adrenergic receptor 1a expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetryInhibition of adrenergic receptor 1a expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetry
ChEMBL 794 5 5 13 3.0 CC(C)CC(=O)O[C@H]1/C=C/C=C/C(=O)O[C@H]2[C@@H](C)C[C@@H]3[C@]2(O)[C@H](O)[C@@]2(CO)O[C@H]2[C@H]2[C@H]4OC5(c6ccccc6)O[C@@H]([C@@H](C)[C@@]23O5)[C@@]4(O)[C@](C)(O)C[C@H]2CC[C@H]1[C@H]2C 10.1021/np3000359
CHEMBL454246 173416 0 None -3 4 Human 7.9 pIC50 = 7.9 Functional
Inhibition of adrenergic receptor 1a expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetryInhibition of adrenergic receptor 1a expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetry
ChEMBL 794 5 5 13 3.0 CC(C)CC(=O)O[C@H]1/C=C/C=C/C(=O)O[C@H]2[C@@H](C)C[C@@H]3[C@]2(O)[C@H](O)[C@@]2(CO)O[C@H]2[C@H]2[C@H]4OC5(c6ccccc6)O[C@@H]([C@@H](C)[C@@]23O5)[C@@]4(O)[C@](C)(O)C[C@H]2CC[C@H]1[C@H]2C 10.1021/np3000359
127044893 139865 0 None 2 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 411 11 3 5 2.4 Cc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3808878 139865 0 None 2 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 411 11 3 5 2.4 Cc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
134157118 153656 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 332 0 0 4 3.6 Cn1c2c(c3ccccc31)CC1c3cc4c(cc3CCN1C2)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3985901 153656 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 332 0 0 4 3.6 Cn1c2c(c3ccccc31)CC1c3cc4c(cc3CCN1C2)OCO4 10.1021/acs.jmedchem.6b01217
123141715 139992 0 None 2 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 459 12 3 6 3.4 COc1cc(Cl)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3810401 139992 0 None 2 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 459 12 3 6 3.4 COc1cc(Cl)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
44347716 16117 0 None -3 3 Rat 4.8 pIC50 = 4.8 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 590 27 4 8 6.3 COc1cccc(CNCCCCCCNCCSSCCNCCCCCCNCc2ccccc2OC)c1 10.1021/jm000995w
CHEMBL122621 16117 0 None -3 3 Rat 4.8 pIC50 = 4.8 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 590 27 4 8 6.3 COc1cccc(CNCCCCCCNCCSSCCNCCCCCCNCc2ccccc2OC)c1 10.1021/jm000995w
145966333 163497 0 None -134 6 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4209188 163497 0 None -134 6 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
123986550 139855 0 None 223 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 521 14 3 6 4.2 CCc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3808717 139855 0 None 223 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 521 14 3 6 4.2 CCc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
134142282 145145 0 None 2 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3916182 145145 0 None 2 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
242 467 117 None -50 12 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
34 467 117 None -50 12 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
60795 467 117 None -50 12 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
CHEMBL1112 467 117 None -50 12 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
DB01238 467 117 None -50 12 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
242 467 117 None -50 12 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
34 467 117 None -50 12 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
60795 467 117 None -50 12 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
CHEMBL1112 467 117 None -50 12 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
DB01238 467 117 None -50 12 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
145983928 165848 0 None -48 6 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4277101 165848 0 None -48 6 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
10820251 96161 0 None -208 3 Rat 5.7 pIC50 = 5.7 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCNCCSSCCNCCCCCCNCc3ccccc3C(=O)N(C)CCCCCCN(C)c3nc(N)c4cc(OC)c(OC)cc4n3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL1203233 96161 0 None -208 3 Rat 5.7 pIC50 = 5.7 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCNCCSSCCNCCCCCCNCc3ccccc3C(=O)N(C)CCCCCCN(C)c3nc(N)c4cc(OC)c(OC)cc4n3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL263434 96161 0 None -208 3 Rat 5.7 pIC50 = 5.7 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCNCCSSCCNCCCCCCNCc3ccccc3C(=O)N(C)CCCCCCN(C)c3nc(N)c4cc(OC)c(OC)cc4n3)nc(N)c2cc1OC 10.1021/jm000995w
10606263 141007 0 None -81 3 Rat 5.7 pIC50 = 5.7 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4ccc(CNCCCCCCNCCSSCCNCCCCCCNCc5ccc(C(=O)N6CCN(c7nc(N)c8cc(OC)c(OC)cc8n7)CC6)cc5)cc4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL384790 141007 0 None -81 3 Rat 5.7 pIC50 = 5.7 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4ccc(CNCCCCCCNCCSSCCNCCCCCCNCc5ccc(C(=O)N6CCN(c7nc(N)c8cc(OC)c(OC)cc8n7)CC6)cc5)cc4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
123472560 139951 0 None 616 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809840 139951 0 None 616 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
129211 3680 75 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/acs.jmedchem.6b01217
2562 3680 75 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/acs.jmedchem.6b01217
488 3680 75 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/acs.jmedchem.6b01217
CHEMBL836 3680 75 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/acs.jmedchem.6b01217
DB00706 3680 75 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/acs.jmedchem.6b01217
123415538 139834 0 None 8 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 491 11 3 5 3.6 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccc(F)cc1Br 10.1021/acs.jmedchem.5b02023
CHEMBL3808511 139834 0 None 8 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 491 11 3 5 3.6 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccc(F)cc1Br 10.1021/acs.jmedchem.5b02023
123667086 139856 0 None -8 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 573 13 3 6 3.8 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Br)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3808726 139856 0 None -8 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 573 13 3 6 3.8 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Br)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
127044912 139885 0 None -26 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 501 14 3 6 4.3 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccccc1OCc1ccccc1 10.1021/acs.jmedchem.5b02023
CHEMBL3809093 139885 0 None -26 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 501 14 3 6 4.3 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccccc1OCc1ccccc1 10.1021/acs.jmedchem.5b02023
117839022 139988 0 None 407 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 C[C@H](Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3810346 139988 0 None 407 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 C[C@H](Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
124018870 139868 0 None -7 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 445 12 3 6 2.3 COc1ccc(F)cc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3808896 139868 0 None -7 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 445 12 3 6 2.3 COc1ccc(F)cc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
123368349 139890 0 None 95 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 505 12 3 6 2.9 COc1cc(Br)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3809175 139890 0 None 95 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 505 12 3 6 2.9 COc1cc(Br)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
123387804 139878 0 None -52 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 423 12 3 5 3.3 CCc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3808999 139878 0 None -52 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 423 12 3 5 3.3 CCc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
156767236 182365 0 None 9 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 449 11 1 5 4.7 COc1ccccc1N1CCN(CCCCn2cc(CCCC(=O)O)c3ccccc32)CC1 10.1016/j.ejmech.2020.112616
CHEMBL4792905 182365 0 None 9 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 449 11 1 5 4.7 COc1ccccc1N1CCN(CCCCn2cc(CCCC(=O)O)c3ccccc32)CC1 10.1016/j.ejmech.2020.112616
134157566 153480 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1cccc2[nH]c3c(c12)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3984249 153480 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1cccc2[nH]c3c(c12)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
134137522 142554 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 336 0 1 3 3.7 Fc1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3895460 142554 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 336 0 1 3 3.7 Fc1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
123204312 139929 0 None 74 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 11 3 5 2.7 Cc1cccc(C)c1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3809532 139929 0 None 74 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 11 3 5 2.7 Cc1cccc(C)c1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
134150827 151623 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 392 5 1 4 4.6 CCCOc1cc2c(cc1OC)CCN1Cc3[nH]c4ccc(OC)cc4c3CC21 10.1021/acs.jmedchem.6b01217
CHEMBL3968227 151623 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 392 5 1 4 4.6 CCCOc1cc2c(cc1OC)CCN1Cc3[nH]c4ccc(OC)cc4c3CC21 10.1021/acs.jmedchem.6b01217
134155537 150441 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 406 6 1 4 5.0 CCCCOc1cc2c(cc1OC)CCN1Cc3[nH]c4ccc(OC)cc4c3CC21 10.1021/acs.jmedchem.6b01217
CHEMBL3958316 150441 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 406 6 1 4 5.0 CCCCOc1cc2c(cc1OC)CCN1Cc3[nH]c4ccc(OC)cc4c3CC21 10.1021/acs.jmedchem.6b01217
123322716 139980 0 None 17 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 12 3 5 2.7 CCc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3810198 139980 0 None 17 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 12 3 5 2.7 CCc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
134149598 147933 0 None 33 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 336 0 1 3 3.7 Fc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3938121 147933 0 None 33 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 336 0 1 3 3.7 Fc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
123801568 139946 0 None 100 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 441 11 3 7 1.9 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.5b02023
CHEMBL3809781 139946 0 None 100 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 441 11 3 7 1.9 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.5b02023
134150128 151556 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 424 3 1 4 5.1 c1ccc(COc2ccc3[nH]c4c(c3c2)CC2c3cc5c(cc3CCN2C4)OCO5)cc1 10.1021/acs.jmedchem.6b01217
CHEMBL3967696 151556 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 424 3 1 4 5.1 c1ccc(COc2ccc3[nH]c4c(c3c2)CC2c3cc5c(cc3CCN2C4)OCO5)cc1 10.1021/acs.jmedchem.6b01217
9891967 107026 33 None 4 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3187195 107026 33 None 4 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
123644751 139960 0 None 125 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3810005 139960 0 None 125 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
123475619 139948 0 None 43 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 503 12 3 6 3.5 COc1cc(Br)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809794 139948 0 None 43 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 503 12 3 6 3.5 COc1cc(Br)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
76071859 149808 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@@H]1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3953156 149808 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@@H]1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
156767234 182004 0 None 10 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 467 11 1 4 5.7 O=C(O)CCCc1cn(CCCCCN2CCN(c3ccccc3Cl)CC2)c2ccccc12 10.1016/j.ejmech.2020.112616
CHEMBL4788144 182004 0 None 10 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 467 11 1 4 5.7 O=C(O)CCCc1cn(CCCCCN2CCN(c3ccccc3Cl)CC2)c2ccccc12 10.1016/j.ejmech.2020.112616
123393714 139931 0 None 3 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 11 3 5 3.1 Cc1ccc(C)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c1C 10.1021/acs.jmedchem.5b02023
CHEMBL3809543 139931 0 None 3 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 11 3 5 3.1 Cc1ccc(C)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c1C 10.1021/acs.jmedchem.5b02023
145993493 166792 0 None -47 6 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 439 6 0 5 4.5 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4294617 166792 0 None -47 6 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 439 6 0 5 4.5 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
145993117 166357 0 None -309 6 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
CHEMBL4286717 166357 0 None -309 6 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
123311113 139978 0 None 91 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 523 14 3 6 3.6 CCc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3810187 139978 0 None 91 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 523 14 3 6 3.6 CCc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c1 10.1021/acs.jmedchem.5b02023
10582125 81408 0 None -47 3 Rat 5.4 pIC50 = 5.4 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4cccc(CNCCCCCCNCCSSCCNCCCCCCNCc5cccc(C(=O)N6CCN(c7nc(N)c8cc(OC)c(OC)cc8n7)CC6)c5)c4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL216443 81408 0 None -47 3 Rat 5.4 pIC50 = 5.4 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4cccc(CNCCCCCCNCCSSCCNCCCCCCNCc5cccc(C(=O)N6CCN(c7nc(N)c8cc(OC)c(OC)cc8n7)CC6)c5)c4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
123688273 139938 0 None 36 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 513 13 3 6 3.2 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc(F)cc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3809630 139938 0 None 36 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 513 13 3 6 3.2 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc(F)cc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
127044911 139905 0 None -10 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 12 3 6 2.7 COc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809319 139905 0 None -10 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 12 3 6 2.7 COc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
123183757 139934 0 None 10 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 445 12 3 6 2.3 COc1cc(F)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3809600 139934 0 None 10 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 445 12 3 6 2.3 COc1cc(F)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
127044894 139824 0 None 3 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 427 12 3 6 2.1 COc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3808408 139824 0 None 3 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 427 12 3 6 2.1 COc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
134147190 149254 0 None 3 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 334 0 2 4 3.3 Oc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3948551 149254 0 None 3 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 334 0 2 4 3.3 Oc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
10034370 156438 0 None -10 3 Rat 7.3 pIC50 = 7.3 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CNCCCCCCNCCSSCCNCCCCCCNCc4cccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)c4)c3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL1203232 156438 0 None -10 3 Rat 7.3 pIC50 = 7.3 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CNCCCCCCNCCSSCCNCCCCCCNCc4cccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)c4)c3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL407315 156438 0 None -10 3 Rat 7.3 pIC50 = 7.3 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CNCCCCCCNCCSSCCNCCCCCCNCc4cccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)c4)c3)nc(N)c2cc1OC 10.1021/jm000995w
127043026 139904 0 None 8 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCN[C@@H](C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809314 139904 0 None 8 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCN[C@@H](C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
16638286 149056 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3C1C2)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3946997 149056 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3C1C2)OCO4 10.1021/acs.jmedchem.6b01217
10034371 165416 0 None -1479 3 Rat 5.3 pIC50 = 5.3 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CNCCCCCCNCCSSCCNCCCCCCNCc4ccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)cc4)cc3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL1203235 165416 0 None -1479 3 Rat 5.3 pIC50 = 5.3 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CNCCCCCCNCCSSCCNCCCCCCNCc4ccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)cc4)cc3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL425267 165416 0 None -1479 3 Rat 5.3 pIC50 = 5.3 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CNCCCCCCNCCSSCCNCCCCCCNCc4ccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)cc4)cc3)nc(N)c2cc1OC 10.1021/jm000995w
10630100 96140 0 None -186 3 Rat 5.3 pIC50 = 5.3 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4ccccc4CNCCCCCCNCCSSCCNCCCCCCNCc4ccccc4C(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL263289 96140 0 None -186 3 Rat 5.3 pIC50 = 5.3 Functional
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4ccccc4CNCCCCCCNCCSSCCNCCCCCCNCc4ccccc4C(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
145947950 167161 0 None 1 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 440 7 0 3 5.8 Cc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
CHEMBL4224703 167161 0 None 1 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 440 7 0 3 5.8 Cc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
CHEMBL4302771 167161 0 None 1 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 440 7 0 3 5.8 Cc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
21171 186383 27 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL490533 186383 27 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1021/acs.jmedchem.6b01217
21823379 144181 2 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 304 1 1 2 3.8 COc1ccc2c(c1)CCN1Cc3[nH]c4ccccc4c3CC21 10.1021/acs.jmedchem.6b01217
CHEMBL3908813 144181 2 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 304 1 1 2 3.8 COc1ccc2c(c1)CCN1Cc3[nH]c4ccccc4c3CC21 10.1021/acs.jmedchem.6b01217
4418 33985 80 None -10 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2018.03.070
CHEMBL142635 33985 80 None -10 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2018.03.070
145947047 167063 0 None -1 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 425 7 0 2 6.6 c1ccc(C2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4227513 167063 0 None -1 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 425 7 0 2 6.6 c1ccc(C2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4301557 167063 0 None -1 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 425 7 0 2 6.6 c1ccc(C2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
123576734 139881 0 None 15 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 455 13 3 6 2.7 CCc1ccc(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c(OC)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809032 139881 0 None 15 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 455 13 3 6 2.7 CCc1ccc(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c(OC)c1 10.1021/acs.jmedchem.5b02023
76071738 147785 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 0 1 3 3.6 c1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2[C@@H]1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3937032 147785 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 0 1 3 3.6 c1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2[C@@H]1C3)OCO4 10.1021/acs.jmedchem.6b01217
145946630 167001 0 None 12 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 456 8 0 4 5.5 COc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4224794 167001 0 None 12 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 456 8 0 4 5.5 COc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4300618 167001 0 None 12 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 456 8 0 4 5.5 COc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
123752717 139927 0 None 26 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 11 3 5 3.1 Cc1cc(C)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c(C)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809500 139927 0 None 26 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 11 3 5 3.1 Cc1cc(C)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c(C)c1 10.1021/acs.jmedchem.5b02023
134145079 149677 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3952204 149677 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
127044906 139875 0 None 7 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 C[C@@H](Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3808981 139875 0 None 7 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 C[C@@H](Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
123183788 139983 0 None 7 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 441 12 3 6 2.4 COc1cc(C)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3810220 139983 0 None 7 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 441 12 3 6 2.4 COc1cc(C)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
123378354 139844 0 None 6 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 493 11 3 5 3.0 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc(F)cc1Br 10.1021/acs.jmedchem.5b02023
CHEMBL3808595 139844 0 None 6 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 493 11 3 5 3.0 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc(F)cc1Br 10.1021/acs.jmedchem.5b02023
145963961 163840 0 None -32 6 Human 7.2 pIC50 = 7.2 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4213342 163840 0 None -32 6 Human 7.2 pIC50 = 7.2 Functional
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
134157568 153910 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 352 4 0 4 3.1 COc1cc2cc[n+]3c(c2cc1OC)Cc1ccc(OC)c(OC)c1C3 10.1021/acs.jmedchem.6b01217
CHEMBL3984336 153910 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 352 4 0 4 3.1 COc1cc2cc[n+]3c(c2cc1OC)Cc1ccc(OC)c(OC)c1C3 10.1021/acs.jmedchem.6b01217
CHEMBL3990197 153910 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 352 4 0 4 3.1 COc1cc2cc[n+]3c(c2cc1OC)Cc1ccc(OC)c(OC)c1C3 10.1021/acs.jmedchem.6b01217
127044916 139939 0 None 1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 443 12 3 6 2.9 COc1cc(F)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809676 139939 0 None 1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 443 12 3 6 2.9 COc1cc(F)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
123437117 139826 0 None 23 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 461 12 3 6 2.8 COc1cc(Cl)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3808417 139826 0 None 23 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 461 12 3 6 2.8 COc1cc(Cl)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
127045050 139850 0 None -5 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 503 14 3 6 3.7 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccccc1OCc1ccccc1 10.1021/acs.jmedchem.5b02023
CHEMBL3808632 139850 0 None -5 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 503 14 3 6 3.7 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccccc1OCc1ccccc1 10.1021/acs.jmedchem.5b02023
118167692 163646 8 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at alpha1A adrenergic receptor (unknown origin)Antagonist activity at alpha1A adrenergic receptor (unknown origin)
ChEMBL 521 7 1 7 3.0 Cn1cnc(-c2cnc(O[C@H]3CCN(C(=O)Cc4ccc(OC(F)(F)F)cc4)C[C@H]3F)c(C(N)=O)c2)c1 10.1021/acs.jmedchem.8b00633
CHEMBL4210892 163646 8 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at alpha1A adrenergic receptor (unknown origin)Antagonist activity at alpha1A adrenergic receptor (unknown origin)
ChEMBL 521 7 1 7 3.0 Cn1cnc(-c2cnc(O[C@H]3CCN(C(=O)Cc4ccc(OC(F)(F)F)cc4)C[C@H]3F)c(C(N)=O)c2)c1 10.1021/acs.jmedchem.8b00633
134134752 143665 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 1 1 2 4.4 COc1ccc2c(c1)CCN1C(C)c3[nH]c4ccccc4c3CC21 10.1021/acs.jmedchem.6b01217
CHEMBL3904395 143665 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 1 1 2 4.4 COc1ccc2c(c1)CCN1C(C)c3[nH]c4ccccc4c3CC21 10.1021/acs.jmedchem.6b01217
10813278 106444 0 None - 0 Rabbit 10.7 pKd = 10.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 446 8 1 6 3.5 Cc1ccc(N2CCN(CCCNc3ncccc3C(=O)N(C)C)CC2)c(-n2cccc2)c1 10.1021/jm970166j
CHEMBL314880 106444 0 None - 0 Rabbit 10.7 pKd = 10.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 446 8 1 6 3.5 Cc1ccc(N2CCN(CCCNc3ncccc3C(=O)N(C)C)CC2)c(-n2cccc2)c1 10.1021/jm970166j
10697270 105684 0 None - 0 Rabbit 10.0 pKd = 10 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 519 9 2 8 3.2 CNC(=O)c1cnc2c(c(C)nn2C)c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL313775 105684 0 None - 0 Rabbit 10.0 pKd = 10 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 519 9 2 8 3.2 CNC(=O)c1cnc2c(c(C)nn2C)c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
10552132 112278 0 None - 0 Rabbit 10.0 pKd = 10 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 465 9 1 6 3.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL330579 112278 0 None - 0 Rabbit 10.0 pKd = 10 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 465 9 1 6 3.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
13305910 11716 1 None - 0 Rat 10.0 pKd = 10.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182155 11716 1 None - 0 Rat 10.0 pKd = 10.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL215421 11716 1 None - 0 Rat 10.0 pKd = 10.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL3741808 11716 1 None - 0 Rat 10.0 pKd = 10.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
13305910 11716 1 None - 0 Rat 10.0 pKd = 10.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL1182155 11716 1 None - 0 Rat 10.0 pKd = 10.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL215421 11716 1 None - 0 Rat 10.0 pKd = 10.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL3741808 11716 1 None - 0 Rat 10.0 pKd = 10.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
10506159 110899 0 None - 0 Rabbit 9.9 pKd = 9.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 520 8 1 9 3.4 Cc1nn(C)c2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccc(F)cc4-c4ncco4)CC3)c12 10.1021/jm970166j
CHEMBL327231 110899 0 None - 0 Rabbit 9.9 pKd = 9.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 520 8 1 9 3.4 Cc1nn(C)c2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccc(F)cc4-c4ncco4)CC3)c12 10.1021/jm970166j
10693231 201065 0 None - 0 Human 9.8 pKd = 9.8 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 416 4 1 6 2.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C#N)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL62033 201065 0 None - 0 Human 9.8 pKd = 9.8 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 416 4 1 6 2.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C#N)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
129211 3680 75 None - 3 Rabbit 9.8 pKd = 9.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
2562 3680 75 None - 3 Rabbit 9.8 pKd = 9.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
488 3680 75 None - 3 Rabbit 9.8 pKd = 9.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
CHEMBL836 3680 75 None - 3 Rabbit 9.8 pKd = 9.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
DB00706 3680 75 None - 3 Rabbit 9.8 pKd = 9.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
10526964 205227 0 None - 0 Rabbit 9.8 pKd = 9.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 437 10 1 6 3.2 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC2CC2)CC1 10.1021/jm970166j
CHEMBL91278 205227 0 None - 0 Rabbit 9.8 pKd = 9.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 437 10 1 6 3.2 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC2CC2)CC1 10.1021/jm970166j
10764021 205253 0 None - 0 Rabbit 9.7 pKd = 9.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 409 9 1 5 3.4 CCCc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL91400 205253 0 None - 0 Rabbit 9.7 pKd = 9.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 409 9 1 5 3.4 CCCc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
24897950 56043 0 None - 0 Rat 9.6 pKd = 9.6 Functional
Antagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 mins
ChEMBL 462 11 2 6 2.9 COc1ccc(C[C@@H](C)NCCOc2ccccc2OCC(F)(F)F)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
CHEMBL1630940 56043 0 None - 0 Rat 9.6 pKd = 9.6 Functional
Antagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 mins
ChEMBL 462 11 2 6 2.9 COc1ccc(C[C@@H](C)NCCOc2ccccc2OCC(F)(F)F)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
71462043 84131 0 None - 0 Rat 9.6 pKd = 9.6 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153555 84131 0 None - 0 Rat 9.6 pKd = 9.6 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220895 84131 0 None - 0 Rat 9.6 pKd = 9.6 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
129211 3680 75 None 1 3 Human 9.5 pKd = 9.5 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
2562 3680 75 None 1 3 Human 9.5 pKd = 9.5 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
488 3680 75 None 1 3 Human 9.5 pKd = 9.5 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
CHEMBL836 3680 75 None 1 3 Human 9.5 pKd = 9.5 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
DB00706 3680 75 None 1 3 Human 9.5 pKd = 9.5 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
129211 3680 75 None 1 3 Human 9.5 pKd = 9.5 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
2562 3680 75 None 1 3 Human 9.5 pKd = 9.5 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
488 3680 75 None 1 3 Human 9.5 pKd = 9.5 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
CHEMBL836 3680 75 None 1 3 Human 9.5 pKd = 9.5 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
DB00706 3680 75 None 1 3 Human 9.5 pKd = 9.5 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
499 4002 15 None - 1 Rat 9.5 pKd = 9.5 Functional
Antagonistic activity at ADRA1A in isolated rat prostatic vas deferensAntagonistic activity at ADRA1A in isolated rat prostatic vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.bmcl.2005.09.027
5685 4002 15 None - 1 Rat 9.5 pKd = 9.5 Functional
Antagonistic activity at ADRA1A in isolated rat prostatic vas deferensAntagonistic activity at ADRA1A in isolated rat prostatic vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.bmcl.2005.09.027
CHEMBL25554 4002 15 None - 1 Rat 9.5 pKd = 9.5 Functional
Antagonistic activity at ADRA1A in isolated rat prostatic vas deferensAntagonistic activity at ADRA1A in isolated rat prostatic vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.bmcl.2005.09.027
499 4002 15 None - 1 Rat 9.5 pKd = 9.5 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
5685 4002 15 None - 1 Rat 9.5 pKd = 9.5 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
CHEMBL25554 4002 15 None - 1 Rat 9.5 pKd = 9.5 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
10526831 110888 0 None - 0 Rabbit 9.5 pKd = 9.5 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 434 8 1 7 3.1 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2-c2ncco2)CC1 10.1021/jm970166j
CHEMBL327168 110888 0 None - 0 Rabbit 9.5 pKd = 9.5 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 434 8 1 7 3.1 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2-c2ncco2)CC1 10.1021/jm970166j
13305910 11716 1 None - 0 Rat 9.5 pKd = 9.5 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182155 11716 1 None - 0 Rat 9.5 pKd = 9.5 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL215421 11716 1 None - 0 Rat 9.5 pKd = 9.5 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL3741808 11716 1 None - 0 Rat 9.5 pKd = 9.5 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
13305910 11716 1 None - 0 Rat 9.5 pKd = 9.5 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL1182155 11716 1 None - 0 Rat 9.5 pKd = 9.5 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL215421 11716 1 None - 0 Rat 9.5 pKd = 9.5 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL3741808 11716 1 None - 0 Rat 9.5 pKd = 9.5 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
129211 3680 75 None - 3 Rat 9.5 pKd = 9.5 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
2562 3680 75 None - 3 Rat 9.5 pKd = 9.5 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
488 3680 75 None - 3 Rat 9.5 pKd = 9.5 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
CHEMBL836 3680 75 None - 3 Rat 9.5 pKd = 9.5 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
DB00706 3680 75 None - 3 Rat 9.5 pKd = 9.5 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
129211 3680 75 None - 3 Rat 9.5 pKd = 9.5 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
2562 3680 75 None - 3 Rat 9.5 pKd = 9.5 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
488 3680 75 None - 3 Rat 9.5 pKd = 9.5 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
CHEMBL836 3680 75 None - 3 Rat 9.5 pKd = 9.5 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
DB00706 3680 75 None - 3 Rat 9.5 pKd = 9.5 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
44289437 169285 0 None - 0 Rat 9.5 pKd = 9.5 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 431 9 1 5 4.7 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2C1=O 10.1021/jm011066n
CHEMBL44403 169285 0 None - 0 Rat 9.5 pKd = 9.5 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 431 9 1 5 4.7 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2C1=O 10.1021/jm011066n
10789770 100405 0 None - 0 Human 9.5 pKd = 9.5 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 6 1 7 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)c(OC)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL293695 100405 0 None - 0 Human 9.5 pKd = 9.5 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 6 1 7 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)c(OC)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
10645210 204743 0 None - 0 Rabbit 9.4 pKd = 9.4 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 409 8 1 5 3.5 CC(C)c1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL88211 204743 0 None - 0 Rabbit 9.4 pKd = 9.4 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 409 8 1 5 3.5 CC(C)c1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
499 4002 15 None - 1 Rat 9.4 pKd = 9.4 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
5685 4002 15 None - 1 Rat 9.4 pKd = 9.4 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
CHEMBL25554 4002 15 None - 1 Rat 9.4 pKd = 9.4 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
499 4002 15 None - 1 Rat 9.4 pKd = 9.4 Functional
Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm021078o
5685 4002 15 None - 1 Rat 9.4 pKd = 9.4 Functional
Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm021078o
CHEMBL25554 4002 15 None - 1 Rat 9.4 pKd = 9.4 Functional
Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm021078o
44289437 169285 0 None - 0 Rat 9.4 pKd = 9.4 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 431 9 1 5 4.7 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2C1=O 10.1021/jm011066n
CHEMBL44403 169285 0 None - 0 Rat 9.4 pKd = 9.4 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 431 9 1 5 4.7 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2C1=O 10.1021/jm011066n
10787790 105497 0 None - 0 Rabbit 9.3 pKd = 9.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 411 9 1 6 2.8 CCOc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL313157 105497 0 None - 0 Rabbit 9.3 pKd = 9.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 411 9 1 6 2.8 CCOc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10744240 106538 0 None - 0 Rabbit 9.3 pKd = 9.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 508 9 2 7 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c(C(N)=O)cccc23)CC1 10.1021/jm970166j
CHEMBL315496 106538 0 None - 0 Rabbit 9.3 pKd = 9.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 508 9 2 7 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c(C(N)=O)cccc23)CC1 10.1021/jm970166j
10763212 167622 0 None - 0 Rabbit 9.3 pKd = 9.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 394 9 1 6 3.3 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)C2CC2)CC1 10.1021/jm970166j
CHEMBL433348 167622 0 None - 0 Rabbit 9.3 pKd = 9.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 394 9 1 6 3.3 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)C2CC2)CC1 10.1021/jm970166j
9893282 204733 0 None - 0 Rabbit 9.3 pKd = 9.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 533 9 1 8 3.5 Cc1nn(C)c2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccccc4OCC(F)(F)F)CC3)c12 10.1021/jm970166j
CHEMBL88160 204733 0 None - 0 Rabbit 9.3 pKd = 9.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 533 9 1 8 3.5 Cc1nn(C)c2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccccc4OCC(F)(F)F)CC3)c12 10.1021/jm970166j
44323795 204872 0 None - 0 Rabbit 9.3 pKd = 9.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 410 8 1 5 3.3 COc1ccccc1N1CCN(CCCNc2cc(C)ccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL89030 204872 0 None - 0 Rabbit 9.3 pKd = 9.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 410 8 1 5 3.3 COc1ccccc1N1CCN(CCCNc2cc(C)ccc2C(=O)N(C)C)CC1 10.1021/jm970166j
499 4002 15 None - 1 Rat 9.3 pKd = 9.3 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
5685 4002 15 None - 1 Rat 9.3 pKd = 9.3 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
CHEMBL25554 4002 15 None - 1 Rat 9.3 pKd = 9.3 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
9824384 118269 1 None - 0 Rat 9.2 pKd = 9.2 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL342062 118269 1 None - 0 Rat 9.2 pKd = 9.2 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
10478121 170225 0 None - 0 Human 9.2 pKd = 9.2 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 435 6 0 7 3.1 COc1cc2ncn(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
CHEMBL445325 170225 0 None - 0 Human 9.2 pKd = 9.2 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 435 6 0 7 3.1 COc1cc2ncn(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
10743446 106575 0 None - 0 Rabbit 9.2 pKd = 9.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 483 8 1 8 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c2nc(C)n3C)CC1 10.1021/jm970166j
CHEMBL315785 106575 0 None - 0 Rabbit 9.2 pKd = 9.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 483 8 1 8 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c2nc(C)n3C)CC1 10.1021/jm970166j
10549680 111878 0 None - 0 Rabbit 9.2 pKd = 9.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 1 6 3.1 CSc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL329601 111878 0 None - 0 Rabbit 9.2 pKd = 9.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 1 6 3.1 CSc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10647512 205287 0 None - 0 Rabbit 9.2 pKd = 9.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 456 8 2 6 1.6 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)c[nH]c3ccn[n+]2-3)CC1 10.1021/jm970166j
CHEMBL91547 205287 0 None - 0 Rabbit 9.2 pKd = 9.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 456 8 2 6 1.6 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)c[nH]c3ccn[n+]2-3)CC1 10.1021/jm970166j
10621397 205353 0 None - 0 Rabbit 9.2 pKd = 9.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 407 8 1 5 3.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2C2CC2)CC1 10.1021/jm970166j
CHEMBL91951 205353 0 None - 0 Rabbit 9.2 pKd = 9.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 407 8 1 5 3.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2C2CC2)CC1 10.1021/jm970166j
499 4002 15 None - 1 Rat 9.2 pKd = 9.2 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
5685 4002 15 None - 1 Rat 9.2 pKd = 9.2 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
CHEMBL25554 4002 15 None - 1 Rat 9.2 pKd = 9.2 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
10574245 111021 0 None - 0 Rabbit 9.1 pKd = 9.1 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 422 8 1 7 2.3 COc1ccccc1N1CCN(CCCNc2ncc(C#N)cc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL327872 111021 0 None - 0 Rabbit 9.1 pKd = 9.1 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 422 8 1 7 2.3 COc1ccccc1N1CCN(CCCNc2ncc(C#N)cc2C(=O)N(C)C)CC1 10.1021/jm970166j
10577066 111906 0 None - 0 Rabbit 9.1 pKd = 9.1 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 490 8 2 6 2.3 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)c[nH]c3c(Cl)cn[n+]2-3)CC1 10.1021/jm970166j
CHEMBL329773 111906 0 None - 0 Rabbit 9.1 pKd = 9.1 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 490 8 2 6 2.3 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)c[nH]c3c(Cl)cn[n+]2-3)CC1 10.1021/jm970166j
10530686 205166 0 None - 0 Rabbit 9.1 pKd = 9.1 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 549 9 1 6 5.2 CN(C)C(=O)c1cnc2c(Cl)cccc2c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL90878 205166 0 None - 0 Rabbit 9.1 pKd = 9.1 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 549 9 1 6 5.2 CN(C)C(=O)c1cnc2c(Cl)cccc2c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
11795906 205327 0 None - 0 Rabbit 9.1 pKd = 9.1 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 411 8 1 6 2.7 COc1cc(C)ccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL91785 205327 0 None - 0 Rabbit 9.1 pKd = 9.1 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 411 8 1 6 2.7 COc1cc(C)ccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
14423371 96992 1 None - 0 Rat 9.0 pKd = 9.0 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 441 11 1 8 3.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL27013 96992 1 None - 0 Rat 9.0 pKd = 9.0 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 441 11 1 8 3.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1021/jm9810654
71462043 84131 0 None - 0 Rat 9.0 pKd = 9.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153555 84131 0 None - 0 Rat 9.0 pKd = 9.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220895 84131 0 None - 0 Rat 9.0 pKd = 9.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
14423371 96992 1 None - 0 Rat 9.0 pKd = 9.0 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 441 11 1 8 3.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1016/s0960-894x(98)00217-0
CHEMBL27013 96992 1 None - 0 Rat 9.0 pKd = 9.0 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 441 11 1 8 3.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1016/s0960-894x(98)00217-0
10456471 100054 0 None - 0 Human 9.0 pKd = 9.0 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 6 1 7 2.4 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
CHEMBL291303 100054 0 None - 0 Human 9.0 pKd = 9.0 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 6 1 7 2.4 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
10572854 112061 0 None - 0 Rabbit 9.0 pKd = 9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 396 8 1 5 3.0 COc1ccccc1N1CCN(CCCNc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL330060 112061 0 None - 0 Rabbit 9.0 pKd = 9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 396 8 1 5 3.0 COc1ccccc1N1CCN(CCCNc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10786203 205528 0 None - 0 Rabbit 9.0 pKd = 9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 8 2 6 2.1 CNC(=O)c1cccnc1NCCCN1CCN(c2ccccc2OC)CC1 10.1021/jm970166j
CHEMBL93054 205528 0 None - 0 Rabbit 9.0 pKd = 9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 8 2 6 2.1 CNC(=O)c1cccnc1NCCCN1CCN(c2ccccc2OC)CC1 10.1021/jm970166j
11430491 62657 0 None - 0 Rat 9.0 pKd = 9 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 435 5 1 9 2.4 COc1cc2nc(N3CCN(C(=O)CC4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
CHEMBL178673 62657 0 None - 0 Rat 9.0 pKd = 9 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 435 5 1 9 2.4 COc1cc2nc(N3CCN(C(=O)CC4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
10527469 155712 1 None - 0 Human 9.0 pKd = 9 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
CHEMBL40650 155712 1 None - 0 Human 9.0 pKd = 9 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
4209 3102 71 None -1 10 Rat 9.0 pKd = 9.0 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
4893 3102 71 None -1 10 Rat 9.0 pKd = 9.0 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
503 3102 71 None -1 10 Rat 9.0 pKd = 9.0 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
5385 3102 71 None -1 10 Rat 9.0 pKd = 9.0 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
CHEMBL2 3102 71 None -1 10 Rat 9.0 pKd = 9.0 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
DB00457 3102 71 None -1 10 Rat 9.0 pKd = 9.0 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
10478121 170225 0 None - 0 Rat 9.0 pKd = 9.0 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 435 6 0 7 3.1 COc1cc2ncn(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
CHEMBL445325 170225 0 None - 0 Rat 9.0 pKd = 9.0 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 435 6 0 7 3.1 COc1cc2ncn(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
16121006 11721 0 None - 0 Rat 9.0 pKd = 9.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182182 11721 0 None - 0 Rat 9.0 pKd = 9.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL217469 11721 0 None - 0 Rat 9.0 pKd = 9.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
11742834 165206 0 None - 0 Rat 9.0 pKd = 9.0 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 419 9 1 5 4.7 COc1cccc(OC)c1OCCNC[C@@H]1C[C@H](c2ccccc2)c2ccccc2O1 10.1021/jm011066n
CHEMBL42472 165206 0 None - 0 Rat 9.0 pKd = 9.0 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 419 9 1 5 4.7 COc1cccc(OC)c1OCCNC[C@@H]1C[C@H](c2ccccc2)c2ccccc2O1 10.1021/jm011066n
10527469 155712 1 None - 0 Rat 8.9 pKd = 8.9 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
CHEMBL40650 155712 1 None - 0 Rat 8.9 pKd = 8.9 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
10834793 84142 0 None - 0 Rat 8.9 pKd = 8.9 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153557 84142 0 None - 0 Rat 8.9 pKd = 8.9 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220925 84142 0 None - 0 Rat 8.9 pKd = 8.9 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
132266 1247 9 None - 0 Rat 8.9 pKd = 8.9 Functional
Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deferenceAntagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm8016046
486 1247 9 None - 0 Rat 8.9 pKd = 8.9 Functional
Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deferenceAntagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm8016046
CHEMBL423294 1247 9 None - 0 Rat 8.9 pKd = 8.9 Functional
Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deferenceAntagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm8016046
10505222 204929 0 None - 0 Rabbit 8.9 pKd = 8.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 490 8 1 7 3.6 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c(C#N)cccc23)CC1 10.1021/jm970166j
CHEMBL89397 204929 0 None - 0 Rabbit 8.9 pKd = 8.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 490 8 1 7 3.6 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c(C#N)cccc23)CC1 10.1021/jm970166j
10575254 205146 0 None - 0 Rabbit 8.9 pKd = 8.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 443 8 1 5 4.1 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1021/jm970166j
CHEMBL90746 205146 0 None - 0 Rabbit 8.9 pKd = 8.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 443 8 1 5 4.1 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1021/jm970166j
10814587 205155 0 None - 0 Rabbit 8.9 pKd = 8.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 480 8 1 7 3.4 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3nc(C)ccc23)CC1 10.1021/jm970166j
CHEMBL90810 205155 0 None - 0 Rabbit 8.9 pKd = 8.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 480 8 1 7 3.4 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3nc(C)ccc23)CC1 10.1021/jm970166j
10646065 205165 0 None - 0 Rabbit 8.9 pKd = 8.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 425 8 2 6 3.2 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)NC(C)(C)C)CC1 10.1021/jm970166j
CHEMBL90874 205165 0 None - 0 Rabbit 8.9 pKd = 8.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 425 8 2 6 3.2 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)NC(C)(C)C)CC1 10.1021/jm970166j
10624682 205299 0 None - 0 Rabbit 8.9 pKd = 8.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 483 8 1 8 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c2c(C)nn3C)CC1 10.1021/jm970166j
CHEMBL91605 205299 0 None - 0 Rabbit 8.9 pKd = 8.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 483 8 1 8 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c2c(C)nn3C)CC1 10.1021/jm970166j
10789770 100405 0 None - 0 Rat 8.9 pKd = 8.9 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 451 6 1 7 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)c(OC)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL293695 100405 0 None - 0 Rat 8.9 pKd = 8.9 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 451 6 1 7 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)c(OC)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
11742834 165206 0 None - 0 Rat 8.9 pKd = 8.9 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 419 9 1 5 4.7 COc1cccc(OC)c1OCCNC[C@@H]1C[C@H](c2ccccc2)c2ccccc2O1 10.1021/jm011066n
CHEMBL42472 165206 0 None - 0 Rat 8.9 pKd = 8.9 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 419 9 1 5 4.7 COc1cccc(OC)c1OCCNC[C@@H]1C[C@H](c2ccccc2)c2ccccc2O1 10.1021/jm011066n
10693231 201065 0 None - 0 Rat 8.8 pKd = 8.8 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 416 4 1 6 2.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C#N)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL62033 201065 0 None - 0 Rat 8.8 pKd = 8.8 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 416 4 1 6 2.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C#N)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
9865577 111804 1 None - 0 Rabbit 8.8 pKd = 8.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL329160 111804 1 None - 0 Rabbit 8.8 pKd = 8.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10621790 163253 0 None - 0 Rabbit 8.8 pKd = 8.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 415 8 1 6 2.6 COc1cc(F)ccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL420620 163253 0 None - 0 Rabbit 8.8 pKd = 8.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 415 8 1 6 2.6 COc1cc(F)ccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10839699 205014 0 None - 0 Rabbit 8.8 pKd = 8.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 520 9 1 8 3.8 Cc1noc2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccccc4OCC(F)(F)F)CC3)c12 10.1021/jm970166j
CHEMBL90022 205014 0 None - 0 Rabbit 8.8 pKd = 8.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 520 9 1 8 3.8 Cc1noc2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccccc4OCC(F)(F)F)CC3)c12 10.1021/jm970166j
10552164 205163 0 None - 0 Rabbit 8.8 pKd = 8.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 466 9 1 6 3.4 CN(C)C(=O)c1cccnc1N1CCC(NCCOc2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL90869 205163 0 None - 0 Rabbit 8.8 pKd = 8.8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 466 9 1 6 3.4 CN(C)C(=O)c1cccnc1N1CCC(NCCOc2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
10549596 84168 0 None - 0 Rat 8.8 pKd = 8.8 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153553 84168 0 None - 0 Rat 8.8 pKd = 8.8 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2221147 84168 0 None - 0 Rat 8.8 pKd = 8.8 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
10501886 110900 0 None - 0 Rabbit 8.7 pKd = 8.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 2 7 2.1 COc1ccccc1N1CCN(CCCNc2ncc(O)cc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL327232 110900 0 None - 0 Rabbit 8.7 pKd = 8.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 2 7 2.1 COc1ccccc1N1CCN(CCCNc2ncc(O)cc2C(=O)N(C)C)CC1 10.1021/jm970166j
10693071 204738 0 None - 0 Rabbit 8.7 pKd = 8.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 0 5 3.7 COc1ccccc1N1CCN(CCCSc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL88181 204738 0 None - 0 Rabbit 8.7 pKd = 8.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 0 5 3.7 COc1ccccc1N1CCN(CCCSc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10833725 204775 0 None - 0 Rabbit 8.7 pKd = 8.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 381 7 1 5 2.7 Cc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL88435 204775 0 None - 0 Rabbit 8.7 pKd = 8.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 381 7 1 5 2.7 Cc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10500734 204843 0 None - 0 Rabbit 8.7 pKd = 8.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 392 7 1 6 2.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2C#N)CC1 10.1021/jm970166j
CHEMBL88856 204843 0 None - 0 Rabbit 8.7 pKd = 8.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 392 7 1 6 2.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2C#N)CC1 10.1021/jm970166j
44324012 205508 0 None - 0 Rabbit 8.0 pKd = 8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 2 6 2.4 COc1ccccc1N1CCN(CCCNc2nc(C)cc(C)c2C(N)=O)CC1 10.1021/jm970166j
CHEMBL92901 205508 0 None - 0 Rabbit 8.0 pKd = 8 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 2 6 2.4 COc1ccccc1N1CCN(CCCNc2nc(C)cc(C)c2C(N)=O)CC1 10.1021/jm970166j
11994673 12195 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL1185036 12195 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL385371 12195 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
10745791 36264 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 579 19 3 9 4.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCN)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL144776 36264 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 579 19 3 9 4.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCN)nc(N)c2cc1OC 10.1021/jm9810654
10394346 16767 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 638 11 2 10 3.0 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C(N)=O)CC3)cccc2c1=O 10.1021/jm030825u
CHEMBL125365 16767 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 638 11 2 10 3.0 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C(N)=O)CC3)cccc2c1=O 10.1021/jm030825u
52945071 17446 0 None - 0 Rat 6.0 pKd = 6.0 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 470 7 2 5 2.7 O=C1NC(=O)C(c2ccccc2)(c2ccccc2)N1CC(O)CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL1258344 17446 0 None - 0 Rat 6.0 pKd = 6.0 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 470 7 2 5 2.7 O=C1NC(=O)C(c2ccccc2)(c2ccccc2)N1CC(O)CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
11133868 154791 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNC[C@H]1C[C@H](c2ccccc2)c2ccccc2S1 10.1021/jm011066n
CHEMBL40325 154791 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNC[C@H]1C[C@H](c2ccccc2)c2ccccc2S1 10.1021/jm011066n
2419 687 22 None - 3 Rat 6.9 pKd = 6.9 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm9810654
9 687 22 None - 3 Rat 6.9 pKd = 6.9 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm9810654
CHEMBL13647 687 22 None - 3 Rat 6.9 pKd = 6.9 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm9810654
2419 687 22 None - 3 Rat 6.9 pKd = 6.9 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(98)00217-0
9 687 22 None - 3 Rat 6.9 pKd = 6.9 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(98)00217-0
CHEMBL13647 687 22 None - 3 Rat 6.9 pKd = 6.9 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(98)00217-0
3584 3706 60 None -25 8 Rat 7.9 pKd = 7.9 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmcl.2018.01.068
5401 3706 60 None -25 8 Rat 7.9 pKd = 7.9 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmcl.2018.01.068
7302 3706 60 None -25 8 Rat 7.9 pKd = 7.9 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmcl.2018.01.068
CHEMBL611 3706 60 None -25 8 Rat 7.9 pKd = 7.9 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmcl.2018.01.068
DB01162 3706 60 None -25 8 Rat 7.9 pKd = 7.9 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmcl.2018.01.068
10574889 106051 0 None - 0 Rabbit 7.9 pKd = 7.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 435 7 1 5 3.4 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2C(F)(F)F)CC1 10.1021/jm970166j
CHEMBL314114 106051 0 None - 0 Rabbit 7.9 pKd = 7.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 435 7 1 5 3.4 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2C(F)(F)F)CC1 10.1021/jm970166j
10787895 110919 0 None - 0 Rabbit 7.9 pKd = 7.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 2 7 2.1 COc1cc(O)ccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL327351 110919 0 None - 0 Rabbit 7.9 pKd = 7.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 2 7 2.1 COc1cc(O)ccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10524875 205630 0 None - 0 Rabbit 7.9 pKd = 7.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ccncc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL93736 205630 0 None - 0 Rabbit 7.9 pKd = 7.9 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ccncc2C(=O)N(C)C)CC1 10.1021/jm970166j
52942664 17447 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 500 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL1258345 17447 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 500 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
52942591 17415 0 None - 0 Rat 5.9 pKd = 5.9 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 542 9 1 7 2.6 COC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL1258228 17415 0 None - 0 Rat 5.9 pKd = 5.9 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 542 9 1 7 2.6 COC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
44428846 91743 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractionAntagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction
ChEMBL 467 5 1 9 3.1 COc1ccc(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)[C@@H]3CCCC[C@@H]32)o1 10.1016/j.bmc.2007.01.028
CHEMBL242508 91743 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractionAntagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction
ChEMBL 467 5 1 9 3.1 COc1ccc(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)[C@@H]3CCCC[C@@H]32)o1 10.1016/j.bmc.2007.01.028
145971621 164042 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 414 9 1 7 2.0 COC(=O)Cc1ccc(OCC(O)CN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmcl.2018.01.068
CHEMBL4215889 164042 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 414 9 1 7 2.0 COC(=O)Cc1ccc(OCC(O)CN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmcl.2018.01.068
10506915 39984 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 552 13 1 9 4.5 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CN4CCSC4)c3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL148061 39984 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 552 13 1 9 4.5 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CN4CCSC4)c3)nc(N)c2cc1OC 10.1021/jm9810654
69782867 161023 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 549 8 1 9 4.4 COc1cc2nc(N3CCN(C(=O)COc4c(OC)cccc4C(C)C)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4129291 161023 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 549 8 1 9 4.4 COc1cc2nc(N3CCN(C(=O)COc4c(OC)cccc4C(C)C)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
25022505 187697 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 586 10 1 8 2.9 COC(=O)C(C)N1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL500266 187697 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 586 10 1 8 2.9 COC(=O)C(C)N1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
44586483 171890 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 600 11 1 8 3.3 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)N(C(C)C(=O)OC)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL448198 171890 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 600 11 1 8 3.3 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)N(C(C)C(=O)OC)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
44586429 183705 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 514 8 1 6 3.0 COc1ccccc1N1CCN(CC(O)CN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL484102 183705 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 514 8 1 6 3.0 COc1ccccc1N1CCN(CC(O)CN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
6603808 126987 2 None - 2 Rat 7.8 pKd = 7.8 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL214986 126987 2 None - 2 Rat 7.8 pKd = 7.8 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL36622 126987 2 None - 2 Rat 7.8 pKd = 7.8 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL3740374 126987 2 None - 2 Rat 7.8 pKd = 7.8 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
9891213 160943 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 477 5 1 8 4.0 COc1cc2nc(N3CCN(C(=O)OCc4ccccc4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4128084 160943 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 477 5 1 8 4.0 COc1cc2nc(N3CCN(C(=O)OCc4ccccc4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
50905589 56045 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 mins
ChEMBL 406 7 2 6 2.1 COc1ccc(C[C@@H](C)NC[C@@H]2Oc3ccccc3O[C@@H]2C)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
CHEMBL1630942 56045 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 mins
ChEMBL 406 7 2 6 2.1 COc1ccc(C[C@@H](C)NC[C@@H]2Oc3ccccc3O[C@@H]2C)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
10530133 36770 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 525 12 1 10 4.2 COc1cc2nc(N(C)CCSSCCN(C)C(=O)c3ccc(CCl)o3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL145181 36770 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 525 12 1 10 4.2 COc1cc2nc(N(C)CCSSCCN(C)C(=O)c3ccc(CCl)o3)nc(N)c2cc1OC 10.1021/jm9810654
132266 1247 9 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractionAntagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2007.01.028
486 1247 9 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractionAntagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2007.01.028
CHEMBL423294 1247 9 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractionAntagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2007.01.028
132266 1247 9 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2018.05.023
486 1247 9 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2018.05.023
CHEMBL423294 1247 9 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2018.05.023
71454865 84166 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153551 84166 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2221145 84166 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
44289261 164349 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 417 9 1 4 5.1 COc1cccc(OC)c1OCCNCC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm011066n
CHEMBL42231 164349 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 417 9 1 4 5.1 COc1cccc(OC)c1OCCNCC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm011066n
44277158 101162 0 None - 0 Rat 5.8 pKd = 5.8 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 449 11 3 10 3.0 COc1cc2nc(NCCSSCCNC(=O)c3ccco3)nc(N)c2cc1OC 10.1016/s0960-894x(98)00217-0
CHEMBL29907 101162 0 None - 0 Rat 5.8 pKd = 5.8 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 449 11 3 10 3.0 COc1cc2nc(NCCSSCCNC(=O)c3ccco3)nc(N)c2cc1OC 10.1016/s0960-894x(98)00217-0
11430126 60224 0 None - 0 Rat 7.7 pKd = 7.7 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 421 4 1 9 2.0 COc1cc2nc(N3CCN(C(=O)C4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
CHEMBL175934 60224 0 None - 0 Rat 7.7 pKd = 7.7 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 421 4 1 9 2.0 COc1cc2nc(N3CCN(C(=O)C4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
6603808 126987 2 None - 2 Rat 7.7 pKd = 7.7 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL214986 126987 2 None - 2 Rat 7.7 pKd = 7.7 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL36622 126987 2 None - 2 Rat 7.7 pKd = 7.7 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL3740374 126987 2 None - 2 Rat 7.7 pKd = 7.7 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
3584 3706 60 None - 8 Rabbit 7.7 pKd = 7.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970166j
5401 3706 60 None - 8 Rabbit 7.7 pKd = 7.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970166j
7302 3706 60 None - 8 Rabbit 7.7 pKd = 7.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970166j
CHEMBL611 3706 60 None - 8 Rabbit 7.7 pKd = 7.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970166j
DB01162 3706 60 None - 8 Rabbit 7.7 pKd = 7.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970166j
44323554 204723 0 None - 0 Rabbit 7.7 pKd = 7.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 446 8 1 7 2.9 CN(C)C(=O)c1cccnc1N1CCC(NCCOc2ccccc2-c2cncnc2)CC1 10.1021/jm970166j
CHEMBL88109 204723 0 None - 0 Rabbit 7.7 pKd = 7.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 446 8 1 7 2.9 CN(C)C(=O)c1cccnc1N1CCC(NCCOc2ccccc2-c2cncnc2)CC1 10.1021/jm970166j
10651334 29523 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 607 20 2 9 5.2 CNCCCCCCN(C)Cc1ccc(C(=O)N(C)CCCCCCN(C)c2nc(N)c3cc(OC)c(OC)cc3n2)cc1 10.1021/jm9810654
CHEMBL138681 29523 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 607 20 2 9 5.2 CNCCCCCCN(C)Cc1ccc(C(=O)N(C)CCCCCCN(C)c2nc(N)c3cc(OC)c(OC)cc3n2)cc1 10.1021/jm9810654
10673882 38474 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 534 13 1 11 3.5 COc1cc2nc(N(C)CCSSCCN(C)C(=O)c3ccc(CN(C)C)o3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL146601 38474 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 534 13 1 11 3.5 COc1cc2nc(N(C)CCSSCCN(C)C(=O)c3ccc(CN(C)C)o3)nc(N)c2cc1OC 10.1021/jm9810654
45268939 194975 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 505 4 1 9 3.0 COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL564481 194975 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 505 4 1 9 3.0 COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
10786159 204904 0 None - 0 Rabbit 6.7 pKd = 6.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 382 7 1 6 2.1 Cc1cnccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL89222 204904 0 None - 0 Rabbit 6.7 pKd = 6.7 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 382 7 1 6 2.1 Cc1cnccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
3157 1437 69 None -2 7 Rat 8.7 pKd = 8.7 Functional
Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deferenceAntagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm8016046
7170 1437 69 None -2 7 Rat 8.7 pKd = 8.7 Functional
Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deferenceAntagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm8016046
954 1437 69 None -2 7 Rat 8.7 pKd = 8.7 Functional
Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deferenceAntagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm8016046
CHEMBL707 1437 69 None -2 7 Rat 8.7 pKd = 8.7 Functional
Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deferenceAntagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm8016046
DB00590 1437 69 None -2 7 Rat 8.7 pKd = 8.7 Functional
Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deferenceAntagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm8016046
3157 1437 69 None -2 7 Rat 8.7 pKd = 8.7 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm000541z
7170 1437 69 None -2 7 Rat 8.7 pKd = 8.7 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm000541z
954 1437 69 None -2 7 Rat 8.7 pKd = 8.7 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm000541z
CHEMBL707 1437 69 None -2 7 Rat 8.7 pKd = 8.7 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm000541z
DB00590 1437 69 None -2 7 Rat 8.7 pKd = 8.7 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm000541z
11039289 116327 0 None - 0 Rat 8.6 pKd = 8.6 Functional
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 600 13 1 9 4.7 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCCCO[N+](=O)[O-])CC3)cccc2c1=O 10.1021/jm030825u
CHEMBL338029 116327 0 None - 0 Rat 8.6 pKd = 8.6 Functional
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 600 13 1 9 4.7 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCCCO[N+](=O)[O-])CC3)cccc2c1=O 10.1021/jm030825u
4209 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
4893 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
503 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
5385 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
CHEMBL2 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
DB00457 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
10555166 204981 0 None - 0 Rabbit 8.6 pKd = 8.6 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 575 9 1 8 4.5 CN(C)C(=O)c1cnc2c(c(C(C)(C)C)nn2C)c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL89822 204981 0 None - 0 Rabbit 8.6 pKd = 8.6 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 575 9 1 8 4.5 CN(C)C(=O)c1cnc2c(c(C(C)(C)C)nn2C)c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
4209 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(98)00217-0
4893 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(98)00217-0
503 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(98)00217-0
5385 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(98)00217-0
CHEMBL2 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(98)00217-0
DB00457 3102 71 None -1 10 Rat 8.6 pKd = 8.6 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(98)00217-0
10549596 84168 0 None - 0 Rat 8.6 pKd = 8.6 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153553 84168 0 None - 0 Rat 8.6 pKd = 8.6 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2221147 84168 0 None - 0 Rat 8.6 pKd = 8.6 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
10456471 100054 0 None - 0 Rat 8.5 pKd = 8.5 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 451 6 1 7 2.4 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
CHEMBL291303 100054 0 None - 0 Rat 8.5 pKd = 8.5 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 451 6 1 7 2.4 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
11133868 154791 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNC[C@H]1C[C@H](c2ccccc2)c2ccccc2S1 10.1021/jm011066n
CHEMBL40325 154791 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNC[C@H]1C[C@H](c2ccccc2)c2ccccc2S1 10.1021/jm011066n
115 340 66 None - 0 Human 6.7 pKd = 6.7 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm000541z
2092 340 66 None - 0 Human 6.7 pKd = 6.7 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm000541z
7109 340 66 None - 0 Human 6.7 pKd = 6.7 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm000541z
CHEMBL709 340 66 None - 0 Human 6.7 pKd = 6.7 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm000541z
DB00346 340 66 None - 0 Human 6.7 pKd = 6.7 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm000541z
11751173 63081 0 None - 0 Rat 7.6 pKd = 7.6 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 445 4 1 9 2.3 COc1cc2nc(N3CCN(C4=CC(=O)c5ccccc5C4=O)CC3)nc(N)c2cc1OC 10.1021/jm049153d
CHEMBL179743 63081 0 None - 0 Rat 7.6 pKd = 7.6 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 445 4 1 9 2.3 COc1cc2nc(N3CCN(C4=CC(=O)c5ccccc5C4=O)CC3)nc(N)c2cc1OC 10.1021/jm049153d
44586479 188032 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 572 10 1 8 2.6 COC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL503007 188032 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 572 10 1 8 2.6 COC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
115 340 66 None - 0 Rat 7.6 pKd = 7.6 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm000541z
2092 340 66 None - 0 Rat 7.6 pKd = 7.6 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm000541z
7109 340 66 None - 0 Rat 7.6 pKd = 7.6 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm000541z
CHEMBL709 340 66 None - 0 Rat 7.6 pKd = 7.6 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm000541z
DB00346 340 66 None - 0 Rat 7.6 pKd = 7.6 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm000541z
10620831 205150 0 None - 0 Rabbit 7.6 pKd = 7.6 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ccc(C(=O)N(C)C)cn2)CC1 10.1021/jm970166j
CHEMBL90778 205150 0 None - 0 Rabbit 7.6 pKd = 7.6 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ccc(C(=O)N(C)C)cn2)CC1 10.1021/jm970166j
44586430 186437 0 None - 0 Rat 7.6 pKd = 7.6 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 528 9 1 6 3.4 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL490865 186437 0 None - 0 Rat 7.6 pKd = 7.6 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 528 9 1 6 3.4 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
3157 1437 69 None - 7 Human 7.6 pKd = 7.6 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm000541z
7170 1437 69 None - 7 Human 7.6 pKd = 7.6 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm000541z
954 1437 69 None - 7 Human 7.6 pKd = 7.6 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm000541z
CHEMBL707 1437 69 None - 7 Human 7.6 pKd = 7.6 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm000541z
DB00590 1437 69 None - 7 Human 7.6 pKd = 7.6 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm000541z
135 2486 38 None -22 31 Human 6.6 pKd = 6.6 Functional
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00370a011
1796 2486 38 None -22 31 Human 6.6 pKd = 6.6 Functional
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00370a011
4184 2486 38 None -22 31 Human 6.6 pKd = 6.6 Functional
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00370a011
CHEMBL6437 2486 38 None -22 31 Human 6.6 pKd = 6.6 Functional
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00370a011
DB06148 2486 38 None -22 31 Human 6.6 pKd = 6.6 Functional
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00370a011
11273296 169717 0 None - 0 Rat 6.6 pKd = 6.6 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 586 11 1 8 2.9 CCOC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL444648 169717 0 None - 0 Rat 6.6 pKd = 6.6 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 586 11 1 8 2.9 CCOC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
10834793 84142 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153557 84142 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220925 84142 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
44289261 164349 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 417 9 1 4 5.1 COc1cccc(OC)c1OCCNCC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm011066n
CHEMBL42231 164349 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 417 9 1 4 5.1 COc1cccc(OC)c1OCCNCC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm011066n
10344976 100732 1 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 477 11 1 10 3.4 COc1cc2nc(N(C)CCSSCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL29591 100732 1 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 477 11 1 10 3.4 COc1cc2nc(N(C)CCSSCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1021/jm9810654
10363912 6445 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (alpha1A receptor)Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (alpha1A receptor)
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
CHEMBL1082862 6445 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (alpha1A receptor)Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (alpha1A receptor)
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
CHEMBL286003 6445 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (alpha1A receptor)Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (alpha1A receptor)
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
10344976 100732 1 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 477 11 1 10 3.4 COc1cc2nc(N(C)CCSSCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1016/s0960-894x(98)00217-0
CHEMBL29591 100732 1 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 477 11 1 10 3.4 COc1cc2nc(N(C)CCSSCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1016/s0960-894x(98)00217-0
10671310 205188 0 None - 0 Rabbit 8.5 pKd = 8.5 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 451 8 1 6 3.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL91036 205188 0 None - 0 Rabbit 8.5 pKd = 8.5 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 451 8 1 6 3.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OC(F)(F)F)CC1 10.1021/jm970166j
21473427 205239 0 None - 0 Rabbit 8.5 pKd = 8.5 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 410 8 1 5 3.3 COc1ccccc1N1CCN(CCCNc2c(C)cccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL91326 205239 0 None - 0 Rabbit 8.5 pKd = 8.5 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 410 8 1 5 3.3 COc1ccccc1N1CCN(CCCNc2c(C)cccc2C(=O)N(C)C)CC1 10.1021/jm970166j
148842 3871 21 None 12 2 Rat 8.4 pKd = 8.4 Functional
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm030825u
496 3871 21 None 12 2 Rat 8.4 pKd = 8.4 Functional
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm030825u
CHEMBL278865 3871 21 None 12 2 Rat 8.4 pKd = 8.4 Functional
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm030825u
489 145 22 None - 1 Rabbit 8.4 pKd = 8.4 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm970166j
5640 145 22 None - 1 Rabbit 8.4 pKd = 8.4 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm970166j
CHEMBL420060 145 22 None - 1 Rabbit 8.4 pKd = 8.4 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm970166j
44323803 204811 0 None - 0 Rabbit 8.4 pKd = 8.4 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 398 8 1 7 1.8 COc1ccccc1N1CCN(CCCNc2cncnc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL88633 204811 0 None - 0 Rabbit 8.4 pKd = 8.4 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 398 8 1 7 1.8 COc1ccccc1N1CCN(CCCNc2cncnc2C(=O)N(C)C)CC1 10.1021/jm970166j
10596968 205240 0 None - 0 Rabbit 8.4 pKd = 8.4 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 0 5 3.0 COc1ccccc1N1CCN(CCCOc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL91338 205240 0 None - 0 Rabbit 8.4 pKd = 8.4 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 0 5 3.0 COc1ccccc1N1CCN(CCCOc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10815708 205359 0 None - 0 Rabbit 8.4 pKd = 8.4 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 515 9 1 6 4.5 CN(C)C(=O)c1cnc2ccccc2c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL91989 205359 0 None - 0 Rabbit 8.4 pKd = 8.4 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 515 9 1 6 4.5 CN(C)C(=O)c1cnc2ccccc2c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
50905588 56044 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 mins
ChEMBL 406 7 2 6 2.1 COc1ccc(C[C@@H](C)NC[C@H]2Oc3ccccc3O[C@H]2C)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
CHEMBL1630941 56044 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 mins
ChEMBL 406 7 2 6 2.1 COc1ccc(C[C@@H](C)NC[C@H]2Oc3ccccc3O[C@H]2C)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
145971816 163969 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 412 8 1 6 2.6 COC(=O)Cc1ccc(OC[C@@H](O)CN2CCN(c3cc(C)ccc3C)CC2)cc1 10.1016/j.bmcl.2018.01.068
CHEMBL4214992 163969 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 412 8 1 6 2.6 COC(=O)Cc1ccc(OC[C@@H](O)CN2CCN(c3cc(C)ccc3C)CC2)cc1 10.1016/j.bmcl.2018.01.068
44428851 91872 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractionAntagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction
ChEMBL 447 4 1 7 3.5 COc1cc2nc(N3CCN(C(=O)c4ccccc4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
CHEMBL242934 91872 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractionAntagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction
ChEMBL 447 4 1 7 3.5 COc1cc2nc(N3CCN(C(=O)c4ccccc4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
145962817 160960 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 385 3 1 7 2.2 COc1cc2nc(N3CCN(C(C)=O)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4128311 160960 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 385 3 1 7 2.2 COc1cc2nc(N3CCN(C(C)=O)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
10788615 205278 0 None - 0 Rabbit 7.5 pKd = 7.5 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 427 9 1 7 2.4 COc1ccc(N2CCN(CCCNc3ncccc3C(=O)N(C)C)CC2)c(OC)c1 10.1021/jm970166j
CHEMBL91480 205278 0 None - 0 Rabbit 7.5 pKd = 7.5 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 427 9 1 7 2.4 COc1ccc(N2CCN(CCCNc3ncccc3C(=O)N(C)C)CC2)c(OC)c1 10.1021/jm970166j
10598692 205405 0 None - 0 Rabbit 7.5 pKd = 7.5 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 429 9 1 5 4.6 COc1ccccc1N1CCN(CCCNc2ccccc2C(=O)c2ccccc2)CC1 10.1021/jm970166j
CHEMBL92259 205405 0 None - 0 Rabbit 7.5 pKd = 7.5 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 429 9 1 5 4.6 COc1ccccc1N1CCN(CCCNc2ccccc2C(=O)c2ccccc2)CC1 10.1021/jm970166j
4418 33985 80 None - 3 Rat 7.5 pKd = 7.5 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2018.01.068
CHEMBL142635 33985 80 None - 3 Rat 7.5 pKd = 7.5 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2018.01.068
132266 1247 9 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/s0960-894x(98)00217-0
486 1247 9 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/s0960-894x(98)00217-0
CHEMBL423294 1247 9 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/s0960-894x(98)00217-0
11133288 165469 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 407 12 1 5 4.3 COc1cccc(OC)c1OCCNCCOc1ccccc1Cc1ccccc1 10.1021/jm011066n
CHEMBL42558 165469 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 407 12 1 5 4.3 COc1cccc(OC)c1OCCNCCOc1ccccc1Cc1ccccc1 10.1021/jm011066n
16721032 91742 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractionAntagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction
ChEMBL 451 4 1 8 3.4 COc1cc2nc(N3CCN(C(=O)c4ccc(C)o4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
CHEMBL242507 91742 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractionAntagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction
ChEMBL 451 4 1 8 3.4 COc1cc2nc(N3CCN(C(=O)c4ccc(C)o4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
10348924 17748 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 620 10 1 10 3.8 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C#N)CC3)cccc2c1=O 10.1021/jm030825u
CHEMBL125989 17748 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 620 10 1 10 3.8 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C#N)CC3)cccc2c1=O 10.1021/jm030825u
44417706 11715 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 395 8 1 6 3.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cc3ccccc3cc2O1 10.1021/jm060358r
CHEMBL1182152 11715 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 395 8 1 6 3.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cc3ccccc3cc2O1 10.1021/jm060358r
CHEMBL215188 11715 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 395 8 1 6 3.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cc3ccccc3cc2O1 10.1021/jm060358r
3584 3706 60 None -54 8 Human 7.4 pKd = 7.4 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
5401 3706 60 None -54 8 Human 7.4 pKd = 7.4 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
7302 3706 60 None -54 8 Human 7.4 pKd = 7.4 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
CHEMBL611 3706 60 None -54 8 Human 7.4 pKd = 7.4 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
DB01162 3706 60 None -54 8 Human 7.4 pKd = 7.4 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
3584 3706 60 None -54 8 Human 7.4 pKd = 7.4 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm000541z
5401 3706 60 None -54 8 Human 7.4 pKd = 7.4 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm000541z
7302 3706 60 None -54 8 Human 7.4 pKd = 7.4 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm000541z
CHEMBL611 3706 60 None -54 8 Human 7.4 pKd = 7.4 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm000541z
DB01162 3706 60 None -54 8 Human 7.4 pKd = 7.4 Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm000541z
10072518 35661 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 451 11 1 7 4.0 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL144224 35661 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 451 11 1 7 4.0 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3)nc(N)c2cc1OC 10.1021/jm9810654
10553385 118647 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 498 13 1 9 3.7 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CN(C)C)o3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL342997 118647 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 498 13 1 9 3.7 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CN(C)C)o3)nc(N)c2cc1OC 10.1021/jm9810654
145964162 163773 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 412 8 1 6 2.6 COC(=O)Cc1ccc(OCC(O)CN2CCN(c3cc(C)ccc3C)CC2)cc1 10.1016/j.bmcl.2018.01.068
CHEMBL4212528 163773 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 412 8 1 6 2.6 COC(=O)Cc1ccc(OCC(O)CN2CCN(c3cc(C)ccc3C)CC2)cc1 10.1016/j.bmcl.2018.01.068
10621592 84134 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153559 84134 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220898 84134 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
9838192 110811 13 None - 3 Rat 5.4 pKd = 5.4 Functional
Antagonist activity at rat spleen adrenergic alpha1A receptorAntagonist activity at rat spleen adrenergic alpha1A receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmc.2008.02.091
CHEMBL326702 110811 13 None - 3 Rat 5.4 pKd = 5.4 Functional
Antagonist activity at rat spleen adrenergic alpha1A receptorAntagonist activity at rat spleen adrenergic alpha1A receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmc.2008.02.091
44289248 168399 0 None - 0 Rat 8.3 pKd = 8.3 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2S1 10.1021/jm011066n
CHEMBL43905 168399 0 None - 0 Rat 8.3 pKd = 8.3 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2S1 10.1021/jm011066n
10767688 36140 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 499 12 1 7 4.7 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CCl)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL144677 36140 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 499 12 1 7 4.7 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CCl)nc(N)c2cc1OC 10.1021/jm9810654
11994673 12195 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL1185036 12195 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL385371 12195 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
10430193 161038 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 385 3 1 7 2.2 COc1cc2nc(N3CCN(C(C)=O)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4129461 161038 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 385 3 1 7 2.2 COc1cc2nc(N3CCN(C(C)=O)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
10719536 120617 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 480 12 2 8 3.5 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CN)c3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL357669 120617 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 480 12 2 8 3.5 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CN)c3)nc(N)c2cc1OC 10.1021/jm9810654
145978803 163275 0 None - 0 Rat 6.3 pKd = 6.3 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 398 8 1 6 2.3 COC(=O)Cc1ccc(OCC(O)CN2CCN(c3ccccc3C)CC2)cc1 10.1016/j.bmcl.2018.01.068
CHEMBL4206435 163275 0 None - 0 Rat 6.3 pKd = 6.3 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 398 8 1 6 2.3 COC(=O)Cc1ccc(OCC(O)CN2CCN(c3ccccc3C)CC2)cc1 10.1016/j.bmcl.2018.01.068
4209 3102 71 None - 10 Rabbit 8.3 pKd = 8.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
4893 3102 71 None - 10 Rabbit 8.3 pKd = 8.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
503 3102 71 None - 10 Rabbit 8.3 pKd = 8.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
5385 3102 71 None - 10 Rabbit 8.3 pKd = 8.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
CHEMBL2 3102 71 None - 10 Rabbit 8.3 pKd = 8.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
DB00457 3102 71 None - 10 Rabbit 8.3 pKd = 8.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
10643699 204815 0 None - 0 Rabbit 8.3 pKd = 8.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 7 2 6 2.1 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2O)CC1 10.1021/jm970166j
CHEMBL88664 204815 0 None - 0 Rabbit 8.3 pKd = 8.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 7 2 6 2.1 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2O)CC1 10.1021/jm970166j
44289262 100891 1 None - 0 Rat 8.2 pKd = 8.2 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 421 9 1 6 4.3 COc1cccc(OC)c1OCCNC[C@@H]1Oc2ccccc2O[C@H]1c1ccccc1 10.1021/jm011066n
CHEMBL297106 100891 1 None - 0 Rat 8.2 pKd = 8.2 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 421 9 1 6 4.3 COc1cccc(OC)c1OCCNC[C@@H]1Oc2ccccc2O[C@H]1c1ccccc1 10.1021/jm011066n
44289262 100891 1 None - 0 Rat 8.2 pKd = 8.2 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 421 9 1 6 4.3 COc1cccc(OC)c1OCCNC[C@@H]1Oc2ccccc2O[C@H]1c1ccccc1 10.1021/jm011066n
CHEMBL297106 100891 1 None - 0 Rat 8.2 pKd = 8.2 Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 421 9 1 6 4.3 COc1cccc(OC)c1OCCNC[C@@H]1Oc2ccccc2O[C@H]1c1ccccc1 10.1021/jm011066n
71454865 84166 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153551 84166 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2221145 84166 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
3894573 3329 4 None - 0 Rabbit 7.3 pKd = 7.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1021/jm970166j
495 3329 4 None - 0 Rabbit 7.3 pKd = 7.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1021/jm970166j
CHEMBL88272 3329 4 None - 0 Rabbit 7.3 pKd = 7.3 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1021/jm970166j
10621592 84134 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153559 84134 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220898 84134 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
10097792 118071 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 508 13 1 8 4.1 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CN(C)C)c3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL341665 118071 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 508 13 1 8 4.1 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CN(C)C)c3)nc(N)c2cc1OC 10.1021/jm9810654
44417713 12301 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1185884 12301 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL439346 12301 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
10602797 36255 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 552 13 1 9 4.5 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CN4CCSC4)cc3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL144768 36255 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 552 13 1 9 4.5 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CN4CCSC4)cc3)nc(N)c2cc1OC 10.1021/jm9810654
11133288 165469 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 407 12 1 5 4.3 COc1cccc(OC)c1OCCNCCOc1ccccc1Cc1ccccc1 10.1021/jm011066n
CHEMBL42558 165469 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 407 12 1 5 4.3 COc1cccc(OC)c1OCCNCCOc1ccccc1Cc1ccccc1 10.1021/jm011066n
11994665 11714 0 None - 0 Rat 8.2 pKd = 8.2 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 391 8 1 5 4.2 COc1cccc(-c2ccccc2)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182151 11714 0 None - 0 Rat 8.2 pKd = 8.2 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 391 8 1 5 4.2 COc1cccc(-c2ccccc2)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL215151 11714 0 None - 0 Rat 8.2 pKd = 8.2 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 391 8 1 5 4.2 COc1cccc(-c2ccccc2)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
44289248 168399 0 None - 0 Rat 8.2 pKd = 8.2 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2S1 10.1021/jm011066n
CHEMBL43905 168399 0 None - 0 Rat 8.2 pKd = 8.2 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2S1 10.1021/jm011066n
10974101 116440 0 None - 0 Rat 8.2 pKd = 8.2 Functional
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 609 10 1 9 4.2 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C)CC3)cccc2c1=O 10.1021/jm030825u
CHEMBL338608 116440 0 None - 0 Rat 8.2 pKd = 8.2 Functional
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 609 10 1 9 4.2 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C)CC3)cccc2c1=O 10.1021/jm030825u
2142 3035 54 None - 14 Rabbit 8.2 pKd = 8.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
4920903 3035 54 None - 14 Rabbit 8.2 pKd = 8.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
502 3035 54 None - 14 Rabbit 8.2 pKd = 8.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
5775 3035 54 None - 14 Rabbit 8.2 pKd = 8.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
CHEMBL597 3035 54 None - 14 Rabbit 8.2 pKd = 8.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
DB00692 3035 54 None - 14 Rabbit 8.2 pKd = 8.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
10766280 111136 0 None - 0 Rabbit 8.2 pKd = 8.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 457 9 1 5 4.0 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2Cc2ccccc2)CC1 10.1021/jm970166j
CHEMBL328545 111136 0 None - 0 Rabbit 8.2 pKd = 8.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 457 9 1 5 4.0 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2Cc2ccccc2)CC1 10.1021/jm970166j
10642742 205058 0 None - 0 Rabbit 8.2 pKd = 8.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 367 7 1 5 2.4 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2)CC1 10.1021/jm970166j
CHEMBL90287 205058 0 None - 0 Rabbit 8.2 pKd = 8.2 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 367 7 1 5 2.4 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2)CC1 10.1021/jm970166j
10814913 35674 0 None - 0 Rat 8.2 pKd = 8.2 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 489 12 1 8 4.3 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CCl)o3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL144238 35674 0 None - 0 Rat 8.2 pKd = 8.2 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 489 12 1 8 4.3 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CCl)o3)nc(N)c2cc1OC 10.1021/jm9810654
145975903 163258 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 412 8 1 6 2.6 COC(=O)Cc1ccc(OC[C@H](O)CN2CCN(c3cc(C)ccc3C)CC2)cc1 10.1016/j.bmcl.2018.01.068
CHEMBL4206260 163258 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
ChEMBL 412 8 1 6 2.6 COC(=O)Cc1ccc(OC[C@H](O)CN2CCN(c3cc(C)ccc3C)CC2)cc1 10.1016/j.bmcl.2018.01.068
11169638 16997 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 600 11 1 8 3.3 CCOC(=O)C(C)N1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL1256344 16997 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 600 11 1 8 3.3 CCOC(=O)C(C)N1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
11454386 62762 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 477 8 1 9 3.6 COc1cc2nc(N3CCN(C(=O)CCCCC4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
CHEMBL178923 62762 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 477 8 1 9 3.6 COc1cc2nc(N3CCN(C(=O)CCCCC4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
10552704 162885 0 None - 0 Rabbit 8.1 pKd = 8.1 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 479 8 1 6 4.0 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c(C)cccc23)CC1 10.1021/jm970166j
CHEMBL419867 162885 0 None - 0 Rabbit 8.1 pKd = 8.1 Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 479 8 1 6 4.0 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c(C)cccc23)CC1 10.1021/jm970166j
10767948 35705 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 508 13 1 8 4.1 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CN(C)C)cc3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL144263 35705 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 508 13 1 8 4.1 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CN(C)C)cc3)nc(N)c2cc1OC 10.1021/jm9810654
11994915 11712 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 391 8 1 5 4.2 COc1cc(-c2ccccc2)ccc1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182145 11712 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 391 8 1 5 4.2 COc1cc(-c2ccccc2)ccc1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL214762 11712 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 391 8 1 5 4.2 COc1cc(-c2ccccc2)ccc1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
10743978 120776 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 499 12 1 7 4.7 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CCl)cc3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL358060 120776 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 499 12 1 7 4.7 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CCl)cc3)nc(N)c2cc1OC 10.1021/jm9810654
69781970 160792 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 477 5 1 8 4.0 COc1cc2nc(N3CCN(C(=O)OCc4ccccc4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4125981 160792 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 477 5 1 8 4.0 COc1cc2nc(N3CCN(C(=O)OCc4ccccc4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
10815228 37022 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 499 12 1 7 4.7 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CCl)c3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL145384 37022 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 499 12 1 7 4.7 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CCl)c3)nc(N)c2cc1OC 10.1021/jm9810654
10531768 35409 0 None - 0 Rat 8.1 pKd = 8.1 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 607 20 2 9 5.2 CNCCCCCCN(C)Cc1cccc(C(=O)N(C)CCCCCCN(C)c2nc(N)c3cc(OC)c(OC)cc3n2)c1 10.1021/jm9810654
CHEMBL144000 35409 0 None - 0 Rat 8.1 pKd = 8.1 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 607 20 2 9 5.2 CNCCCCCCN(C)Cc1cccc(C(=O)N(C)CCCCCCN(C)c2nc(N)c3cc(OC)c(OC)cc3n2)c1 10.1021/jm9810654
52941981 17319 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 502 7 1 5 3.1 CN1C(=O)N(CC(O)CN2CCN(c3ccccc3F)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL1257883 17319 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 502 7 1 5 3.1 CN1C(=O)N(CC(O)CN2CCN(c3ccccc3F)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
3584 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile response
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmcl.2018.01.068
5401 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile response
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmcl.2018.01.068
7302 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile response
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmcl.2018.01.068
CHEMBL611 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile response
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmcl.2018.01.068
DB01162 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile responseAntagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile response
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmcl.2018.01.068
3584 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
5401 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
7302 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
CHEMBL611 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
DB01162 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
3584 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm000541z
5401 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm000541z
7302 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm000541z
CHEMBL611 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm000541z
DB01162 3706 60 None -25 8 Rat 8.0 pKd = 8.0 Functional
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm000541z
11994797 12193 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 369 7 1 5 3.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)CCCC2 10.1021/jm060358r
CHEMBL1185017 12193 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 369 7 1 5 3.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)CCCC2 10.1021/jm060358r
CHEMBL383938 12193 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 369 7 1 5 3.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)CCCC2 10.1021/jm060358r
10553687 38630 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 508 13 1 8 4.1 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CN(C)C)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL146724 38630 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 508 13 1 8 4.1 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CN(C)C)nc(N)c2cc1OC 10.1021/jm9810654
49800167 17484 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 514 9 2 6 3.1 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)NC(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL1258457 17484 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Antagonist activity at adrenergic alpha1A receptor in rat tail arteryAntagonist activity at adrenergic alpha1A receptor in rat tail artery
ChEMBL 514 9 2 6 3.1 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)NC(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
2419 687 22 None - 3 Rat 7.0 pKd = 7.0 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm011066n
9 687 22 None - 3 Rat 7.0 pKd = 7.0 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm011066n
CHEMBL13647 687 22 None - 3 Rat 7.0 pKd = 7.0 Functional
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm011066n
9827677 167847 0 None - 0 Human 9.7 pKi = 9.7 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 510 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL43491 167847 0 None - 0 Human 9.7 pKi = 9.7 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 510 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
44288945 168338 0 None - 0 Human 9.4 pKi = 9.4 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 485 7 2 3 4.4 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL43860 168338 0 None - 0 Human 9.4 pKi = 9.4 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 485 7 2 3 4.4 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
499 4002 15 None - 1 Human 9.4 pKi = 9.4 Functional
Antagonistic affinity tested against isolated Human recombinant Thoracic Aorta Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Human recombinant Thoracic Aorta Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
5685 4002 15 None - 1 Human 9.4 pKi = 9.4 Functional
Antagonistic affinity tested against isolated Human recombinant Thoracic Aorta Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Human recombinant Thoracic Aorta Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
CHEMBL25554 4002 15 None - 1 Human 9.4 pKi = 9.4 Functional
Antagonistic affinity tested against isolated Human recombinant Thoracic Aorta Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Human recombinant Thoracic Aorta Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
44289100 99674 0 None - 0 Human 9.2 pKi = 9.2 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 499 7 1 3 4.7 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL287791 99674 0 None - 0 Human 9.2 pKi = 9.2 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 499 7 1 3 4.7 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
10436842 99779 0 None - 0 Human 9.1 pKi = 9.1 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 524 7 1 4 4.6 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL288772 99779 0 None - 0 Human 9.1 pKi = 9.1 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 524 7 1 4 4.6 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
44288874 100613 0 None - 0 Human 9.0 pKi = 9 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 528 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL295001 100613 0 None - 0 Human 9.0 pKi = 9 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 528 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
44289107 165616 0 None - 0 Human 9.0 pKi = 9 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 492 7 2 4 4.1 CC1=C(C(=O)NCCCN2CCC(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL42640 165616 0 None - 0 Human 9.0 pKi = 9 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 492 7 2 4 4.1 CC1=C(C(=O)NCCCN2CCC(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
44288769 100666 0 None - 0 Human 9.0 pKi = 9.0 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 542 7 1 4 4.5 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL295395 100666 0 None - 0 Human 9.0 pKi = 9.0 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 542 7 1 4 4.5 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
44288847 164746 0 None - 0 Human 8.9 pKi = 8.9 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 535 7 2 5 3.9 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL42335 164746 0 None - 0 Human 8.9 pKi = 8.9 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 535 7 2 5 3.9 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
44288917 99778 0 None - 0 Human 8.7 pKi = 8.7 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 510 7 2 4 4.0 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL288768 99778 0 None - 0 Human 8.7 pKi = 8.7 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 510 7 2 4 4.0 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
44289035 100035 0 None - 0 Human 8.7 pKi = 8.7 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 524 7 1 4 4.4 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL291166 100035 0 None - 0 Human 8.7 pKi = 8.7 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 524 7 1 4 4.4 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
53327992 63060 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation countingAntagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation counting
ChEMBL 461 7 0 5 3.6 COc1ccccc1N1CCN(CCCCN2C(=O)CC3(CCc4ccccc43)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796050 63060 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation countingAntagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation counting
ChEMBL 461 7 0 5 3.6 COc1ccccc1N1CCN(CCCCN2C(=O)CC3(CCc4ccccc43)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
71451044 80049 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146807 80049 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
25071930 18874 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 366 2 1 4 3.7 O=C1OC2(CCN(c3nc4cc(F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289039 18874 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 366 2 1 4 3.7 O=C1OC2(CCN(c3nc4cc(F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
25072242 19127 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 2 1 4 4.6 O=C1OC2(CCN(c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1290706 19127 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 2 1 4 4.6 O=C1OC2(CCN(c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
25022356 19128 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 348 2 1 4 3.6 O=C1OC2(CCN(c3nc4ccccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1290707 19128 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 348 2 1 4 3.6 O=C1OC2(CCN(c3nc4ccccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
71452871 80043 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146801 80043 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
71458203 80047 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146805 80047 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
25071310 18907 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 431 3 1 4 5.5 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289267 18907 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 431 3 1 4 5.5 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
25072876 19001 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 2 1 4 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.09.064
CHEMBL1289936 19001 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 2 1 4 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.09.064
44288843 168102 0 None - 0 Human 7.9 pKi = 7.9 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 531 7 1 5 4.1 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL43651 168102 0 None - 0 Human 7.9 pKi = 7.9 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 531 7 1 5 4.1 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
71461781 80044 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 409 7 0 4 4.9 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146802 80044 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 409 7 0 4 4.9 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
71458205 80053 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146811 80053 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
25072875 18958 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 446 3 1 5 5.2 Cc1cccc(N2C[C@]3(CC[C@@H](c4nc5cc(OC(F)(F)F)ccc5[nH]4)CC3)OC2=O)n1 10.1016/j.bmcl.2010.09.064
CHEMBL1289609 18958 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 446 3 1 5 5.2 Cc1cccc(N2C[C@]3(CC[C@@H](c4nc5cc(OC(F)(F)F)ccc5[nH]4)CC3)OC2=O)n1 10.1016/j.bmcl.2010.09.064
71456359 80045 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 411 7 0 5 3.8 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146803 80045 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 411 7 0 5 3.8 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
71449250 80046 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccncc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146804 80046 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccncc2c1=O 10.1016/j.bmc.2012.08.032
71458204 80051 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146809 80051 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
25071621 18893 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 3 1 5 4.5 O=C1OC2(CCN(c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289154 18893 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 3 1 5 4.5 O=C1OC2(CCN(c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
25073191 18943 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 3 1 5 4.9 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.09.064
CHEMBL1289503 18943 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 3 1 5 4.9 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.09.064
25071931 18991 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 415 2 1 3 5.6 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289820 18991 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 415 2 1 3 5.6 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
53327748 63043 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation countingAntagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation counting
ChEMBL 435 8 0 5 3.5 COc1ccccc1N1CCN(CCCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796033 63043 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation countingAntagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation counting
ChEMBL 435 8 0 5 3.5 COc1ccccc1N1CCN(CCCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
44288864 162898 0 None - 0 Human 6.6 pKi = 6.6 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 507 7 1 5 3.6 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL41996 162898 0 None - 0 Human 6.6 pKi = 6.6 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 507 7 1 5 3.6 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
44289103 155072 0 None - 0 Human 8.5 pKi = 8.5 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 506 7 1 4 4.4 CC1=C(C(=O)NCCCN2CCC(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL40464 155072 0 None - 0 Human 8.5 pKi = 8.5 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 506 7 1 4 4.4 CC1=C(C(=O)NCCCN2CCC(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
44288858 168578 0 None - 0 Human 8.5 pKi = 8.5 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 517 7 2 5 3.8 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL44042 168578 0 None - 0 Human 8.5 pKi = 8.5 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 517 7 2 5 3.8 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
49864841 15540 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human adrenergic alpha1A receptor assessed as intracellular calcium luminescence by cell based aequorin assayAntagonist activity at human adrenergic alpha1A receptor assessed as intracellular calcium luminescence by cell based aequorin assay
ChEMBL 266 1 1 4 1.6 C1=C(N2CCNCC2)c2nccn2Cc2ccccc21 10.1016/j.bmcl.2010.07.029
CHEMBL1222552 15540 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human adrenergic alpha1A receptor assessed as intracellular calcium luminescence by cell based aequorin assayAntagonist activity at human adrenergic alpha1A receptor assessed as intracellular calcium luminescence by cell based aequorin assay
ChEMBL 266 1 1 4 1.6 C1=C(N2CCNCC2)c2nccn2Cc2ccccc21 10.1016/j.bmcl.2010.07.029
53327991 63056 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation countingAntagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation counting
ChEMBL 449 8 0 5 3.7 COc1ccccc1N1CCN(CCCCN2C(=O)CC(C)(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796046 63056 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation countingAntagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation counting
ChEMBL 449 8 0 5 3.7 COc1ccccc1N1CCN(CCCCN2C(=O)CC(C)(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
15254720 60957 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL1767136 60957 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
24804150 80055 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 641 14 0 7 7.2 O=c1c2ccncc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
CHEMBL2146813 80055 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 641 14 0 7 7.2 O=c1c2ccncc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
71456360 80050 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146808 80050 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
2419 687 22 None - 3 Human 6.4 pKi = 6.4 Functional
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm021078o
9 687 22 None - 3 Human 6.4 pKi = 6.4 Functional
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm021078o
CHEMBL13647 687 22 None - 3 Human 6.4 pKi = 6.4 Functional
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm021078o
17747460 60985 8 None - 2 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
CHEMBL1767164 60985 8 None - 2 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
25071929 18873 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 426 2 1 4 4.3 O=C1OC2(CCN(c3nc4cc(Br)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289038 18873 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 426 2 1 4 4.3 O=C1OC2(CCN(c3nc4cc(Br)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
71456361 80054 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 369 4 0 6 2.5 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2nccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146812 80054 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 369 4 0 6 2.5 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2nccnc2c1=O 10.1016/j.bmc.2012.08.032
44288729 163176 0 None - 0 Human 7.4 pKi = 7.4 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 507 7 2 5 3.5 CC1=C(C(=O)NCC(C)CN2CCC(C#N)(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL42053 163176 0 None - 0 Human 7.4 pKi = 7.4 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 507 7 2 5 3.5 CC1=C(C(=O)NCC(C)CN2CCC(C#N)(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
2267 553 64 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
271 553 64 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
7121 553 64 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
CHEMBL639 553 64 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
DB00972 553 64 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
71454639 80052 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146810 80052 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
25073801 18975 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 450 3 1 5 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1cccc(F)n1 10.1016/j.bmcl.2010.09.064
CHEMBL1289714 18975 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 450 3 1 5 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1cccc(F)n1 10.1016/j.bmcl.2010.09.064
71461782 80048 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146806 80048 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
71452872 80009 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146484 80009 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingAntagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
44288877 168023 0 None - 0 Human 8.2 pKi = 8.2 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 549 7 1 5 4.3 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL43594 168023 0 None - 0 Human 8.2 pKi = 8.2 Functional
In vitro antagonism at Alpha-1A adrenergic receptorIn vitro antagonism at Alpha-1A adrenergic receptor
ChEMBL 549 7 1 5 4.3 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
25073189 18908 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 449 3 1 4 5.7 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1F 10.1016/j.bmcl.2010.09.064
CHEMBL1289268 18908 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 449 3 1 4 5.7 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1F 10.1016/j.bmcl.2010.09.064
25072880 18927 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 449 3 1 4 5.7 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccc(F)cc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289386 18927 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human alpha1A receptor expressed in rat 1 fibroblast cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 449 3 1 4 5.7 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccc(F)cc1 10.1016/j.bmcl.2010.09.064
135398745 2858 108 None -2 22 Rat 7.4 pA2 = 7.4 Functional
Measured as antagonism of phenylephrine-induced contraction of endothelium-denuded rat small mesenteric artery.Measured as antagonism of phenylephrine-induced contraction of endothelium-denuded rat small mesenteric artery.
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 18542932
47 2858 108 None -2 22 Rat 7.4 pA2 = 7.4 Functional
Measured as antagonism of phenylephrine-induced contraction of endothelium-denuded rat small mesenteric artery.Measured as antagonism of phenylephrine-induced contraction of endothelium-denuded rat small mesenteric artery.
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 18542932
CHEMBL715 2858 108 None -2 22 Rat 7.4 pA2 = 7.4 Functional
Measured as antagonism of phenylephrine-induced contraction of endothelium-denuded rat small mesenteric artery.Measured as antagonism of phenylephrine-induced contraction of endothelium-denuded rat small mesenteric artery.
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 18542932
DB00334 2858 108 None -2 22 Rat 7.4 pA2 = 7.4 Functional
Measured as antagonism of phenylephrine-induced contraction of endothelium-denuded rat small mesenteric artery.Measured as antagonism of phenylephrine-induced contraction of endothelium-denuded rat small mesenteric artery.
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 18542932
41835 215976 0 None -54 2 Human 6.1 pA2 = 6.1 Functional
NoneNone
Drug Central 372 8 4 6 1.9 CC(CCC1=CC2=C(OCO2)C=C1)NCC(O)C1=CC(C(N)=O)=C(O)C=C1 None
1753 2458 26 None -12 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC None
483 2458 26 None -12 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC None
6082 2458 26 None -12 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC None
CHEMBL524 2458 26 None -12 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC None
DB00723 2458 26 None -12 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC None
2435 713 98 None -14 8 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
395 713 98 None -14 8 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
520 713 98 None -14 8 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
5386 713 98 None -14 8 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
CHEMBL844 713 98 None -14 8 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
DB00484 713 98 None -14 8 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
521 1372 64 None -104 4 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
5311068 1372 64 None -104 4 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
835 1372 64 None -104 4 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
CHEMBL778 1372 64 None -104 4 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
DB00633 1372 64 None -104 4 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
2683 3762 57 None -1 3 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
5487 3762 57 None -1 3 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
7308 3762 57 None -1 3 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
CHEMBL1079 3762 57 None -1 3 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
DB00697 3762 57 None -1 3 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
2803 939 53 None -6 11 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 939 53 None -6 11 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 939 53 None -6 11 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 939 53 None -6 11 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 939 53 None -6 11 Bovine 8.2 pEC50 = 8.2 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
135 2486 38 None -2 31 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 None -2 31 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 None -2 31 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 None -2 31 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 None -2 31 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2801 161313 56 None -2 25 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL1200710 161313 56 None -2 25 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL415 161313 56 None -2 25 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
4543 169972 36 None -6 26 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL1201156 169972 36 None -6 26 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL445 169972 36 None -6 26 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
180 397 50 None -3 27 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 None -3 27 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 None -3 27 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 None -3 27 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 None -3 27 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1225 1438 24 None -5 11 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1438 24 None -5 11 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1438 24 None -5 11 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1438 24 None -5 11 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1438 24 None -5 11 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3823 49936 38 None 5 13 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
76973198 49936 38 None 5 13 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL157101 49936 38 None 5 13 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
2812 4696 96 None -3 39 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4696 96 None -3 39 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
1016 3678 75 None -41 35 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3678 75 None -41 35 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3678 75 None -41 35 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3678 75 None -41 35 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3678 75 None -41 35 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3678 75 None -41 35 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
3198 203792 73 None -1 36 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 203792 73 None -1 36 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 203792 73 None -1 36 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
448537 159691 86 None 7 26 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 159691 86 None 7 26 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
441383 20118 54 None 1 17 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL1306 20118 54 None 1 17 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
10219 188200 30 None -4 5 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 None
CHEMBL493439 188200 30 None -4 5 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 None
CHEMBL50588 188200 30 None -4 5 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 None
1599 2299 47 None -123 13 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
3955 2299 47 None -123 13 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
7215 2299 47 None -123 13 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
CHEMBL841 2299 47 None -123 13 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
DB00836 2299 47 None -123 13 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
2291 3123 52 None -3 10 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
2561 3123 52 None -3 10 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4932 3123 52 None -3 10 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
CHEMBL631 3123 52 None -3 10 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
DB01182 3123 52 None -3 10 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
1935 3664 92 None -1 8 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 None
2551 3664 92 None -1 8 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 None
6687 3664 92 None -1 8 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 None
CHEMBL95 3664 92 None -1 8 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 None
DB00382 3664 92 None -1 8 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 None
3191 102372 93 None -6 27 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102372 93 None -6 27 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
2351 3222 60 None -16 22 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2820 3222 60 None -16 22 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
5035 3222 60 None -16 22 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
CHEMBL81 3222 60 None -16 22 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
DB00481 3222 60 None -16 22 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2520 202301 65 None 1 12 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
CHEMBL1280 202301 65 None 1 12 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
CHEMBL6966 202301 65 None 1 12 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
2105 2993 34 None -22 19 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 2993 34 None -22 19 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 2993 34 None -22 19 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 2993 34 None -22 19 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 2993 34 None -22 19 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
1547484 925 70 None -1 19 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 925 70 None -1 19 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 925 70 None -1 19 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 925 70 None -1 19 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 925 70 None -1 19 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
2771 193337 67 None 2 7 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 193337 67 None 2 7 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 193337 67 None 2 7 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
1343 1850 55 None -7 8 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519 1850 55 None -7 8 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
522 1850 55 None -7 8 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
CHEMBL862 1850 55 None -7 8 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
DB01018 1850 55 None -7 8 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
102 4051 44 None -13 13 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 None -13 13 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 None -13 13 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 None -13 13 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 None -13 13 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
4735 193435 92 None 11 10 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
CHEMBL361506 193435 92 None 11 10 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
CHEMBL55 193435 92 None 11 10 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
12488 1619 51 None -2 25 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
941361 1619 51 None -2 25 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
CHEMBL30008 1619 51 None -2 25 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
DB04841 1619 51 None -2 25 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
1028 287 69 None -1 16 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 None -1 16 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 None -1 16 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 None -1 16 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 None -1 16 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 None -1 16 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
4011 81982 43 None -6 23 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 81982 43 None -6 23 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
3952 1849 33 None -1 14 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5353646 1849 33 None -1 14 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5443 1849 33 None -1 14 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5702063 1849 33 None -1 14 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL1331786 1849 33 None -1 14 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL420 1849 33 None -1 14 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
191 399 92 None -30 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 None -30 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 None -30 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 None -30 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 None -30 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
3151 1429 93 None -16 18 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 1429 93 None -16 18 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 1429 93 None -16 18 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 1429 93 None -16 18 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 1429 93 None -16 18 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
277 1269 55 None -40 25 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1269 55 None -40 25 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1269 55 None -40 25 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1269 55 None -40 25 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1269 55 None -40 25 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
6075 149563 36 None -1 16 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
CHEMBL395110 149563 36 None -1 16 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
1201549 590 22 None -57 20 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 590 22 None -57 20 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 590 22 None -57 20 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 590 22 None -57 20 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL438151 590 22 None -57 20 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 590 22 None -57 20 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
213 3780 50 None -3 18 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3780 50 None -3 18 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3780 50 None -3 18 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3780 50 None -3 18 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3780 50 None -3 18 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
36811 1421 34 None 3 7 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O None
535 1421 34 None 3 7 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O None
937 1421 34 None 3 7 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O None
CHEMBL926 1421 34 None 3 7 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O None
DB00841 1421 34 None 3 7 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O None
3033538 1287 36 None -3 8 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
7155 1287 36 None -3 8 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
781 1287 36 None -3 8 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
CHEMBL1201216 1287 36 None -3 8 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
DB00298 1287 36 None -3 8 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
133 2450 48 None -66 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2450 48 None -66 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2450 48 None -66 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2450 48 None -66 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2450 48 None -66 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2337 3193 72 None -1 22 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3193 72 None -1 22 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3193 72 None -1 22 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3193 72 None -1 22 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3193 72 None -1 22 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3193 72 None -3 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3193 72 None -3 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3193 72 None -3 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3193 72 None -3 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3193 72 None -3 22 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2286 3122 48 None -6 21 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3122 48 None -6 21 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3122 48 None -6 21 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3122 48 None -6 21 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3122 48 None -6 21 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
135398745 2858 108 None -2 22 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 None -2 22 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 None -2 22 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 None -2 22 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1531 2226 64 None -2 7 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869 2226 64 None -2 7 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
7207 2226 64 None -2 7 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
CHEMBL429 2226 64 None -2 7 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
DB00598 2226 64 None -2 7 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
2136 3034 29 None -1 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
4768 3034 29 None -1 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
7268 3034 29 None -1 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
CHEMBL753 3034 29 None -1 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
DB00925 3034 29 None -1 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
26987 934 29 None -46 21 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 934 29 None -46 21 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 934 29 None -46 21 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 934 29 None -46 21 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 934 29 None -46 21 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
2274 3112 53 None -2 26 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3112 53 None -2 26 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3112 53 None -2 26 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3112 53 None -2 26 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3112 53 None -2 26 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1427 1974 50 None -9 11 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1974 50 None -9 11 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1974 50 None -9 11 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1974 50 None -9 11 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1974 50 None -9 11 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
2247 502 77 None -1 34 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 502 77 None -1 34 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 502 77 None -1 34 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 502 77 None -1 34 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 502 77 None -1 34 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1212 1624 45 None -22 31 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1624 45 None -22 31 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1624 45 None -22 31 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1624 45 None -22 31 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1624 45 None -22 31 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1588 2284 24 None -77 20 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2284 24 None -77 20 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2284 24 None -77 20 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2284 24 None -77 20 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2284 24 None -77 20 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
180 397 50 None -16 27 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 None -16 27 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 None -16 27 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 None -16 27 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 None -16 27 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
100 3733 52 None -1 28 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3733 52 None -1 28 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3733 52 None -1 28 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3733 52 None -1 28 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3733 52 None -1 28 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
134551 355 25 None -15 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 355 25 None -15 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 355 25 None -15 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 355 25 None -15 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
2142 3035 54 None -8 14 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3035 54 None -8 14 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3035 54 None -8 14 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3035 54 None -8 14 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3035 54 None -8 14 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3035 54 None -8 14 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2284 3121 27 None -1 25 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3121 27 None -1 25 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3121 27 None -1 25 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3121 27 None -1 25 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3121 27 None -1 25 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2726 904 64 None -3 35 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 904 64 None -3 35 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 904 64 None -3 35 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 904 64 None -3 35 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 904 64 None -3 35 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
11954224 214164 0 None -1 5 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
2585 788 100 None -44 19 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 788 100 None -44 19 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 788 100 None -44 19 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 788 100 None -44 19 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 788 100 None -44 19 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
31101 719 39 None -12 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 719 39 None -12 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 719 39 None -12 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 719 39 None -12 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 719 39 None -12 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
100 3733 52 None -1 28 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3733 52 None -1 28 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3733 52 None -1 28 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3733 52 None -1 28 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3733 52 None -1 28 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
6761 67442 17 None -3 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 67442 17 None -3 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
10531 1387 18 None -7 18 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 1387 18 None -7 18 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 1387 18 None -7 18 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 1387 18 None -7 18 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 1387 18 None -7 18 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
3168 9157 84 None -1 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9157 84 None -1 17 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
107715 199250 18 None -2 19 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 199250 18 None -2 19 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 199250 18 None -2 19 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
3157 1437 69 None -2 7 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
7170 1437 69 None -2 7 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
954 1437 69 None -2 7 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
CHEMBL707 1437 69 None -2 7 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
DB00590 1437 69 None -2 7 Rat 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
4151 3537 85 None -1 5 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
Drug Central 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N None
493 3537 85 None -1 5 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
Drug Central 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N None
5312125 3537 85 None -1 5 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
Drug Central 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N None
CHEMBL24778 3537 85 None -1 5 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
Drug Central 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N None
DB06207 3537 85 None -1 5 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
Drug Central 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N None
213 3780 50 None 1 18 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3780 50 None 1 18 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3780 50 None 1 18 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3780 50 None 1 18 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3780 50 None 1 18 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2995 202690 49 None -2 7 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 202690 49 None -2 7 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 202690 49 None -2 7 Rat 8.0 pIC50 = 8.0 Functional
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
4011 81982 43 None -1 23 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 81982 43 None -1 23 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
4038180 202 11 None -2 5 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 7616455
4038180 202 11 None -2 5 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 9249248
480 202 11 None -2 5 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 7616455
480 202 11 None -2 5 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 9249248
CHEMBL109783 202 11 None -2 5 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 7616455
CHEMBL109783 202 11 None -2 5 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 9249248




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
129211 3680 75 None -1 16 Human 10.2 pEC50 = 10.2 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmc.2016.09.017
2562 3680 75 None -1 16 Human 10.2 pEC50 = 10.2 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmc.2016.09.017
488 3680 75 None -1 16 Human 10.2 pEC50 = 10.2 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmc.2016.09.017
CHEMBL836 3680 75 None -1 16 Human 10.2 pEC50 = 10.2 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmc.2016.09.017
DB00706 3680 75 None -1 16 Human 10.2 pEC50 = 10.2 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmc.2016.09.017
132578519 149165 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 484 10 1 5 4.3 CC(C)Oc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2F)CC1 10.1016/j.bmc.2016.09.017
CHEMBL3947830 149165 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 484 10 1 5 4.3 CC(C)Oc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2F)CC1 10.1016/j.bmc.2016.09.017
134154987 150287 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 438 9 1 5 3.4 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmc.2016.09.017
CHEMBL3956998 150287 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 438 9 1 5 3.4 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmc.2016.09.017
9813756 8913 0 None - 3 Rabbit 5.9 pEC50 = 5.9 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 255 2 2 2 2.8 CC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL109848 8913 0 None - 3 Rabbit 5.9 pEC50 = 5.9 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 255 2 2 2 2.8 CC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
118727916 120169 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 335 6 0 3 2.9 O=C1CCCN1CCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2015.03.009
CHEMBL3400597 120169 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 335 6 0 3 2.9 O=C1CCCN1CCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2015.03.009
CHEMBL3547118 120169 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 335 6 0 3 2.9 O=C1CCCN1CCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2015.03.009
134156323 153711 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 455 9 1 6 3.3 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cncc3ccccc23)CC1 10.1016/j.bmc.2016.09.017
CHEMBL3986337 153711 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 455 9 1 6 3.3 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cncc3ccccc23)CC1 10.1016/j.bmc.2016.09.017
134148920 147905 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 456 9 1 5 3.6 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cc(Cl)ccc2F)CC1 10.1016/j.bmc.2016.09.017
CHEMBL3937911 147905 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 456 9 1 5 3.6 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cc(Cl)ccc2F)CC1 10.1016/j.bmc.2016.09.017
9944409 7517 0 None - 5 Rabbit 7.8 pEC50 = 7.8 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 307 3 3 4 2.0 CS(=O)(=O)Nc1c(O)ccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL108804 7517 0 None - 5 Rabbit 7.8 pEC50 = 7.8 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 307 3 3 4 2.0 CS(=O)(=O)Nc1c(O)ccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
134151231 151667 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 464 11 1 7 2.8 COc1ccc(S(=O)(=O)NCC2CCN(CCOc3ccccc3OC)CC2)cc1OC 10.1016/j.bmc.2016.09.017
CHEMBL3968662 151667 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 464 11 1 7 2.8 COc1ccc(S(=O)(=O)NCC2CCN(CCOc3ccccc3OC)CC2)cc1OC 10.1016/j.bmc.2016.09.017
76326541 84903 0 None - 4 Rabbit 6.8 pEC50 = 6.8 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCC[C@H]2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL2261355 84903 0 None - 4 Rabbit 6.8 pEC50 = 6.8 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCC[C@H]2c1c[nH]cn1 10.1007/s00044-004-0020-z
168290235 192356 0 None -16 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192356 0 None -16 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192356 0 None -16 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
9815005 109160 0 None - 3 Rabbit 4.7 pEC50 = 4.7 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 305 3 2 3 2.6 CS(=O)(=O)Nc1cccc2c1CCCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL322492 109160 0 None - 3 Rabbit 4.7 pEC50 = 4.7 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 305 3 2 3 2.6 CS(=O)(=O)Nc1cccc2c1CCCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
134148037 149228 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 450 10 1 7 2.5 COc1ccc(S(=O)(=O)NC2CCN(CCOc3ccccc3OC)CC2)cc1OC 10.1016/j.bmc.2016.09.017
CHEMBL3948333 149228 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 450 10 1 7 2.5 COc1ccc(S(=O)(=O)NC2CCN(CCOc3ccccc3OC)CC2)cc1OC 10.1016/j.bmc.2016.09.017
164612037 184785 0 None -4 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 184785 0 None -4 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
146762 13184 6 None - 0 Human 7.6 pEC50 = 7.6 Binding
Effective concentration (EC50) against alpha-1-adrenoceptor in the isolated rabbit ear arteryEffective concentration (EC50) against alpha-1-adrenoceptor in the isolated rabbit ear artery
ChEMBL 244 5 3 4 0.5 CNCCc1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm00380a017
CHEMBL1191956 13184 6 None - 0 Human 7.6 pEC50 = 7.6 Binding
Effective concentration (EC50) against alpha-1-adrenoceptor in the isolated rabbit ear arteryEffective concentration (EC50) against alpha-1-adrenoceptor in the isolated rabbit ear artery
ChEMBL 244 5 3 4 0.5 CNCCc1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm00380a017
CHEMBL543126 13184 6 None - 0 Human 7.6 pEC50 = 7.6 Binding
Effective concentration (EC50) against alpha-1-adrenoceptor in the isolated rabbit ear arteryEffective concentration (EC50) against alpha-1-adrenoceptor in the isolated rabbit ear artery
ChEMBL 244 5 3 4 0.5 CNCCc1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm00380a017
9903797 9333 5 None - 4 Rabbit 5.6 pEC50 = 5.6 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 279 5 2 3 2.1 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1C 10.1007/s00044-004-0020-z
CHEMBL111734 9333 5 None - 4 Rabbit 5.6 pEC50 = 5.6 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 279 5 2 3 2.1 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1C 10.1007/s00044-004-0020-z
11183468 109371 2 None - 6 Rabbit 6.6 pEC50 = 6.6 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 213 1 2 2 2.5 Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL323402 109371 2 None - 6 Rabbit 6.6 pEC50 = 6.6 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 213 1 2 2 2.5 Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
9950711 108706 0 None - 4 Rabbit 5.6 pEC50 = 5.6 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 359 4 2 3 3.2 O=S(=O)(CC(F)(F)F)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL321644 108706 0 None - 4 Rabbit 5.6 pEC50 = 5.6 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 359 4 2 3 3.2 O=S(=O)(CC(F)(F)F)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
118727910 120157 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 427 8 0 3 4.1 O=C1CCCN1CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.03.009
CHEMBL3400594 120157 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 427 8 0 3 4.1 O=C1CCCN1CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.03.009
CHEMBL3547015 120157 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 427 8 0 3 4.1 O=C1CCCN1CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.03.009
134136412 142410 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 483 10 1 6 4.1 CC(C)Oc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc3cccnc23)CC1 10.1016/j.bmc.2016.09.017
CHEMBL3894175 142410 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 483 10 1 6 4.1 CC(C)Oc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc3cccnc23)CC1 10.1016/j.bmc.2016.09.017
168294767 192407 0 None -4 20 Human 5.5 pEC50 = 5.5 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192407 0 None -4 20 Human 5.5 pEC50 = 5.5 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192407 0 None -4 20 Human 5.5 pEC50 = 5.5 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
9904117 9297 3 None - 5 Rabbit 6.4 pEC50 = 6.4 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL111554 9297 3 None - 5 Rabbit 6.4 pEC50 = 6.4 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
3584 3706 60 None -2 14 Human 7.3 pEC50 = 7.3 Binding
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmc.2015.03.009
5401 3706 60 None -2 14 Human 7.3 pEC50 = 7.3 Binding
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmc.2015.03.009
7302 3706 60 None -2 14 Human 7.3 pEC50 = 7.3 Binding
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmc.2015.03.009
CHEMBL611 3706 60 None -2 14 Human 7.3 pEC50 = 7.3 Binding
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmc.2015.03.009
DB01162 3706 60 None -2 14 Human 7.3 pEC50 = 7.3 Binding
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmc.2015.03.009
3584 3706 60 None -2 14 Human 7.3 pEC50 = 7.3 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmc.2016.09.017
5401 3706 60 None -2 14 Human 7.3 pEC50 = 7.3 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmc.2016.09.017
7302 3706 60 None -2 14 Human 7.3 pEC50 = 7.3 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmc.2016.09.017
CHEMBL611 3706 60 None -2 14 Human 7.3 pEC50 = 7.3 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmc.2016.09.017
DB01162 3706 60 None -2 14 Human 7.3 pEC50 = 7.3 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.bmc.2016.09.017
9796525 9302 0 None - 3 Rabbit 5.3 pEC50 = 5.3 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 305 3 1 4 2.3 Cn1cnc(C2CCCc3c(NS(C)(=O)=O)cccc32)c1 10.1007/s00044-004-0020-z
CHEMBL111584 9302 0 None - 3 Rabbit 5.3 pEC50 = 5.3 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 305 3 1 4 2.3 Cn1cnc(C2CCCc3c(NS(C)(=O)=O)cccc32)c1 10.1007/s00044-004-0020-z
2146 3039 63 None -23 8 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assayAgonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1016/j.bmc.2015.03.009
485 3039 63 None -23 8 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assayAgonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1016/j.bmc.2015.03.009
6041 3039 63 None -23 8 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assayAgonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1016/j.bmc.2015.03.009
CHEMBL1215 3039 63 None -23 8 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assayAgonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1016/j.bmc.2015.03.009
DB00388 3039 63 None -23 8 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assayAgonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1016/j.bmc.2015.03.009
2146 3039 63 None -23 8 Human 7.3 pEC50 = 7.3 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1016/j.bmc.2016.09.017
485 3039 63 None -23 8 Human 7.3 pEC50 = 7.3 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1016/j.bmc.2016.09.017
6041 3039 63 None -23 8 Human 7.3 pEC50 = 7.3 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1016/j.bmc.2016.09.017
CHEMBL1215 3039 63 None -23 8 Human 7.3 pEC50 = 7.3 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1016/j.bmc.2016.09.017
DB00388 3039 63 None -23 8 Human 7.3 pEC50 = 7.3 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1016/j.bmc.2016.09.017
10267873 110158 0 None - 2 Rabbit 5.3 pEC50 = 5.3 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 317 4 2 3 2.8 O=S(=O)(Nc1cccc2c1CCCC2c1c[nH]cn1)C1CC1 10.1007/s00044-004-0020-z
CHEMBL325897 110158 0 None - 2 Rabbit 5.3 pEC50 = 5.3 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 317 4 2 3 2.8 O=S(=O)(Nc1cccc2c1CCCC2c1c[nH]cn1)C1CC1 10.1007/s00044-004-0020-z
9838192 110811 13 None - 6 Human 6.2 pEC50 = 6.2 Binding
Effective concentration in vitro against rabbit urethra Alpha-1A adrenergic receptorEffective concentration in vitro against rabbit urethra Alpha-1A adrenergic receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1021/jm025550h
CHEMBL326702 110811 13 None - 6 Human 6.2 pEC50 = 6.2 Binding
Effective concentration in vitro against rabbit urethra Alpha-1A adrenergic receptorEffective concentration in vitro against rabbit urethra Alpha-1A adrenergic receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1021/jm025550h
9838192 110811 13 None - 6 Rabbit 6.2 pEC50 = 6.2 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1007/s00044-004-0020-z
CHEMBL326702 110811 13 None - 6 Rabbit 6.2 pEC50 = 6.2 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1007/s00044-004-0020-z
9926529 9284 2 None - 5 Rabbit 6.2 pEC50 = 6.2 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL111496 9284 2 None - 5 Rabbit 6.2 pEC50 = 6.2 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
9879119 9340 0 None - 5 Rabbit 7.2 pEC50 = 7.2 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL111771 9340 0 None - 5 Rabbit 7.2 pEC50 = 7.2 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
11301627 9293 0 None - 2 Rabbit 5.2 pEC50 = 5.2 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 319 4 2 3 3.0 CC(C)S(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL111537 9293 0 None - 2 Rabbit 5.2 pEC50 = 5.2 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 319 4 2 3 3.0 CC(C)S(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
43260 5393 61 None - 5 Rabbit 5.2 pEC50 = 5.2 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1007/s00044-004-0020-z
CHEMBL1076 5393 61 None - 5 Rabbit 5.2 pEC50 = 5.2 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1007/s00044-004-0020-z
43260 5393 61 None - 5 Human 5.2 pEC50 = 5.2 Binding
Effective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptorEffective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptor
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1021/jm025550h
CHEMBL1076 5393 61 None - 5 Human 5.2 pEC50 = 5.2 Binding
Effective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptorEffective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptor
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1021/jm025550h
134136428 142598 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 456 9 1 5 3.6 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2F)CC1 10.1016/j.bmc.2016.09.017
CHEMBL3895815 142598 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 456 9 1 5 3.6 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2F)CC1 10.1016/j.bmc.2016.09.017
168295528 192419 0 None -4 20 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192419 0 None -4 20 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192419 0 None -4 20 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
4038180 202 11 None - 6 Human 8.0 pEC50 = 8.0 Binding
Effective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptorEffective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptor
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm025550h
480 202 11 None - 6 Human 8.0 pEC50 = 8.0 Binding
Effective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptorEffective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptor
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm025550h
CHEMBL109783 202 11 None - 6 Human 8.0 pEC50 = 8.0 Binding
Effective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptorEffective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptor
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm025550h
4038180 202 11 None - 6 Rabbit 8.0 pEC50 = 8.0 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
480 202 11 None - 6 Rabbit 8.0 pEC50 = 8.0 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
CHEMBL109783 202 11 None - 6 Rabbit 8.0 pEC50 = 8.0 Binding
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
132578518 148108 0 None - 0 Human 7.0 pEC50 = 7 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 441 8 1 6 3.1 COc1ccccc1OCCN1CCC(NS(=O)(=O)c2cncc3ccccc23)CC1 10.1016/j.bmc.2016.09.017
CHEMBL3939560 148108 0 None - 0 Human 7.0 pEC50 = 7 Binding
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
ChEMBL 441 8 1 6 3.1 COc1ccccc1OCCN1CCC(NS(=O)(=O)c2cncc3ccccc23)CC1 10.1016/j.bmc.2016.09.017
3158 55959 21 None -295 20 Rat 11.0 pIC50 = 11 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/jm9910369
CHEMBL1628227 55959 21 None -295 20 Rat 11.0 pIC50 = 11 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/jm9910369
180 397 50 None -10 39 Rat 10.7 pIC50 = 10.7 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
200 397 50 None -10 39 Rat 10.7 pIC50 = 10.7 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
2160 397 50 None -10 39 Rat 10.7 pIC50 = 10.7 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
CHEMBL629 397 50 None -10 39 Rat 10.7 pIC50 = 10.7 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
DB00321 397 50 None -10 39 Rat 10.7 pIC50 = 10.7 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
2801 161313 56 None -4 29 Rat 10.4 pIC50 = 10.4 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 10.1021/jm9910369
CHEMBL1200710 161313 56 None -4 29 Rat 10.4 pIC50 = 10.4 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 10.1021/jm9910369
CHEMBL415 161313 56 None -4 29 Rat 10.4 pIC50 = 10.4 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 10.1021/jm9910369
4543 169972 36 None -24 30 Rat 10.4 pIC50 = 10.4 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 10.1021/jm9910369
CHEMBL1201156 169972 36 None -24 30 Rat 10.4 pIC50 = 10.4 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 10.1021/jm9910369
CHEMBL445 169972 36 None -24 30 Rat 10.4 pIC50 = 10.4 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 10.1021/jm9910369
135 2486 38 None -46 58 Rat 10.2 pIC50 = 10.2 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm9910369
1796 2486 38 None -46 58 Rat 10.2 pIC50 = 10.2 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm9910369
4184 2486 38 None -46 58 Rat 10.2 pIC50 = 10.2 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm9910369
CHEMBL6437 2486 38 None -46 58 Rat 10.2 pIC50 = 10.2 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm9910369
DB06148 2486 38 None -46 58 Rat 10.2 pIC50 = 10.2 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm9910369
4209 3102 71 None -3 34 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
4893 3102 71 None -3 34 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
503 3102 71 None -3 34 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
5385 3102 71 None -3 34 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL2 3102 71 None -3 34 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
DB00457 3102 71 None -3 34 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
2995 202690 49 None - 23 Rat 9.6 pIC50 = 9.6 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm9910369
CHEMBL1696 202690 49 None - 23 Rat 9.6 pIC50 = 9.6 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm9910369
CHEMBL72 202690 49 None - 23 Rat 9.6 pIC50 = 9.6 Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm9910369
4209 3102 71 None -3 34 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm900458r
4893 3102 71 None -3 34 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm900458r
503 3102 71 None -3 34 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm900458r
5385 3102 71 None -3 34 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm900458r
CHEMBL2 3102 71 None -3 34 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm900458r
DB00457 3102 71 None -3 34 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm900458r
11638677 84152 0 None -5 6 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
ChEMBL 340 5 0 5 2.8 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2011.04.032
CHEMBL2153423 84152 0 None -5 6 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
ChEMBL 340 5 0 5 2.8 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2011.04.032
CHEMBL2220978 84152 0 None -5 6 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
ChEMBL 340 5 0 5 2.8 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2011.04.032
10809876 102167 0 None - 0 Bovine 9.3 pIC50 = 9.3 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 381 5 0 5 2.4 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCC(=O)N3C)CC1 10.1021/jm970298c
CHEMBL304438 102167 0 None - 0 Bovine 9.3 pIC50 = 9.3 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 381 5 0 5 2.4 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCC(=O)N3C)CC1 10.1021/jm970298c
76071739 142253 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@H]1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3892879 142253 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@H]1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
10547091 200404 0 None - 0 Bovine 9.2 pIC50 = 9.2 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 369 5 1 6 3.4 COc1ccccc1N1CCN(CCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
CHEMBL60885 200404 0 None - 0 Bovine 9.2 pIC50 = 9.2 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 369 5 1 6 3.4 COc1ccccc1N1CCN(CCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
122179430 120914 0 None -3 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 599 8 1 13 2.7 CCN(CC)c1ccc2cc(-n3cc(C(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)nn3)c(=O)oc2c1 10.1021/ml5004298
CHEMBL3582270 120914 0 None -3 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 599 8 1 13 2.7 CCN(CC)c1ccc2cc(-n3cc(C(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)nn3)c(=O)oc2c1 10.1021/ml5004298
4209 3102 71 None -3 34 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
4893 3102 71 None -3 34 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
503 3102 71 None -3 34 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
5385 3102 71 None -3 34 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
CHEMBL2 3102 71 None -3 34 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
DB00457 3102 71 None -3 34 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
3157 1437 69 None -1 12 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1016/j.ejmech.2017.10.026
7170 1437 69 None -1 12 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1016/j.ejmech.2017.10.026
954 1437 69 None -1 12 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1016/j.ejmech.2017.10.026
CHEMBL707 1437 69 None -1 12 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1016/j.ejmech.2017.10.026
DB00590 1437 69 None -1 12 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1016/j.ejmech.2017.10.026
4151 3537 85 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
493 3537 85 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
5312125 3537 85 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
CHEMBL24778 3537 85 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
DB06207 3537 85 None - 3 Rat 9.1 pIC50 = 9.1 Binding
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
10524876 201625 0 None - 0 Bovine 9.1 pIC50 = 9.1 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 397 7 1 6 4.2 COc1ccccc1N1CCN(CCCCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
CHEMBL64878 201625 0 None - 0 Bovine 9.1 pIC50 = 9.1 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 397 7 1 6 4.2 COc1ccccc1N1CCN(CCCCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
2389 3267 114 None -7 68 Rat 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3267 114 None -7 68 Rat 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3267 114 None -7 68 Rat 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3267 114 None -7 68 Rat 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3267 114 None -7 68 Rat 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
10691383 100295 0 None - 0 Bovine 9.0 pIC50 = 9 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 383 6 1 6 3.8 COc1ccccc1N1CCN(CCCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
CHEMBL292935 100295 0 None - 0 Bovine 9.0 pIC50 = 9 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 383 6 1 6 3.8 COc1ccccc1N1CCN(CCCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
19972363 93957 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 539 9 1 6 5.5 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OC(C)C)CC3)cccc2c1=O 10.1021/jm960697s
CHEMBL25098 93957 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 539 9 1 6 5.5 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OC(C)C)CC3)cccc2c1=O 10.1021/jm960697s
44275384 98341 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 529 7 1 5 5.7 Cc1ccc(Cl)cc1N1CCN(CCCNC(=O)c2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1 10.1021/jm960697s
CHEMBL278518 98341 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 529 7 1 5 5.7 Cc1ccc(Cl)cc1N1CCN(CCCNC(=O)c2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1 10.1021/jm960697s
2142 3035 54 None -2 37 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
4920903 3035 54 None -2 37 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
502 3035 54 None -2 37 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
5775 3035 54 None -2 37 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
CHEMBL597 3035 54 None -2 37 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
DB00692 3035 54 None -2 37 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
19972428 97632 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 496 8 0 6 5.6 COc1ccccc1N1CCN(CCCC(=O)c2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1 10.1021/jm960697s
CHEMBL27341 97632 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 496 8 0 6 5.6 COc1ccccc1N1CCN(CCCC(=O)c2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1 10.1021/jm960697s
3157 1437 69 None -1 12 Rat 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
7170 1437 69 None -1 12 Rat 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
954 1437 69 None -1 12 Rat 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
CHEMBL707 1437 69 None -1 12 Rat 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
DB00590 1437 69 None -1 12 Rat 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
107715 199250 18 None -1 20 Rat 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 199250 18 None -1 20 Rat 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 199250 18 None -1 20 Rat 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
3168 9157 84 None 1 22 Rat 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9157 84 None 1 22 Rat 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
1427 1974 50 None - 27 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm00172a035
357 1974 50 None - 27 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm00172a035
3696 1974 50 None - 27 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm00172a035
CHEMBL11 1974 50 None - 27 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm00172a035
DB00458 1974 50 None - 27 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm00172a035
9821397 100441 15 None - 0 Bovine 8.0 pIC50 = 8 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 383 5 0 6 3.0 COc1ccccc1N1CCN(CCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
CHEMBL293923 100441 15 None - 0 Bovine 8.0 pIC50 = 8 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 383 5 0 6 3.0 COc1ccccc1N1CCN(CCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
2389 3267 114 None -14 68 Human 8.0 pIC50 = 8 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2016.04.087
5073 3267 114 None -14 68 Human 8.0 pIC50 = 8 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2016.04.087
96 3267 114 None -14 68 Human 8.0 pIC50 = 8 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2016.04.087
CHEMBL85 3267 114 None -14 68 Human 8.0 pIC50 = 8 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2016.04.087
DB00734 3267 114 None -14 68 Human 8.0 pIC50 = 8 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2016.04.087
19972481 93063 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 498 9 0 6 5.8 COc1ccccc1N1CCN(CCCCOc2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1 10.1021/jm960697s
CHEMBL24629 93063 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 498 9 0 6 5.8 COc1ccccc1N1CCN(CCCCOc2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1 10.1021/jm960697s
119146 96690 15 None - 5 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]prazosin from rat cerebral cortex alpha1 adrenergic receptorDisplacement of [3H]prazosin from rat cerebral cortex alpha1 adrenergic receptor
ChEMBL 409 6 0 4 3.6 CN1CN(c2ccccc2)C2(CCN(CCCC(=O)c3ccc(F)cc3)CC2)C1=O 10.1021/acs.jmedchem.2c00633
CHEMBL267932 96690 15 None - 5 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]prazosin from rat cerebral cortex alpha1 adrenergic receptorDisplacement of [3H]prazosin from rat cerebral cortex alpha1 adrenergic receptor
ChEMBL 409 6 0 4 3.6 CN1CN(c2ccccc2)C2(CCN(CCCC(=O)c3ccc(F)cc3)CC2)C1=O 10.1021/acs.jmedchem.2c00633
10409553 18705 0 None - 0 Bovine 7.0 pIC50 = 7 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 414 5 1 5 3.1 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccccc3)CC1)O2 10.1021/jm00099a028
CHEMBL1203299 18705 0 None - 0 Bovine 7.0 pIC50 = 7 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 414 5 1 5 3.1 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccccc3)CC1)O2 10.1021/jm00099a028
CHEMBL128451 18705 0 None - 0 Bovine 7.0 pIC50 = 7 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 414 5 1 5 3.1 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccccc3)CC1)O2 10.1021/jm00099a028
11198145 9707 2 None 1 5 Human 7.0 pIC50 = 7 Binding
Inhibition of Alpha-1 adrenergic receptorInhibition of Alpha-1 adrenergic receptor
ChEMBL 325 5 2 3 3.8 C[C@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/jm990199u
CHEMBL113830 9707 2 None 1 5 Human 7.0 pIC50 = 7 Binding
Inhibition of Alpha-1 adrenergic receptorInhibition of Alpha-1 adrenergic receptor
ChEMBL 325 5 2 3 3.8 C[C@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/jm990199u
13520310 163276 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 281 4 1 2 3.7 CN(C)CC(c1ccc(Cl)cc1)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL420644 163276 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 281 4 1 2 3.7 CN(C)CC(c1ccc(Cl)cc1)C1(O)CCCCC1 10.1021/jm00172a035
10072866 195789 0 None - 0 Bovine 6.0 pIC50 = 6 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51561 195789 0 None - 0 Bovine 6.0 pIC50 = 6 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL56990 195789 0 None - 0 Bovine 6.0 pIC50 = 6 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10478362 19885 0 None - 0 Bovine 6.0 pIC50 = 6 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 439 5 1 6 3.0 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc(C#N)cc3)CC1)O2 10.1021/jm00099a028
CHEMBL1203297 19885 0 None - 0 Bovine 6.0 pIC50 = 6 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 439 5 1 6 3.0 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc(C#N)cc3)CC1)O2 10.1021/jm00099a028
CHEMBL130410 19885 0 None - 0 Bovine 6.0 pIC50 = 6 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 439 5 1 6 3.0 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc(C#N)cc3)CC1)O2 10.1021/jm00099a028
10048445 35036 4 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 432 5 1 3 4.6 Cc1ccc2c(c1)c(-c1ccc(F)cc1)c(C)n2C1=CCN(CCN2CCNC2=O)CC1 10.1021/jm00104a007
CHEMBL143617 35036 4 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 432 5 1 3 4.6 Cc1ccc2c(c1)c(-c1ccc(F)cc1)c(C)n2C1=CCN(CCN2CCNC2=O)CC1 10.1021/jm00104a007
10391177 188655 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.04.016
CHEMBL511747 188655 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.04.016
9978353 11134 0 None - 0 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
CHEMBL1178987 11134 0 None - 0 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
CHEMBL52785 11134 0 None - 0 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
11743327 98236 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1 10.1021/jm00038a007
CHEMBL27763 98236 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1 10.1021/jm00038a007
9975915 99262 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 362 9 0 5 2.8 CCCN(CCCCN1CCOCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL284912 99262 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 362 9 0 5 2.8 CCCN(CCCCN1CCOCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
11524225 188402 0 None - 1 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 403 4 0 5 4.3 Cc1cccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12 10.1016/j.bmcl.2008.10.034
CHEMBL508712 188402 0 None - 1 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 403 4 0 5 4.3 Cc1cccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12 10.1016/j.bmcl.2008.10.034
131001 98523 7 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 249 5 1 3 2.8 CCCN(CCC)C1COc2cccc(O)c2C1 10.1021/jm00038a007
CHEMBL27995 98523 7 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 249 5 1 3 2.8 CCCN(CCC)C1COc2cccc(O)c2C1 10.1021/jm00038a007
10364722 98615 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280608 98615 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51888 98615 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10199052 206205 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 258 5 3 4 1.0 O=C(NC1CC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL97044 206205 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 258 5 3 4 1.0 O=C(NC1CC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
3158 55959 21 None -295 20 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55959 21 None -295 20 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
11108001 10756 2 None -3 6 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL117248 10756 2 None -3 6 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL540542 10756 2 None -3 6 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
12488 1619 51 None -77 23 Rat 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1619 51 None -77 23 Rat 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1619 51 None -77 23 Rat 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1619 51 None -77 23 Rat 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
5656 201368 82 None - 43 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 10.1021/jm00172a035
CHEMBL637 201368 82 None - 43 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 10.1021/jm00172a035
134551 355 25 None -3 21 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 355 25 None -3 21 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 355 25 None -3 21 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 355 25 None -3 21 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
2142 3035 54 None -2 37 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
4920903 3035 54 None -2 37 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
502 3035 54 None -2 37 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
5775 3035 54 None -2 37 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
CHEMBL597 3035 54 None -2 37 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
DB00692 3035 54 None -2 37 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
73453 29388 22 None -6 17 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29388 22 None -6 17 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
10094822 164325 4 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 440 5 1 3 4.8 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00104a007
CHEMBL422130 164325 4 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 440 5 1 3 4.8 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00104a007
10595604 113625 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 374 5 0 4 4.1 Fc1ccc(-n2cc(OCCN3CCOCC3)c3cc(Cl)ccc32)cc1 10.1021/jm960159f
CHEMBL332913 113625 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 374 5 0 4 4.1 Fc1ccc(-n2cc(OCCN3CCOCC3)c3cc(Cl)ccc32)cc1 10.1021/jm960159f
36811 1421 34 None -2 7 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
535 1421 34 None -2 7 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
937 1421 34 None -2 7 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
CHEMBL926 1421 34 None -2 7 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
DB00841 1421 34 None -2 7 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
11668594 186082 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 405 7 0 5 4.9 CC(C)n1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL488251 186082 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 405 7 0 5 4.9 CC(C)n1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
44376958 57162 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1ccn2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc2c1 10.1016/s0960-894x(99)00591-0
CHEMBL165796 57162 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1ccn2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc2c1 10.1016/s0960-894x(99)00591-0
22120332 55739 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 389 4 0 6 3.4 COc1cccn2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc12 10.1016/s0960-894x(99)00591-0
CHEMBL162490 55739 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 389 4 0 6 3.4 COc1cccn2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc12 10.1016/s0960-894x(99)00591-0
10015132 163306 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
CHEMBL420683 163306 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
44573964 178068 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 483 7 0 4 4.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1 10.1016/j.bmcl.2009.04.016
CHEMBL467668 178068 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 483 7 0 4 4.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1 10.1016/j.bmcl.2009.04.016
213 3780 50 None -4 44 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3780 50 None -4 44 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3780 50 None -4 44 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3780 50 None -4 44 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3780 50 None -4 44 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
10503470 163760 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 444 9 1 4 4.1 CCN(CCOc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
CHEMBL421239 163760 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 444 9 1 4 4.1 CCN(CCOc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
127049863 139709 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
CHEMBL3805518 139709 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
240 929 39 None -4 25 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 929 39 None -4 25 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 929 39 None -4 25 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 929 39 None -4 25 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 929 39 None -4 25 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 929 39 None -4 25 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 929 39 None -4 25 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
85469808 136094 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 439 7 0 4 3.8 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3739900 136094 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 439 7 0 4 3.8 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmc.2015.11.020
42 2024 50 None - 18 Bovine 5.9 pIC50 = 5.9 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
56971 2024 50 None - 18 Bovine 5.9 pIC50 = 5.9 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
CHEMBL8412 2024 50 None - 18 Bovine 5.9 pIC50 = 5.9 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
4735 193435 92 None -77 10 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL361506 193435 92 None -77 10 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL55 193435 92 None -77 10 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
102 4051 44 None -1258 50 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
3659 4051 44 None -1258 50 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969 4051 44 None -1258 50 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
CHEMBL15245 4051 44 None -1258 50 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
DB01392 4051 44 None -1258 50 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
13520332 4214 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 263 5 1 3 2.6 COc1ccc(C(CN(C)C)C2(O)CCCC2)cc1 10.1021/jm00172a035
CHEMBL100774 4214 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 263 5 1 3 2.6 COc1ccc(C(CN(C)C)C2(O)CCCC2)cc1 10.1021/jm00172a035
85469757 136203 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 468 6 0 5 3.9 N#Cc1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)c(F)c1 10.1016/j.bmc.2015.11.020
CHEMBL3740874 136203 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 468 6 0 5 3.9 N#Cc1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)c(F)c1 10.1016/j.bmc.2015.11.020
44362511 118830 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 267 4 1 4 2.4 Cc1ccnc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL344294 118830 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 267 4 1 4 2.4 Cc1ccnc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
10829244 16316 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 316 4 0 2 4.5 CN(C)CCc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12 10.1021/jm960159f
CHEMBL123640 16316 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 316 4 0 2 4.5 CN(C)CCc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12 10.1021/jm960159f
10265758 4396 4 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 281 4 1 2 3.7 CN(C)CC(c1cccc(Cl)c1)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL101899 4396 4 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 281 4 1 2 3.7 CN(C)CC(c1cccc(Cl)c1)C1(O)CCCCC1 10.1021/jm00172a035
2995 202690 49 None - 23 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm00172a035
CHEMBL1696 202690 49 None - 23 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm00172a035
CHEMBL72 202690 49 None - 23 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm00172a035
11689687 190675 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 391 7 0 5 4.3 CCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL519067 190675 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 391 7 0 5 4.3 CCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
45485061 197066 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL583014 197066 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
441383 20118 54 None -257 17 Rat 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 20118 54 None -257 17 Rat 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
1343 1850 55 None -87 9 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
3519 1850 55 None -87 9 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
522 1850 55 None -87 9 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL862 1850 55 None -87 9 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
DB01018 1850 55 None -87 9 Rat 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
72197484 102008 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL2393243 102008 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL3040324 102008 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
10645487 15566 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 414 7 1 3 3.9 CN(CCc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12)CCN1CCNC1=O 10.1021/jm960159f
CHEMBL122269 15566 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 414 7 1 3 3.9 CN(CCc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12)CCN1CCNC1=O 10.1021/jm960159f
10788685 117943 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 428 8 1 3 4.3 CN(CCCN1CCNC1=O)CCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
CHEMBL341229 117943 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 428 8 1 3 4.3 CN(CCCN1CCNC1=O)CCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
19972519 93800 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 497 7 1 6 4.3 COc1ccccc1N1CCN(CCNC(=O)c2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1 10.1021/jm960697s
CHEMBL25012 93800 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 497 7 1 6 4.3 COc1ccccc1N1CCN(CCNC(=O)c2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1 10.1021/jm960697s
180 397 50 None -10 39 Rat 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -10 39 Rat 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -10 39 Rat 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -10 39 Rat 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -10 39 Rat 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
85469809 136165 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 467 7 0 5 4.1 CC(=O)c1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3740558 136165 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 467 7 0 5 4.1 CC(=O)c1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
10381889 106573 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against Alpha-1A adrenergic receptorBinding affinity against Alpha-1A adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL315772 106573 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against Alpha-1A adrenergic receptorBinding affinity against Alpha-1A adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
10381889 106573 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL315772 106573 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
5656 201368 82 None - 43 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 10.1021/jm00172a035
CHEMBL637 201368 82 None - 43 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 10.1021/jm00172a035
1201549 590 22 None -51 20 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 590 22 None -51 20 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 590 22 None -51 20 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 590 22 None -51 20 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 590 22 None -51 20 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 590 22 None -51 20 Rat 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
6075 149563 36 None -11 16 Rat 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 149563 36 None -11 16 Rat 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
11796106 15389 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 414 7 1 3 3.9 CN(CCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
CHEMBL122113 15389 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 414 7 1 3 3.9 CN(CCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
85469811 136348 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 459 6 0 4 4.5 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3742198 136348 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 459 6 0 4 4.5 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmc.2015.11.020
9886555 16303 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 387 5 0 4 4.0 CN1CCN(CCOc2cn(-c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1021/jm960159f
CHEMBL123584 16303 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 387 5 0 4 4.0 CN1CCN(CCOc2cn(-c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1021/jm960159f
13520317 4269 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 277 5 1 3 3.0 COc1cccc(C(CN(C)C)C2(O)CCCCC2)c1 10.1021/jm00172a035
CHEMBL101055 4269 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 277 5 1 3 3.0 COc1cccc(C(CN(C)C)C2(O)CCCCC2)c1 10.1021/jm00172a035
160023 19233 5 None - 0 Bovine 5.8 pIC50 = 5.8 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 456 5 1 8 2.6 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc4nonc4c3)CC1)O2 10.1021/jm00099a028
CHEMBL1204345 19233 5 None - 0 Bovine 5.8 pIC50 = 5.8 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 456 5 1 8 2.6 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc4nonc4c3)CC1)O2 10.1021/jm00099a028
CHEMBL129583 19233 5 None - 0 Bovine 5.8 pIC50 = 5.8 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 456 5 1 8 2.6 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc4nonc4c3)CC1)O2 10.1021/jm00099a028
10255678 116855 0 None - 0 Bovine 4.8 pIC50 = 4.8 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 507 7 2 7 2.5 CS(=O)(=O)Nc1ccc(CCN2CCC3(CC2)CC(=O)c2cc(NS(C)(=O)=O)ccc2O3)cc1 10.1021/jm00099a028
CHEMBL1203296 116855 0 None - 0 Bovine 4.8 pIC50 = 4.8 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 507 7 2 7 2.5 CS(=O)(=O)Nc1ccc(CCN2CCC3(CC2)CC(=O)c2cc(NS(C)(=O)=O)ccc2O3)cc1 10.1021/jm00099a028
CHEMBL339769 116855 0 None - 0 Bovine 4.8 pIC50 = 4.8 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 507 7 2 7 2.5 CS(=O)(=O)Nc1ccc(CCN2CCC3(CC2)CC(=O)c2cc(NS(C)(=O)=O)ccc2O3)cc1 10.1021/jm00099a028
85469698 136290 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 425 6 0 4 3.8 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3741658 136290 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 425 6 0 4 3.8 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2015.11.020
5282322 77844 16 None - 1 Rat 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 785 11 4 15 2.4 CO[C@@H]1[C@@H](O[C@@H]2O[C@H](C)[C@@H](O[C@H]3C[C@@](C)(O)[C@@H](OC(=O)CC(C)C)[C@H](C)O3)[C@H](N(C)C)[C@H]2O)[C@@H](CC=O)C[C@@H](C)[C@@H](O)/C=C/C=C/C[C@@H](C)OC(=O)C[C@H]1O nan
CHEMBL2106399 77844 16 None - 1 Rat 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 785 11 4 15 2.4 CO[C@@H]1[C@@H](O[C@@H]2O[C@H](C)[C@@H](O[C@H]3C[C@@](C)(O)[C@@H](OC(=O)CC(C)C)[C@H](C)O3)[C@H](N(C)C)[C@H]2O)[C@@H](CC=O)C[C@@H](C)[C@@H](O)/C=C/C=C/C[C@@H](C)OC(=O)C[C@H]1O nan
135398737 942 89 None - 92 Bovine 6.8 pIC50 = 6.8 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970298c
38 942 89 None - 92 Bovine 6.8 pIC50 = 6.8 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970298c
722 942 89 None - 92 Bovine 6.8 pIC50 = 6.8 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970298c
CHEMBL42 942 89 None - 92 Bovine 6.8 pIC50 = 6.8 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970298c
DB00363 942 89 None - 92 Bovine 6.8 pIC50 = 6.8 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970298c
2477 732 54 None - 29 Bovine 4.8 pIC50 = 4.8 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
36 732 54 None - 29 Bovine 4.8 pIC50 = 4.8 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
437 732 54 None - 29 Bovine 4.8 pIC50 = 4.8 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
CHEMBL49 732 54 None - 29 Bovine 4.8 pIC50 = 4.8 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
DB00490 732 54 None - 29 Bovine 4.8 pIC50 = 4.8 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
10246054 106049 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 330 2 0 3 3.7 CN(C)CC1CC2c3cc(F)ccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL314107 106049 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 330 2 0 3 3.7 CN(C)CC1CC2c3cc(F)ccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
44343410 11435 2 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 219 4 2 3 2.7 CSc1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL118055 11435 2 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 219 4 2 3 2.7 CSc1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
10592734 16885 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 332 5 0 3 4.4 CN(C)CCOc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
CHEMBL125483 16885 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 332 5 0 3 4.4 CN(C)CCOc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
8459 3234 3 None - 3 Bovine 7.8 pIC50 = 7.8 Binding
Binding affinity was tested on cloned bovine Alpha-1A adrenergic receptorBinding affinity was tested on cloned bovine Alpha-1A adrenergic receptor
ChEMBL 495 8 1 9 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)COc1c(OC)cccc1C(C)C 10.1021/jm960697s
9891980 3234 3 None - 3 Bovine 7.8 pIC50 = 7.8 Binding
Binding affinity was tested on cloned bovine Alpha-1A adrenergic receptorBinding affinity was tested on cloned bovine Alpha-1A adrenergic receptor
ChEMBL 495 8 1 9 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)COc1c(OC)cccc1C(C)C 10.1021/jm960697s
CHEMBL430717 3234 3 None - 3 Bovine 7.8 pIC50 = 7.8 Binding
Binding affinity was tested on cloned bovine Alpha-1A adrenergic receptorBinding affinity was tested on cloned bovine Alpha-1A adrenergic receptor
ChEMBL 495 8 1 9 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)COc1c(OC)cccc1C(C)C 10.1021/jm960697s
242 467 117 None -14 52 Human 6.8 pIC50 = 6.8 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
34 467 117 None -14 52 Human 6.8 pIC50 = 6.8 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
60795 467 117 None -14 52 Human 6.8 pIC50 = 6.8 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
CHEMBL1112 467 117 None -14 52 Human 6.8 pIC50 = 6.8 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
DB01238 467 117 None -14 52 Human 6.8 pIC50 = 6.8 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
10544602 116953 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 332 5 0 3 4.4 CN(C)CCOc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12 10.1021/jm960159f
CHEMBL339919 116953 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 332 5 0 3 4.4 CN(C)CCOc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12 10.1021/jm960159f
10739024 69475 0 None -33 6 Human 5.8 pIC50 = 5.8 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype.Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype.
ChEMBL 388 4 3 8 0.9 COc1cc2nc(N3CCN[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
CHEMBL19376 69475 0 None -33 6 Human 5.8 pIC50 = 5.8 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype.Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype.
ChEMBL 388 4 3 8 0.9 COc1cc2nc(N3CCN[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
2771 193337 67 None -8 27 Rat 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL1200781 193337 67 None -8 27 Rat 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL549 193337 67 None -8 27 Rat 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
10518508 101569 1 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 302 3 0 2 4.5 CN(C)Cc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
CHEMBL301956 101569 1 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 302 3 0 2 4.5 CN(C)Cc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
11502343 185558 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 405 8 0 5 4.7 CCCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL487230 185558 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 405 8 0 5 4.7 CCCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
10477439 35762 4 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 424 5 1 3 4.2 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3cc(F)ccc32)CC1 10.1021/jm00104a007
CHEMBL144318 35762 4 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 424 5 1 3 4.2 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3cc(F)ccc32)CC1 10.1021/jm00104a007
10426286 118835 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 322 2 0 2 5.0 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1CCN(C)CC1 10.1021/jm00104a007
CHEMBL344335 118835 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 322 2 0 2 5.0 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1CCN(C)CC1 10.1021/jm00104a007
10254306 120349 4 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 474 5 1 3 5.1 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3cc(C(F)(F)F)ccc32)CC1 10.1021/jm00104a007
CHEMBL355917 120349 4 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 474 5 1 3 5.1 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3cc(C(F)(F)F)ccc32)CC1 10.1021/jm00104a007
13520327 206614 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 355 5 1 3 3.8 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1Br 10.1021/jm00172a035
CHEMBL99503 206614 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 355 5 1 3 3.8 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1Br 10.1021/jm00172a035
19426635 203871 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL81485 203871 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
22493269 46548 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 256 4 2 5 2.1 Cc1ncoc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL154023 46548 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 256 4 2 5 2.1 Cc1ncoc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
22493289 49405 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 253 4 2 5 1.6 c1cnc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
CHEMBL156661 49405 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 253 4 2 5 1.6 c1cnc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
9934955 71917 0 None -489 6 Human 5.7 pIC50 = 5.7 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtypeCompound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype
ChEMBL 482 5 2 9 2.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
CHEMBL19826 71917 0 None -489 6 Human 5.7 pIC50 = 5.7 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtypeCompound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype
ChEMBL 482 5 2 9 2.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
25014630 83112 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of alpha1A adrenergic receptorInhibition of alpha1A adrenergic receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
CHEMBL2203713 83112 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of alpha1A adrenergic receptorInhibition of alpha1A adrenergic receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
44461606 105502 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 308 3 0 3 3.8 CN(C)CCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL313189 105502 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 308 3 0 3 3.8 CN(C)CCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
10073934 186897 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cncn1 10.1016/j.bmcl.2009.04.016
CHEMBL494155 186897 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cncn1 10.1016/j.bmcl.2009.04.016
44573932 186898 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 482 7 0 7 2.9 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cnnn1 10.1016/j.bmcl.2009.04.016
CHEMBL494156 186898 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 482 7 0 7 2.9 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cnnn1 10.1016/j.bmcl.2009.04.016
1547484 925 70 None -125 20 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 925 70 None -125 20 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 925 70 None -125 20 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 925 70 None -125 20 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 925 70 None -125 20 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
10345121 186860 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1ccnn1 10.1016/j.bmcl.2009.04.016
CHEMBL493967 186860 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1ccnn1 10.1016/j.bmcl.2009.04.016
2105 2993 34 None -1258 33 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 2993 34 None -1258 33 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 2993 34 None -1258 33 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 2993 34 None -1258 33 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 2993 34 None -1258 33 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
448537 159691 86 None -1584 25 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159691 86 None -1584 25 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
9837963 62627 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cellsInhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17851 62627 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cellsInhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
148842 3871 21 None -8 5 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm960697s
496 3871 21 None -8 5 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm960697s
CHEMBL278865 3871 21 None -8 5 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm960697s
85469933 136112 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 439 6 0 4 4.2 Cc1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3740019 136112 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 439 6 0 4 4.2 Cc1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
56961506 120912 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 544 5 2 13 1.6 COc1cc2nc(N3CCN(C(=O)c4cn(-c5cc6ccc(O)cc6oc5=O)nn4)CC3)nc(N)c2cc1OC 10.1021/ml5004298
CHEMBL3582269 120912 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 544 5 2 13 1.6 COc1cc2nc(N3CCN(C(=O)c4cn(-c5cc6ccc(O)cc6oc5=O)nn4)CC3)nc(N)c2cc1OC 10.1021/ml5004298
137380627 162104 2 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
ChEMBL 772 17 2 14 4.7 COc1cc2nc(N3CCN(C(=O)CCCCCCCCCCC(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)CC3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.10.026
CHEMBL4170029 162104 2 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
ChEMBL 772 17 2 14 4.7 COc1cc2nc(N3CCN(C(=O)CCCCCCCCCCC(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)CC3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.10.026
1353 1872 85 None - 86 Bovine 7.7 pIC50 = 7.7 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970298c
3559 1872 85 None - 86 Bovine 7.7 pIC50 = 7.7 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970298c
86 1872 85 None - 86 Bovine 7.7 pIC50 = 7.7 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970298c
CHEMBL54 1872 85 None - 86 Bovine 7.7 pIC50 = 7.7 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970298c
DB00502 1872 85 None - 86 Bovine 7.7 pIC50 = 7.7 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970298c
10573576 198738 0 None - 0 Bovine 7.7 pIC50 = 7.7 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 409 7 0 5 3.2 COc1ccccc1N1CCN(CCCCc2ccc3c(c2)OCC(=O)N3C)CC1 10.1021/jm970298c
CHEMBL59823 198738 0 None - 0 Bovine 7.7 pIC50 = 7.7 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 409 7 0 5 3.2 COc1ccccc1N1CCN(CCCCc2ccc3c(c2)OCC(=O)N3C)CC1 10.1021/jm970298c
10671211 201030 0 None - 0 Bovine 6.7 pIC50 = 6.7 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 449 6 0 5 4.8 Cn1c(=O)sc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
CHEMBL61818 201030 0 None - 0 Bovine 6.7 pIC50 = 6.7 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 449 6 0 5 4.8 Cn1c(=O)sc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
10319624 98517 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL27991 98517 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL298534 98517 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10265863 192711 0 None - 0 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1 10.1021/jm00038a007
CHEMBL52438 192711 0 None - 0 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1 10.1021/jm00038a007
9934955 71917 0 None -165 6 Rat 5.7 pIC50 = 5.7 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtypeCompound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype
ChEMBL 482 5 2 9 2.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
CHEMBL19826 71917 0 None -165 6 Rat 5.7 pIC50 = 5.7 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtypeCompound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype
ChEMBL 482 5 2 9 2.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
121852 10056 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 10056 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 10056 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
44376975 55680 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 435 5 0 5 4.6 O=c1c(CCN2CCc3oc4ccccc4c3C2)c(Cc2ccccc2)nc2ccccn12 10.1016/s0960-894x(99)00591-0
CHEMBL162436 55680 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 435 5 0 5 4.6 O=c1c(CCN2CCc3oc4ccccc4c3C2)c(Cc2ccccc2)nc2ccccn12 10.1016/s0960-894x(99)00591-0
9903313 172099 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 260 5 2 4 1.2 CCN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL450018 172099 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 260 5 2 4 1.2 CCN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
14739944 206649 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 261 4 1 2 3.3 Cc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 10.1021/jm00172a035
CHEMBL99670 206649 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 261 4 1 2 3.3 Cc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 10.1021/jm00172a035
2520 202301 65 None -147 12 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL1280 202301 65 None -147 12 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL6966 202301 65 None -147 12 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
3198 203792 73 None -1698 34 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203792 73 None -1698 34 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203792 73 None -1698 34 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
9951544 57063 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 375 3 0 5 3.8 Cc1nc2ccccn2c(=O)c1CCN1CCc2sc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL165181 57063 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 375 3 0 5 3.8 Cc1nc2ccccn2c(=O)c1CCN1CCc2sc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
10198532 205952 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 232 4 3 4 0.5 CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL95523 205952 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 232 4 3 4 0.5 CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
11581337 186080 0 None - 3 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL488248 186080 0 None - 3 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL557214 186080 0 None - 3 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
2351 3222 60 None -138 21 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3222 60 None -138 21 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3222 60 None -138 21 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3222 60 None -138 21 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3222 60 None -138 21 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
1016 3678 75 None -1737 35 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3678 75 None -1737 35 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3678 75 None -1737 35 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3678 75 None -1737 35 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3678 75 None -1737 35 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3678 75 None -1737 35 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
44329797 107607 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 261 5 2 5 1.7 CC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL319553 107607 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 261 5 2 5 1.7 CC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
135 2486 38 None -46 58 Rat 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2486 38 None -46 58 Rat 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2486 38 None -46 58 Rat 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2486 38 None -46 58 Rat 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2486 38 None -46 58 Rat 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
85469870 136114 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 439 6 0 4 4.2 Cc1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
CHEMBL3740042 136114 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 439 6 0 4 4.2 Cc1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
85469934 136199 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 443 6 0 4 4.0 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(F)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3740847 136199 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 443 6 0 4 4.0 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(F)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
10834872 15374 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 400 6 1 3 3.9 CN(CCN1CCNC1=O)Cc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
CHEMBL122018 15374 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 400 6 1 3 3.9 CN(CCN1CCNC1=O)Cc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
1588 2284 24 None -38 44 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2284 24 None -38 44 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2284 24 None -38 44 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2284 24 None -38 44 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2284 24 None -38 44 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
10047772 36426 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 420 5 1 3 4.4 Cc1cccc2c(-c3ccc(F)cc3)cn(C3CCN(CCN4CCNC4=O)CC3)c12 10.1021/jm00104a007
CHEMBL144901 36426 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 420 5 1 3 4.4 Cc1cccc2c(-c3ccc(F)cc3)cn(C3CCN(CCN4CCNC4=O)CC3)c12 10.1021/jm00104a007
44573821 192121 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 503 6 0 2 6.8 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL522037 192121 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 503 6 0 2 6.8 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
3082597 99085 8 None - 1 Bovine 5.6 pIC50 = 5.6 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283606 99085 8 None - 1 Bovine 5.6 pIC50 = 5.6 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
11753909 18764 0 None - 0 Bovine 5.6 pIC50 = 5.6 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 458 5 2 8 2.5 CS(=O)(=O)Nc1ccc2c(c1)C(O)CC1(CCN(CCc3ccc4nonc4c3)CC1)O2 10.1021/jm00099a028
CHEMBL1203301 18764 0 None - 0 Bovine 5.6 pIC50 = 5.6 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 458 5 2 8 2.5 CS(=O)(=O)Nc1ccc2c(c1)C(O)CC1(CCN(CCc3ccc4nonc4c3)CC1)O2 10.1021/jm00099a028
CHEMBL128745 18764 0 None - 0 Bovine 5.6 pIC50 = 5.6 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 458 5 2 8 2.5 CS(=O)(=O)Nc1ccc2c(c1)C(O)CC1(CCN(CCc3ccc4nonc4c3)CC1)O2 10.1021/jm00099a028
9845791 118713 4 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 434 5 1 3 4.7 Cc1ccc2c(c1)c(-c1ccc(F)cc1)c(C)n2C1CCN(CCN2CCNC2=O)CC1 10.1021/jm00104a007
CHEMBL343444 118713 4 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 434 5 1 3 4.7 Cc1ccc2c(c1)c(-c1ccc(F)cc1)c(C)n2C1CCN(CCN2CCNC2=O)CC1 10.1021/jm00104a007
44376954 55436 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 387 3 0 5 4.0 Cc1cc(C)n2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc2c1 10.1016/s0960-894x(99)00591-0
CHEMBL162232 55436 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 387 3 0 5 4.0 Cc1cc(C)n2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc2c1 10.1016/s0960-894x(99)00591-0
2247 502 77 None -5 42 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -5 42 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -5 42 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -5 42 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -5 42 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
1212 1624 45 None -19 66 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1624 45 None -19 66 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1624 45 None -19 66 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1624 45 None -19 66 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1624 45 None -19 66 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3584 3706 60 None -2 14 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
5401 3706 60 None -2 14 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
7302 3706 60 None -2 14 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
CHEMBL611 3706 60 None -2 14 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
DB01162 3706 60 None -2 14 Rat 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
9931837 118655 4 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 418 5 1 3 4.3 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1=CCN(CCN2CCNC2=O)CC1 10.1021/jm00104a007
CHEMBL343034 118655 4 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 418 5 1 3 4.3 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1=CCN(CCN2CCNC2=O)CC1 10.1021/jm00104a007
44563063 185433 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 439 7 0 5 5.3 O=c1c2ccccc2nc(-c2ccc(OCCCN3CCCCC3)cc2)n1-c1ccccc1 10.1016/j.bmcl.2008.10.034
CHEMBL487060 185433 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 439 7 0 5 5.3 O=c1c2ccccc2nc(-c2ccc(OCCCN3CCCCC3)cc2)n1-c1ccccc1 10.1016/j.bmcl.2008.10.034
277 1269 55 None -117 46 Rat 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1269 55 None -117 46 Rat 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1269 55 None -117 46 Rat 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1269 55 None -117 46 Rat 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1269 55 None -117 46 Rat 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
44376900 55960 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 375 3 1 6 3.1 Cc1nc2c(O)cccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL162826 55960 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 375 3 1 6 3.1 Cc1nc2c(O)cccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
11292933 56085 39 None - 9 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat adrenergic alpha1A receptorInhibition of rat adrenergic alpha1A receptor
ChEMBL 415 5 1 4 3.4 Cc1ccc2c(N3CCN(CCc4cccc(N5CCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631540 56085 39 None - 9 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat adrenergic alpha1A receptorInhibition of rat adrenergic alpha1A receptor
ChEMBL 415 5 1 4 3.4 Cc1ccc2c(N3CCN(CCc4cccc(N5CCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
22493258 98198 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cellsInhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
CHEMBL277375 98198 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cellsInhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
73603034 125418 21 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at alpha 1a adrenergic receptor (unknown origin)Antagonist activity at alpha 1a adrenergic receptor (unknown origin)
ChEMBL 465 4 3 8 2.9 Cn1ncc(NC(=O)c2nc(-c3c(F)cccc3F)sc2N)c1N1CC[C@@H](N)[C@H](F)CC1 10.1021/acs.jmedchem.8b01857
CHEMBL3648680 125418 21 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at alpha 1a adrenergic receptor (unknown origin)Antagonist activity at alpha 1a adrenergic receptor (unknown origin)
ChEMBL 465 4 3 8 2.9 Cn1ncc(NC(=O)c2nc(-c3c(F)cccc3F)sc2N)c1N1CC[C@@H](N)[C@H](F)CC1 10.1021/acs.jmedchem.8b01857
44376993 56175 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 427 3 0 5 4.7 Cc1nc2c(Cl)cc(Cl)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL163247 56175 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 427 3 0 5 4.7 Cc1nc2c(Cl)cc(Cl)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
14739954 108610 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 325 4 1 2 3.8 CN(C)CC(c1ccccc1Br)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL321364 108610 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 325 4 1 2 3.8 CN(C)CC(c1ccccc1Br)C1(O)CCCCC1 10.1021/jm00172a035
3191 102372 93 None -204 25 Rat 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102372 93 None -204 25 Rat 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
2812 4696 96 None -2238 34 Rat 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4696 96 None -2238 34 Rat 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
10341964 32836 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 418 5 1 3 4.3 Cc1cccc2c(-c3ccc(F)cc3)cn(C3=CCN(CCN4CCNC4=O)CC3)c12 10.1021/jm00104a007
CHEMBL141667 32836 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 418 5 1 3 4.3 Cc1cccc2c(-c3ccc(F)cc3)cn(C3=CCN(CCN4CCNC4=O)CC3)c12 10.1021/jm00104a007
44269124 28590 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
CHEMBL13789 28590 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
10427137 35806 4 None -512 3 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 336 2 0 2 5.3 Cc1ccc2c(c1)c(-c1ccc(F)cc1)c(C)n2C1CCN(C)CC1 10.1021/jm00104a007
CHEMBL144362 35806 4 None -512 3 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 336 2 0 2 5.3 Cc1ccc2c(c1)c(-c1ccc(F)cc1)c(C)n2C1CCN(C)CC1 10.1021/jm00104a007
1935 3664 92 None -190 6 Rat 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 nan
2551 3664 92 None -190 6 Rat 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 nan
6687 3664 92 None -190 6 Rat 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 nan
CHEMBL95 3664 92 None -190 6 Rat 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 nan
DB00382 3664 92 None -190 6 Rat 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 nan
45485062 195482 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL567993 195482 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
9956013 37389 4 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 462 6 0 3 5.5 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1CCN(CCN2CCN(C(C)C)C2=O)CC1 10.1021/jm00104a007
CHEMBL145712 37389 4 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 462 6 0 3 5.5 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1CCN(CCN2CCN(C(C)C)C2=O)CC1 10.1021/jm00104a007
44377007 56838 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 393 3 0 5 4.0 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3c(Cl)cccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL164612 56838 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 393 3 0 5 4.0 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3c(Cl)cccc3c2C1 10.1016/s0960-894x(99)00591-0
9795167 106995 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL318544 106995 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
10399043 119644 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 232 5 2 5 1.1 CO/N=C/c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL351542 119644 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 232 5 2 5 1.1 CO/N=C/c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
3151 1429 93 None -147 27 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 1429 93 None -147 27 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 1429 93 None -147 27 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 1429 93 None -147 27 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 1429 93 None -147 27 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
22120322 55616 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1ccc2nc(C)c(CCN3CCc4oc5ccccc5c4C3)c(=O)n2c1 10.1016/s0960-894x(99)00591-0
CHEMBL162370 55616 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1ccc2nc(C)c(CCN3CCc4oc5ccccc5c4C3)c(=O)n2c1 10.1016/s0960-894x(99)00591-0
12575 1949 28 None - 17 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/s0960-894x(99)00591-0
54459 1949 28 None - 17 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/s0960-894x(99)00591-0
CHEMBL10316 1949 28 None - 17 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/s0960-894x(99)00591-0
11516386 185439 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 377 6 0 5 3.9 Cn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL487064 185439 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 377 6 0 5 3.9 Cn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
2435 3520 78 None - 49 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm960159f
60149 3520 78 None - 49 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm960159f
98 3520 78 None - 49 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm960159f
CHEMBL12713 3520 78 None - 49 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm960159f
DB06144 3520 78 None - 49 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm960159f
2435 3520 78 None - 49 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm00104a007
60149 3520 78 None - 49 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm00104a007
98 3520 78 None - 49 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm00104a007
CHEMBL12713 3520 78 None - 49 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm00104a007
DB06144 3520 78 None - 49 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm00104a007
56961460 120911 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 477 4 2 10 2.0 COc1cc2nc(N3CCN(C(=O)c4cc5ccc(O)cc5oc4=O)CC3)nc(N)c2cc1OC 10.1021/ml5004298
CHEMBL3582268 120911 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 477 4 2 10 2.0 COc1cc2nc(N3CCN(C(=O)c4cc5ccc(O)cc5oc4=O)CC3)nc(N)c2cc1OC 10.1021/ml5004298
10809238 199446 0 None - 0 Bovine 7.5 pIC50 = 7.5 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 371 4 0 5 3.1 Cn1c(=O)sc2cc(CCN3CCN(c4ccc(F)cc4)CC3)ccc21 10.1021/jm970298c
CHEMBL60318 199446 0 None - 0 Bovine 7.5 pIC50 = 7.5 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 371 4 0 5 3.1 Cn1c(=O)sc2cc(CCN3CCN(c4ccc(F)cc4)CC3)ccc21 10.1021/jm970298c
10501785 201031 0 None - 0 Bovine 7.5 pIC50 = 7.5 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 411 7 0 6 3.8 COc1ccccc1N1CCN(CCCCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
CHEMBL61819 201031 0 None - 0 Bovine 7.5 pIC50 = 7.5 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 411 7 0 6 3.8 COc1ccccc1N1CCN(CCCCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
10718277 201562 0 None - 0 Bovine 7.5 pIC50 = 7.5 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 447 6 0 4 4.2 CN1C(=O)COc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
CHEMBL64610 201562 0 None - 0 Bovine 7.5 pIC50 = 7.5 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 447 6 0 4 4.2 CN1C(=O)COc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
85469932 136250 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 455 7 0 5 3.9 COc1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
CHEMBL3741318 136250 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 455 7 0 5 3.9 COc1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
1305 508 10 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9934033 508 10 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL182150 508 10 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
138753277 176711 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of adrenergic receptor alpha1a (unknown origin)Inhibition of adrenergic receptor alpha1a (unknown origin)
ChEMBL 303 1 2 3 3.3 Cc1cc(Br)c(NC2=NCCN2)c2ccccc12 10.1021/acs.jmedchem.9b01870
CHEMBL4636550 176711 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of adrenergic receptor alpha1a (unknown origin)Inhibition of adrenergic receptor alpha1a (unknown origin)
ChEMBL 303 1 2 3 3.3 Cc1cc(Br)c(NC2=NCCN2)c2ccccc12 10.1021/acs.jmedchem.9b01870
13520336 4270 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 291 5 1 3 3.4 COc1ccc(C(CN(C)C)C2(O)CCCCCC2)cc1 10.1021/jm00172a035
CHEMBL101056 4270 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 291 5 1 3 3.4 COc1ccc(C(CN(C)C)C2(O)CCCCCC2)cc1 10.1021/jm00172a035
3501942 9359 48 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 263 5 2 3 2.7 CNCC(c1ccc(OC)cc1)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL1119 9359 48 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 263 5 2 3 2.7 CNCC(c1ccc(OC)cc1)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL1628258 9359 48 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 263 5 2 3 2.7 CNCC(c1ccc(OC)cc1)C1(O)CCCCC1 10.1021/jm00172a035
13520306 206484 10 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 247 4 1 2 3.0 CN(C)CC(c1ccccc1)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL98660 206484 10 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 247 4 1 2 3.0 CN(C)CC(c1ccccc1)C1(O)CCCCC1 10.1021/jm00172a035
10251234 11126 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 11126 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 11126 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10476735 13604 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1195096 13604 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL553833 13604 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9981024 95638 0 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26018 95638 0 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL300735 95638 0 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9980269 98613 0 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280586 98613 0 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL54266 98613 0 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10342423 98997 0 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL28312 98997 0 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL48925 98997 0 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10366072 116384 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 442 5 1 7 3.0 CS(=O)(=O)Nc1ccc2c(c1)CCC1(CCN(CCc3ccc4nonc4c3)CC1)O2 10.1021/jm00099a028
CHEMBL1203300 116384 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 442 5 1 7 3.0 CS(=O)(=O)Nc1ccc2c(c1)CCC1(CCN(CCc3ccc4nonc4c3)CC1)O2 10.1021/jm00099a028
CHEMBL338361 116384 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 442 5 1 7 3.0 CS(=O)(=O)Nc1ccc2c(c1)CCC1(CCN(CCc3ccc4nonc4c3)CC1)O2 10.1021/jm00099a028
23027245 195442 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL567791 195442 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
1220 186 46 None - 45 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00038a007
31 186 46 None - 45 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00038a007
7 186 46 None - 45 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00038a007
CHEMBL56 186 46 None - 45 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00038a007
44343257 10385 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 250 4 1 2 3.7 c1ccc(-c2ccccc2OCc2c[nH]cn2)cc1 10.1016/s0960-894x(02)00753-9
CHEMBL116700 10385 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 250 4 1 2 3.7 c1ccc(-c2ccccc2OCc2c[nH]cn2)cc1 10.1016/s0960-894x(02)00753-9
4543 169972 36 None -24 30 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169972 36 None -24 30 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169972 36 None -24 30 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
10497675 15906 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 344 6 0 2 5.3 CN(C)CCCCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
CHEMBL122384 15906 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 344 6 0 2 5.3 CN(C)CCCCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
1816 2494 99 None - 17 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1016/s0960-894x(99)00591-0
4205 2494 99 None - 17 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1016/s0960-894x(99)00591-0
7241 2494 99 None - 17 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1016/s0960-894x(99)00591-0
CHEMBL654 2494 99 None - 17 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1016/s0960-894x(99)00591-0
DB00370 2494 99 None - 17 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1016/s0960-894x(99)00591-0
10499570 16736 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 372 5 0 3 5.3 Fc1ccc(-n2cc(OCCN3CCCCC3)c3cc(Cl)ccc32)cc1 10.1021/jm960159f
CHEMBL125291 16736 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 372 5 0 3 5.3 Fc1ccc(-n2cc(OCCN3CCCCC3)c3cc(Cl)ccc32)cc1 10.1021/jm960159f
2274 3112 53 None -6 32 Rat 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3112 53 None -6 32 Rat 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3112 53 None -6 32 Rat 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3112 53 None -6 32 Rat 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3112 53 None -6 32 Rat 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
44362195 120563 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 241 4 2 3 2.1 c1c[nH]c(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL357129 120563 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 241 4 2 3 2.1 c1c[nH]c(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
85469812 136150 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 469 8 0 5 4.2 CCOc1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
CHEMBL3740351 136150 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 469 8 0 5 4.2 CCOc1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
15987265 195202 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL566075 195202 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
196129 67441 12 None -1698 15 Rat 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67441 12 None -1698 15 Rat 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
10409893 118598 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 420 5 1 3 4.4 Cc1cccc2c1c(-c1ccc(F)cc1)cn2C1CCN(CCN2CCNC2=O)CC1 10.1021/jm00104a007
CHEMBL342730 118598 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 420 5 1 3 4.4 Cc1cccc2c1c(-c1ccc(F)cc1)cn2C1CCN(CCN2CCNC2=O)CC1 10.1021/jm00104a007
85469930 136338 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 473 6 0 4 4.8 Cc1ccc(Cl)cc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
CHEMBL3742103 136338 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 473 6 0 4 4.8 Cc1ccc(Cl)cc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
10060965 34993 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 256 4 1 4 2.6 Cc1ccoc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL143562 34993 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 256 4 1 4 2.6 Cc1ccoc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
506 2212 32 None -97 6 Rat 6.5 pIC50 = 6.5 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype.Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype.
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
6603904 2212 32 None -97 6 Rat 6.5 pIC50 = 6.5 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype.Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype.
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
CHEMBL19476 2212 32 None -97 6 Rat 6.5 pIC50 = 6.5 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype.Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype.
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
44574357 178120 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468298 178120 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2009.04.016
85469753 136225 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 503 6 0 4 4.6 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(Br)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3741079 136225 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 503 6 0 4 4.6 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(Br)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
3045401 55752 28 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 359 3 0 5 3.4 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL162501 55752 28 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 359 3 0 5 3.4 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
2477 732 54 None -218 29 Rat 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
36 732 54 None -218 29 Rat 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
437 732 54 None -218 29 Rat 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
CHEMBL49 732 54 None -218 29 Rat 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
DB00490 732 54 None -218 29 Rat 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
127049862 139714 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 425 8 1 5 4.4 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805559 139714 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 425 8 1 5 4.4 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
22493280 47996 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ccno2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL155327 47996 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ccno2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44573820 192655 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 489 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL523882 192655 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 489 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
3082597 99085 8 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283606 99085 8 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
191 399 92 None -107 29 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 399 92 None -107 29 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 399 92 None -107 29 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 399 92 None -107 29 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 399 92 None -107 29 Rat 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
3823 49936 38 None -3019 11 Rat 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
76973198 49936 38 None -3019 11 Rat 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL157101 49936 38 None -3019 11 Rat 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
127041710 136080 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 450 6 0 4 4.4 [C-]#[N+]c1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
CHEMBL3739762 136080 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 450 6 0 4 4.4 [C-]#[N+]c1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
10403428 206646 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 315 4 1 2 4.0 CN(C)CC(c1cccc(C(F)(F)F)c1)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL99653 206646 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 315 4 1 2 4.0 CN(C)CC(c1cccc(C(F)(F)F)c1)C1(O)CCCCC1 10.1021/jm00172a035
45484995 196832 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577904 196832 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
44573931 186859 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 479 7 0 4 5.6 CN(CCCC1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL493962 186859 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 479 7 0 4 5.6 CN(CCCC1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
146431 206525 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 315 4 1 2 4.3 CN(C)CC(c1ccc(Cl)c(Cl)c1)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL98894 206525 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 315 4 1 2 4.3 CN(C)CC(c1ccc(Cl)c(Cl)c1)C1(O)CCCCC1 10.1021/jm00172a035
2803 939 53 None -3 19 Rat 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
516 939 53 None -3 19 Rat 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
704 939 53 None -3 19 Rat 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
CHEMBL134 939 53 None -3 19 Rat 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
DB00575 939 53 None -3 19 Rat 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
135398737 942 89 None -5 92 Rat 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 942 89 None -5 92 Rat 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 942 89 None -5 92 Rat 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 942 89 None -5 92 Rat 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 942 89 None -5 92 Rat 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
124 2921 44 None -13 33 Rat 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2921 44 None -13 33 Rat 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2921 44 None -13 33 Rat 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2921 44 None -13 33 Rat 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2921 44 None -13 33 Rat 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
85469873 136056 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 493 6 0 4 4.9 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccc3C(F)(F)F)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3739542 136056 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 493 6 0 4 4.9 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccc3C(F)(F)F)CC2)cc1 10.1016/j.bmc.2015.11.020
3952 1849 33 None -26 12 Rat 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5353646 1849 33 None -26 12 Rat 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5443 1849 33 None -26 12 Rat 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5702063 1849 33 None -26 12 Rat 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL1331786 1849 33 None -26 12 Rat 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL420 1849 33 None -26 12 Rat 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
10108561 112432 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against Alpha-1A adrenergic receptorBinding affinity against Alpha-1A adrenergic receptor
ChEMBL 295 2 0 4 2.8 CN(C)CC1CC2c3ccccc3Cc3ccncc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL331077 112432 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against Alpha-1A adrenergic receptorBinding affinity against Alpha-1A adrenergic receptor
ChEMBL 295 2 0 4 2.8 CN(C)CC1CC2c3ccccc3Cc3ccncc3N2O1 10.1016/s0960-894x(02)00796-5
44376923 56118 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1nc2cccc(C)n2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL163190 56118 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1nc2cccc(C)n2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
137399257 161888 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
ChEMBL 513 8 1 8 3.7 COc1cc2nc(N3CCN(C(=O)Cc4ccc(OCc5ccccc5)cc4)CC3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.10.026
CHEMBL4166644 161888 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
ChEMBL 513 8 1 8 3.7 COc1cc2nc(N3CCN(C(=O)Cc4ccc(OCc5ccccc5)cc4)CC3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.10.026
10734233 113232 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 316 4 0 2 4.5 CN(C)CCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
CHEMBL332365 113232 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 316 4 0 2 4.5 CN(C)CCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
10717072 162680 0 None - 0 Bovine 6.4 pIC50 = 6.4 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 421 4 0 5 4.0 Cn1c(=O)sc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
CHEMBL418499 162680 0 None - 0 Bovine 6.4 pIC50 = 6.4 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 421 4 0 5 4.0 Cn1c(=O)sc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
10527817 112556 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 456 8 0 3 5.0 CC(C)N1CCN(CCN(C)CCc2cn(-c3ccc(F)cc3)c3cc(Cl)ccc23)C1=O 10.1021/jm960159f
CHEMBL331193 112556 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 456 8 0 3 5.0 CC(C)N1CCN(CCN(C)CCc2cn(-c3ccc(F)cc3)c3cc(Cl)ccc23)C1=O 10.1021/jm960159f
10070029 164854 0 None - 1 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL423841 164854 0 None - 1 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL54089 164854 0 None - 1 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
121852 10056 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 10056 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 10056 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10014217 99274 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 233 2 0 3 2.1 COc1cccc2c1CC(N1CCCC1)CO2 10.1021/jm00038a007
CHEMBL285010 99274 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 233 2 0 3 2.1 COc1cccc2c1CC(N1CCCC1)CO2 10.1021/jm00038a007
135 2486 38 None -40 58 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
1796 2486 38 None -40 58 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
4184 2486 38 None -40 58 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
CHEMBL6437 2486 38 None -40 58 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
DB06148 2486 38 None -40 58 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
10550615 114075 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 430 8 1 4 3.8 CN(CCOc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12)CCN1CCNC1=O 10.1021/jm960159f
CHEMBL333774 114075 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 430 8 1 4 3.8 CN(CCOc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12)CCN1CCNC1=O 10.1021/jm960159f
44318842 204378 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 308 2 0 3 3.7 Cc1ccc2c(c1)N1OC(CN(C)C)CC1c1ccccc1C2 10.1016/s0960-894x(01)00721-1
CHEMBL85735 204378 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 308 2 0 3 3.7 Cc1ccc2c(c1)N1OC(CN(C)C)CC1c1ccccc1C2 10.1016/s0960-894x(01)00721-1
11517341 173157 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 419 5 0 6 4.0 COc1cccc2nc(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)n(C)c(=O)c12 10.1016/j.bmcl.2008.10.034
CHEMBL453653 173157 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 419 5 0 6 4.0 COc1cccc2nc(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)n(C)c(=O)c12 10.1016/j.bmcl.2008.10.034
10812487 15380 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 428 8 1 3 4.3 CN(CCCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
CHEMBL122042 15380 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 428 8 1 3 4.3 CN(CCCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
10361439 109132 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of alpha 1A adrenergic receptor (unknown origin)Inhibition of alpha 1A adrenergic receptor (unknown origin)
ChEMBL 364 6 0 3 4.7 COc1cccc2c1CCCC2CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL322275 109132 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of alpha 1A adrenergic receptor (unknown origin)Inhibition of alpha 1A adrenergic receptor (unknown origin)
ChEMBL 364 6 0 3 4.7 COc1cccc2c1CCCC2CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5206987 109132 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of alpha 1A adrenergic receptor (unknown origin)Inhibition of alpha 1A adrenergic receptor (unknown origin)
ChEMBL 364 6 0 3 4.7 COc1cccc2c1CCCC2CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00633
13520334 112040 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 297 4 1 2 3.0 CN(C)CC(c1ccc(Br)cc1)C1(O)CCC1 10.1021/jm00172a035
CHEMBL329923 112040 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 297 4 1 2 3.0 CN(C)CC(c1ccc(Br)cc1)C1(O)CCC1 10.1021/jm00172a035
44318454 204280 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL84931 204280 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
10789000 201618 0 None - 0 Bovine 7.4 pIC50 = 7.4 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 435 6 1 5 5.2 Oc1nc2ccc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)cc2s1 10.1021/jm970298c
CHEMBL64845 201618 0 None - 0 Bovine 7.4 pIC50 = 7.4 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 435 6 1 5 5.2 Oc1nc2ccc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)cc2s1 10.1021/jm970298c
134142282 145145 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3916182 145145 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
22493352 47995 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ncco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL155326 47995 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ncco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
11502381 173562 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 407 4 0 5 4.1 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(F)cccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL454642 173562 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 407 4 0 5 4.1 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(F)cccc2c1=O 10.1016/j.bmcl.2008.10.034
9794803 10888 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL117381 10888 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
85469754 136359 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 503 7 0 6 3.3 CS(=O)(=O)c1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
CHEMBL3742276 136359 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 503 7 0 6 3.3 CS(=O)(=O)c1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1 10.1016/j.bmc.2015.11.020
10378649 108093 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 274 7 3 4 1.6 CCCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL320419 108093 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 274 7 3 4 1.6 CCCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
5074 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm960159f
97 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm960159f
CHEMBL267777 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm960159f
DB12693 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm960159f
5074 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Compound was tested for i the displacement of [3H]prazosin from alpha-1 adrenergic receptorCompound was tested for i the displacement of [3H]prazosin from alpha-1 adrenergic receptor
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00104a007
97 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Compound was tested for i the displacement of [3H]prazosin from alpha-1 adrenergic receptorCompound was tested for i the displacement of [3H]prazosin from alpha-1 adrenergic receptor
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00104a007
CHEMBL267777 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Compound was tested for i the displacement of [3H]prazosin from alpha-1 adrenergic receptorCompound was tested for i the displacement of [3H]prazosin from alpha-1 adrenergic receptor
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00104a007
DB12693 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Compound was tested for i the displacement of [3H]prazosin from alpha-1 adrenergic receptorCompound was tested for i the displacement of [3H]prazosin from alpha-1 adrenergic receptor
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00104a007
5074 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Compound was tested for the displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat striatal membranesCompound was tested for the displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat striatal membranes
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00104a006
97 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Compound was tested for the displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat striatal membranesCompound was tested for the displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat striatal membranes
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00104a006
CHEMBL267777 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Compound was tested for the displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat striatal membranesCompound was tested for the displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat striatal membranes
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00104a006
DB12693 3268 75 None - 30 Rat 7.3 pIC50 = 7.3 Binding
Compound was tested for the displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat striatal membranesCompound was tested for the displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat striatal membranes
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00104a006
44573822 186872 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 505 6 0 3 6.4 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CC2)OCc2ccccc23)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL494009 186872 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 505 6 0 3 6.4 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CC2)OCc2ccccc23)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
44376984 55915 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 485 3 0 5 4.0 Cc1nc2ccc(I)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL162682 55915 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 485 3 0 5 4.0 Cc1nc2ccc(I)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
85469869 136055 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 426 6 0 5 3.2 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3739533 136055 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 426 6 0 5 3.2 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2015.11.020
44574359 178148 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2cccc(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468509 178148 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2cccc(F)c2)cc1 10.1016/j.bmcl.2009.04.016
10531 1387 18 None -5 24 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1387 18 None -5 24 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1387 18 None -5 24 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1387 18 None -5 24 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1387 18 None -5 24 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
100 3733 52 None 1 56 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3733 52 None 1 56 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3733 52 None 1 56 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3733 52 None 1 56 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3733 52 None 1 56 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
6761 67442 17 None 1 18 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67442 17 None 1 18 Rat 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
9802796 163767 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 430 8 1 4 3.8 CN(CCOc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
CHEMBL421244 163767 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 430 8 1 4 3.8 CN(CCOc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
44362185 120503 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 253 4 1 4 2.1 c1cncc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL356605 120503 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
ChEMBL 253 4 1 4 2.1 c1cncc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
10364538 4305 0 None - 1 Bovine 6.3 pIC50 = 6.3 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 415 5 1 6 2.5 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccccn3)CC1)O2 10.1021/jm00099a028
CHEMBL101322 4305 0 None - 1 Bovine 6.3 pIC50 = 6.3 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 415 5 1 6 2.5 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccccn3)CC1)O2 10.1021/jm00099a028
CHEMBL1204312 4305 0 None - 1 Bovine 6.3 pIC50 = 6.3 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
ChEMBL 415 5 1 6 2.5 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccccn3)CC1)O2 10.1021/jm00099a028
10245637 32900 2 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 323 2 0 3 3.6 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2N1CCN(C)CC1 10.1021/jm00104a007
CHEMBL141721 32900 2 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 323 2 0 3 3.6 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2N1CCN(C)CC1 10.1021/jm00104a007
9885114 119086 3 None -47 12 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
CHEMBL346389 119086 3 None -47 12 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
59271992 117532 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of alpha-adrenoceptor 1A (unknown origin)Inhibition of alpha-adrenoceptor 1A (unknown origin)
ChEMBL 513 13 2 7 3.5 COCCCOc1cc(C(=O)N(C[C@@H]2CNC[C@H]2OC(=O)NCc2ccccc2)C(C)C)ccc1OC 10.1016/j.bmcl.2015.02.040
CHEMBL3403995 117532 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of alpha-adrenoceptor 1A (unknown origin)Inhibition of alpha-adrenoceptor 1A (unknown origin)
ChEMBL 513 13 2 7 3.5 COCCCOc1cc(C(=O)N(C[C@@H]2CNC[C@H]2OC(=O)NCc2ccccc2)C(C)C)ccc1OC 10.1016/j.bmcl.2015.02.040
10092409 11926 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1183479 11926 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL299561 11926 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10095594 12247 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1185501 12247 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL417550 12247 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10251673 99017 0 None - 1 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283207 99017 0 None - 1 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL52396 99017 0 None - 1 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10338595 161937 0 None - 1 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL416747 161937 0 None - 1 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
13520313 107252 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 325 4 1 2 3.8 CN(C)CC(c1cccc(Br)c1)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL319142 107252 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 325 4 1 2 3.8 CN(C)CC(c1cccc(Br)c1)C1(O)CCCCC1 10.1021/jm00172a035
122179431 120916 0 None -1 3 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 585 9 1 13 3.1 CCN(CC)c1ccc2cc(-n3cc(CN4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)nn3)c(=O)oc2c1 10.1021/ml5004298
CHEMBL3582272 120916 0 None -1 3 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 585 9 1 13 3.1 CCN(CC)c1ccc2cc(-n3cc(CN4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)nn3)c(=O)oc2c1 10.1021/ml5004298
132499 106747 8 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 281 4 1 2 3.7 CN(C)CC(c1ccccc1Cl)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL316862 106747 8 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 281 4 1 2 3.7 CN(C)CC(c1ccccc1Cl)C1(O)CCCCC1 10.1021/jm00172a035
44376845 55242 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 419 5 0 7 3.4 COc1cc2nc(C)c(CCN3CCc4oc5ccccc5c4C3)c(=O)n2cc1OC 10.1016/s0960-894x(99)00591-0
CHEMBL162058 55242 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 419 5 0 7 3.4 COc1cc2nc(C)c(CCN3CCc4oc5ccccc5c4C3)c(=O)n2cc1OC 10.1016/s0960-894x(99)00591-0
26987 934 29 None -75 21 Rat 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 934 29 None -75 21 Rat 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 934 29 None -75 21 Rat 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 934 29 None -75 21 Rat 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 934 29 None -75 21 Rat 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
9904205 204125 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against Alpha-1A adrenergic receptorBinding affinity against Alpha-1A adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL83658 204125 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against Alpha-1A adrenergic receptorBinding affinity against Alpha-1A adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
9904205 204125 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL83658 204125 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
10432755 113284 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 428 8 1 3 4.3 CN(CCCN1CCNC1=O)CCc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12 10.1021/jm960159f
CHEMBL332425 113284 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 428 8 1 3 4.3 CN(CCCN1CCNC1=O)CCc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12 10.1021/jm960159f
10047887 120523 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 422 5 1 3 4.7 CNC(=O)N(C)CCN1CCC(n2cc(-c3ccc(F)cc3)c3cc(C)ccc32)CC1 10.1021/jm00104a007
CHEMBL356799 120523 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 422 5 1 3 4.7 CNC(=O)N(C)CCN1CCC(n2cc(-c3ccc(F)cc3)c3cc(C)ccc32)CC1 10.1021/jm00104a007
4452 2711 18 None - 19 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm960159f
983 2711 18 None - 19 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm960159f
CHEMBL20734 2711 18 None - 19 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm960159f
44574358 178121 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 467 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(C)cc2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468299 178121 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 467 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(C)cc2)cc1 10.1016/j.bmcl.2009.04.016
85469872 136269 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 459 6 0 4 4.5 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3741483 136269 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 459 6 0 4 4.5 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
4418 33985 80 None -1 7 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmc.2015.11.020
CHEMBL142635 33985 80 None -1 7 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmc.2015.11.020
44596863 197239 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 367 6 1 6 2.3 C=Cc1c(C)nn(CCCN2CCN(c3ccc(C)cc3)CC2)c(=O)c1N 10.1021/jm900458r
CHEMBL584606 197239 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 367 6 1 6 2.3 C=Cc1c(C)nn(CCCN2CCN(c3ccc(C)cc3)CC2)c(=O)c1N 10.1021/jm900458r
4011 81982 43 None -125 24 Rat 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81982 43 None -125 24 Rat 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
1531 2226 64 None -3 15 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
3869 2226 64 None -3 15 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
7207 2226 64 None -3 15 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
CHEMBL429 2226 64 None -3 15 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
DB00598 2226 64 None -3 15 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
44376927 55333 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 461 3 0 5 5.0 Cc1nc2c(Cl)cc(C(F)(F)F)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL162147 55333 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 461 3 0 5 5.0 Cc1nc2c(Cl)cc(C(F)(F)F)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
506 2212 32 None -81 6 Human 6.2 pIC50 = 6.2 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtypeCompound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
6603904 2212 32 None -81 6 Human 6.2 pIC50 = 6.2 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtypeCompound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
CHEMBL19476 2212 32 None -81 6 Human 6.2 pIC50 = 6.2 Binding
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtypeCompound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
11502638 173161 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 419 5 0 6 4.0 COc1ccc2nc(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2008.10.034
CHEMBL453654 173161 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 419 5 0 6 4.0 COc1ccc2nc(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2008.10.034
10644514 100575 0 None - 0 Bovine 8.2 pIC50 = 8.2 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 397 6 0 6 3.4 COc1ccccc1N1CCN(CCCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
CHEMBL294730 100575 0 None - 0 Bovine 8.2 pIC50 = 8.2 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 397 6 0 6 3.4 COc1ccccc1N1CCN(CCCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
10409070 121397 4 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 406 5 1 3 4.1 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3ccccc32)CC1 10.1021/jm00104a007
CHEMBL359031 121397 4 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 406 5 1 3 4.1 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3ccccc32)CC1 10.1021/jm00104a007
31101 719 39 None -4 36 Rat 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 719 39 None -4 36 Rat 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 719 39 None -4 36 Rat 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 719 39 None -4 36 Rat 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 719 39 None -4 36 Rat 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
125017 9345 94 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 263 4 2 3 2.7 CN(C)CC(c1ccc(O)cc1)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL1118 9345 94 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 263 4 2 3 2.7 CN(C)CC(c1ccc(O)cc1)C1(O)CCCCC1 10.1021/jm00172a035
10528455 15381 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 472 9 0 4 4.9 CC(C)N1CCN(CCN(C)CCOc2cn(-c3ccc(F)cc3)c3cc(Cl)ccc23)C1=O 10.1021/jm960159f
CHEMBL122047 15381 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 472 9 0 4 4.9 CC(C)N1CCN(CCN(C)CCOc2cn(-c3ccc(F)cc3)c3cc(Cl)ccc23)C1=O 10.1021/jm960159f
10413283 186875 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 490 7 0 3 5.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
CHEMBL494016 186875 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 490 7 0 3 5.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
121852 10056 7 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 10056 7 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 10056 7 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10024943 96927 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26975 96927 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL52485 96927 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
2291 3123 52 None -446 12 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3123 52 None -446 12 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3123 52 None -446 12 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3123 52 None -446 12 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3123 52 None -446 12 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
14183742 206571 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 325 4 1 2 3.8 CN(C)CC(c1ccc(Br)cc1)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL99175 206571 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 325 4 1 2 3.8 CN(C)CC(c1ccc(Br)cc1)C1(O)CCCCC1 10.1021/jm00172a035
119081417 151115 31 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]prazosin from recombinant human adrenergic A1a receptor after 60 mins by scintillation counting methodDisplacement of [3H]prazosin from recombinant human adrenergic A1a receptor after 60 mins by scintillation counting method
ChEMBL 488 10 0 7 5.2 CCCOc1ccc(CCc2nc3cc(-c4c(C)noc4C)ccc3n2CCN2CCOCC2)cc1 10.1021/acs.jmedchem.6b01839
CHEMBL3963965 151115 31 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]prazosin from recombinant human adrenergic A1a receptor after 60 mins by scintillation counting methodDisplacement of [3H]prazosin from recombinant human adrenergic A1a receptor after 60 mins by scintillation counting method
ChEMBL 488 10 0 7 5.2 CCCOc1ccc(CCc2nc3cc(-c4c(C)noc4C)ccc3n2CCN2CCOCC2)cc1 10.1021/acs.jmedchem.6b01839
11567596 174000 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 403 4 0 5 4.4 Cn1c(-c2ccc(OC3CCN(C4CCCC4)CC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL455681 174000 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 403 4 0 5 4.4 Cn1c(-c2ccc(OC3CCN(C4CCCC4)CC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
1599 2299 47 None -3019 16 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
3955 2299 47 None -3019 16 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
7215 2299 47 None -3019 16 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
CHEMBL841 2299 47 None -3019 16 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
DB00836 2299 47 None -3019 16 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
1028 287 69 None -47 30 Rat 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
139148732 287 69 None -47 30 Rat 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
479 287 69 None -47 30 Rat 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
5816 287 69 None -47 30 Rat 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL679 287 69 None -47 30 Rat 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
DB00668 287 69 None -47 30 Rat 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
11618024 186081 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 389 4 0 5 4.0 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL488249 186081 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 389 4 0 5 4.0 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
2435 713 98 None -436 12 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
395 713 98 None -436 12 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
520 713 98 None -436 12 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
5386 713 98 None -436 12 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
CHEMBL844 713 98 None -436 12 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
DB00484 713 98 None -436 12 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
135398745 2858 108 None -13 66 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2858 108 None -13 66 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2858 108 None -13 66 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2858 108 None -13 66 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
10647075 16700 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 446 8 1 4 4.5 CN(CCSc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
CHEMBL125072 16700 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 446 8 1 4 4.5 CN(CCSc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
11618702 173262 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 423 4 0 5 4.7 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(Cl)cccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL453893 173262 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 423 4 0 5 4.7 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(Cl)cccc2c1=O 10.1016/j.bmcl.2008.10.034
23151199 185436 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 377 6 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.10.034
CHEMBL487063 185436 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 377 6 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.10.034
10219 188200 30 None -467 5 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 nan
CHEMBL493439 188200 30 None -467 5 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 nan
CHEMBL50588 188200 30 None -467 5 Rat 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 nan
44269124 28590 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(02)00753-9
CHEMBL13789 28590 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(02)00753-9
85469931 136356 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 493 6 0 4 4.9 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3742253 136356 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 493 6 0 4 4.9 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
10003405 120549 4 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 440 5 1 3 4.8 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00104a007
CHEMBL357019 120549 4 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 440 5 1 3 4.8 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00104a007
1353 1872 85 None -10 86 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1872 85 None -10 86 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1872 85 None -10 86 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1872 85 None -10 86 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1872 85 None -10 86 Rat 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
44377035 119612 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1nc2c(C)cccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL351200 119612 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1nc2c(C)cccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
2585 788 100 None -5 22 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 788 100 None -5 22 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 788 100 None -5 22 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 788 100 None -5 22 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 788 100 None -5 22 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
9826570 112800 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 482 6 0 3 5.7 CC(C)N1CCN(CCN2CCC(c3cn(-c4ccc(F)cc4)c4cc(Cl)ccc34)CC2)C1=O 10.1021/jm960159f
CHEMBL331545 112800 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 482 6 0 3 5.7 CC(C)N1CCN(CCN2CCC(c3cn(-c4ccc(F)cc4)c4cc(Cl)ccc34)CC2)C1=O 10.1021/jm960159f
9826570 112800 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 482 6 0 3 5.7 CC(C)N1CCN(CCN2CCC(c3cn(-c4ccc(F)cc4)c4cc(Cl)ccc34)CC2)C1=O 10.1021/jm00104a007
CHEMBL331545 112800 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 482 6 0 3 5.7 CC(C)N1CCN(CCN2CCC(c3cn(-c4ccc(F)cc4)c4cc(Cl)ccc34)CC2)C1=O 10.1021/jm00104a007
14739952 4392 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 307 6 1 4 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1OC 10.1021/jm00172a035
CHEMBL101819 4392 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 307 6 1 4 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1OC 10.1021/jm00172a035
10251234 11126 0 None - 0 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 11126 0 None - 0 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 11126 0 None - 0 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9981024 95638 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26018 95638 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL300735 95638 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10047322 96679 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
CHEMBL26783 96679 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
CHEMBL50993 96679 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
10008463 11130 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 457 9 0 4 4.3 CCC[N+](C)(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178971 11130 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 457 9 0 4 4.3 CCC[N+](C)(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51985 11130 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 457 9 0 4 4.3 CCC[N+](C)(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10364835 36252 4 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 420 5 1 3 4.4 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1CCN(CCN2CCNC2=O)CC1 10.1021/jm00104a007
CHEMBL144767 36252 4 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 420 5 1 3 4.4 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1CCN(CCN2CCNC2=O)CC1 10.1021/jm00104a007
11641036 185431 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 453 8 0 5 5.4 O=c1c2ccccc2nc(-c2ccc(OCCCN3CCCCC3)cc2)n1Cc1ccccc1 10.1016/j.bmcl.2008.10.034
CHEMBL487059 185431 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
ChEMBL 453 8 0 5 5.4 O=c1c2ccccc2nc(-c2ccc(OCCCN3CCCCC3)cc2)n1Cc1ccccc1 10.1016/j.bmcl.2008.10.034
44377036 119638 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 393 3 0 5 4.0 Cc1nc2ccc(Cl)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL351483 119638 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 393 3 0 5 4.0 Cc1nc2ccc(Cl)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
10544460 16218 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 330 5 0 2 4.9 CN(C)CCCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
CHEMBL123094 16218 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 330 5 0 2 4.9 CN(C)CCCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
42636941 178361 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]prazosin form human recombinant alpha1A adrenergic receptorDisplacement of [3H]prazosin form human recombinant alpha1A adrenergic receptor
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL470432 178361 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]prazosin form human recombinant alpha1A adrenergic receptorDisplacement of [3H]prazosin form human recombinant alpha1A adrenergic receptor
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
23027527 195107 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL565551 195107 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
44343247 110133 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 258 6 3 3 2.2 CCCNC(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL325745 110133 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
ChEMBL 258 6 3 3 2.2 CCCNC(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
2286 3122 48 None -10 30 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3122 48 None -10 30 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3122 48 None -10 30 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3122 48 None -10 30 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3122 48 None -10 30 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
1043 1545 13 None -35 29 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1545 13 None -35 29 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1545 13 None -35 29 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1545 13 None -35 29 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1545 13 None -35 29 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
2726 904 64 None -2 73 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 904 64 None -2 73 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 904 64 None -2 73 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 904 64 None -2 73 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 904 64 None -2 73 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
56961507 120915 0 None 1 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 678 6 4 11 5.0 COc1cc2nc(N3CCN(C(=S)Nc4ccc(-c5c6ccc(=O)cc-6oc6cc(O)ccc56)c(C(=O)O)c4)CC3)nc(N)c2cc1OC 10.1021/ml5004298
CHEMBL3582271 120915 0 None 1 3 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 678 6 4 11 5.0 COc1cc2nc(N3CCN(C(=S)Nc4ccc(-c5c6ccc(=O)cc-6oc6cc(O)ccc56)c(C(=O)O)c4)CC3)nc(N)c2cc1OC 10.1021/ml5004298
10251234 11126 0 None - 0 Bovine 5.1 pIC50 = 5.1 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 11126 0 None - 0 Bovine 5.1 pIC50 = 5.1 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 11126 0 None - 0 Bovine 5.1 pIC50 = 5.1 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10252000 98082 0 None - 1 Bovine 5.1 pIC50 = 5.1 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL27650 98082 0 None - 1 Bovine 5.1 pIC50 = 5.1 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50188 98082 0 None - 1 Bovine 5.1 pIC50 = 5.1 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
3082597 99085 8 None - 1 Bovine 4.1 pIC50 = 4.1 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283606 99085 8 None - 1 Bovine 4.1 pIC50 = 4.1 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
22493392 46876 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 252 4 2 4 2.2 c1ccc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
CHEMBL154298 46876 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
ChEMBL 252 4 2 4 2.2 c1ccc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
44376936 57157 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 373 4 0 5 3.7 Cc1nc2ccccn2c(=O)c1CCCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL165776 57157 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 373 4 0 5 3.7 Cc1nc2ccccn2c(=O)c1CCCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
46182745 57014 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand binding to human adrenergic alpha1a receptorInhibition of radioligand binding to human adrenergic alpha1a receptor
ChEMBL 461 6 1 3 6.2 O=C(O)c1cc(-c2cccc(COc3ccc4c(c3)CN(C3CCCC3)C4=O)c2)ccc1Cl 10.1021/jm3005306
CHEMBL1651208 57014 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand binding to human adrenergic alpha1a receptorInhibition of radioligand binding to human adrenergic alpha1a receptor
ChEMBL 461 6 1 3 6.2 O=C(O)c1cc(-c2cccc(COc3ccc4c(c3)CN(C3CCCC3)C4=O)c2)ccc1Cl 10.1021/jm3005306
10736518 16201 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 348 5 0 3 5.1 CN(C)CCSc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
CHEMBL123027 16201 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 348 5 0 3 5.1 CN(C)CCSc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12 10.1021/jm960159f
10788207 199073 0 None - 0 Bovine 7.1 pIC50 = 7.1 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 419 4 0 4 3.4 CN1C(=O)COc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
CHEMBL60047 199073 0 None - 0 Bovine 7.1 pIC50 = 7.1 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 419 4 0 4 3.4 CN1C(=O)COc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
9816986 163576 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL421011 163576 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
2337 3193 72 None -3 63 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3193 72 None -3 63 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3193 72 None -3 63 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3193 72 None -3 63 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3193 72 None -3 63 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
10551704 116325 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 454 9 1 4 3.8 C#CCN(CCOc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
CHEMBL338022 116325 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
ChEMBL 454 9 1 4 3.8 C#CCN(CCOc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O 10.1021/jm960159f
13520319 162841 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 315 4 1 2 4.0 CN(C)CC(c1ccc(C(F)(F)F)cc1)C1(O)CCCCC1 10.1021/jm00172a035
CHEMBL419533 162841 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 315 4 1 2 4.0 CN(C)CC(c1ccc(C(F)(F)F)cc1)C1(O)CCCCC1 10.1021/jm00172a035
85469756 136051 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 455 7 0 5 3.9 COc1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3739513 136051 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 455 7 0 5 3.9 COc1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
10093723 36191 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 422 5 1 3 4.7 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1CCN(CCNC(=O)N(C)C)CC1 10.1021/jm00104a007
CHEMBL144710 36191 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
ChEMBL 422 5 1 3 4.7 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1CCN(CCNC(=O)N(C)C)CC1 10.1021/jm00104a007
85469868 136244 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 450 6 0 5 3.7 N#Cc1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3741260 136244 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 450 6 0 5 3.7 N#Cc1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)cc1 10.1016/j.bmc.2015.11.020
85469755 136233 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 461 6 0 4 4.1 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(F)cc3F)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3741161 136233 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 461 6 0 4 4.1 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(F)cc3F)CC2)cc1 10.1016/j.bmc.2015.11.020
44377200 57104 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 437 3 0 5 4.1 Cc1nc2ccc(Br)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL165350 57104 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
ChEMBL 437 3 0 5 4.1 Cc1nc2ccc(Br)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
2284 3121 27 None -1 29 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3121 27 None -1 29 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3121 27 None -1 29 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3121 27 None -1 29 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3121 27 None -1 29 Rat 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
10645076 198616 0 None - 0 Bovine 7.1 pIC50 = 7.1 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 407 4 1 5 4.4 Oc1nc2ccc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)cc2s1 10.1021/jm970298c
CHEMBL59741 198616 0 None - 0 Bovine 7.1 pIC50 = 7.1 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
ChEMBL 407 4 1 5 4.4 Oc1nc2ccc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)cc2s1 10.1021/jm970298c
5656 201368 82 None - 43 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 10.1021/jm00172a035
CHEMBL637 201368 82 None - 43 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 10.1021/jm00172a035
10321964 18648 0 None - 0 Bovine 6.1 pIC50 = 6.1 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor determined in a filtration-based assay using [3H]prazosin as the radioligand.Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor determined in a filtration-based assay using [3H]prazosin as the radioligand.
ChEMBL 459 6 1 7 3.0 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc([N+](=O)[O-])cc3)CC1)O2 10.1021/jm00099a028
CHEMBL1203302 18648 0 None - 0 Bovine 6.1 pIC50 = 6.1 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor determined in a filtration-based assay using [3H]prazosin as the radioligand.Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor determined in a filtration-based assay using [3H]prazosin as the radioligand.
ChEMBL 459 6 1 7 3.0 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc([N+](=O)[O-])cc3)CC1)O2 10.1021/jm00099a028
CHEMBL128132 18648 0 None - 0 Bovine 6.1 pIC50 = 6.1 Binding
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor determined in a filtration-based assay using [3H]prazosin as the radioligand.Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor determined in a filtration-based assay using [3H]prazosin as the radioligand.
ChEMBL 459 6 1 7 3.0 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc([N+](=O)[O-])cc3)CC1)O2 10.1021/jm00099a028
9795857 206397 57 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 249 4 2 3 2.4 COc1ccc(C(CN)C2(O)CCCCC2)cc1 10.1021/jm00172a035
CHEMBL98158 206397 57 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 249 4 2 3 2.4 COc1ccc(C(CN)C2(O)CCCCC2)cc1 10.1021/jm00172a035
10321248 98954 0 None - 1 Bovine 5.1 pIC50 = 5.1 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL28287 98954 0 None - 1 Bovine 5.1 pIC50 = 5.1 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50722 98954 0 None - 1 Bovine 5.1 pIC50 = 5.1 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
53246941 69064 36 None - 0 Human 6.0 pIC50 = 6.0 Binding
Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRA1ASelectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRA1A
ChEMBL 458 6 2 6 3.9 C[C@@H]1CCNC(=O)c2cc3ccc(C(=O)Nc4nc5ccccc5n4CCCN(C)C)cc3n21 nan
CHEMBL1933288 69064 36 None - 0 Human 6.0 pIC50 = 6.0 Binding
Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRA1ASelectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRA1A
ChEMBL 458 6 2 6 3.9 C[C@@H]1CCNC(=O)c2cc3ccc(C(=O)Nc4nc5ccccc5n4CCCN(C)C)cc3n21 nan
44573823 192621 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 491 6 0 3 6.1 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)N(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
CHEMBL523697 192621 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 491 6 0 3 6.1 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)N(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
3033538 1287 36 None -7 9 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
7155 1287 36 None -7 9 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
781 1287 36 None -7 9 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
CHEMBL1201216 1287 36 None -7 9 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
DB00298 1287 36 None -7 9 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
133 2450 48 None -70 43 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2450 48 None -70 43 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2450 48 None -70 43 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2450 48 None -70 43 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2450 48 None -70 43 Rat 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
14739950 206515 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 263 5 1 3 2.6 COc1cccc(C(CN(C)C)C2(O)CCCC2)c1 10.1021/jm00172a035
CHEMBL98842 206515 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
ChEMBL 263 5 1 3 2.6 COc1cccc(C(CN(C)C)C2(O)CCCC2)c1 10.1021/jm00172a035
19063108 93038 0 None - 0 Bovine 6.0 pIC50 = 6.0 Binding
Binding affinity was tested on cloned bovine Alpha-1A adrenergic receptorBinding affinity was tested on cloned bovine Alpha-1A adrenergic receptor
ChEMBL 546 9 1 10 4.6 COc1ccc(CC2c3cc(OC)c(OC)cc3CCN2c2nc(N)c3cc(OC)c(OC)cc3n2)cc1OC 10.1021/jm960697s
CHEMBL24619 93038 0 None - 0 Bovine 6.0 pIC50 = 6.0 Binding
Binding affinity was tested on cloned bovine Alpha-1A adrenergic receptorBinding affinity was tested on cloned bovine Alpha-1A adrenergic receptor
ChEMBL 546 9 1 10 4.6 COc1ccc(CC2c3cc(OC)c(OC)cc3CCN2c2nc(N)c3cc(OC)c(OC)cc3n2)cc1OC 10.1021/jm960697s
85469871 136048 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 443 6 0 4 4.0 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccc3F)CC2)cc1 10.1016/j.bmc.2015.11.020
CHEMBL3739505 136048 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
ChEMBL 443 6 0 4 4.0 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccc3F)CC2)cc1 10.1016/j.bmc.2015.11.020
2801 161313 56 None -4 29 Rat 7.0 pIC50 = 7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161313 56 None -4 29 Rat 7.0 pIC50 = 7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161313 56 None -4 29 Rat 7.0 pIC50 = 7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
4209 3102 71 None -3 34 Rat 9.8 pKd = 9.8 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00025a012
4893 3102 71 None -3 34 Rat 9.8 pKd = 9.8 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00025a012
503 3102 71 None -3 34 Rat 9.8 pKd = 9.8 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00025a012
5385 3102 71 None -3 34 Rat 9.8 pKd = 9.8 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00025a012
CHEMBL2 3102 71 None -3 34 Rat 9.8 pKd = 9.8 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00025a012
DB00457 3102 71 None -3 34 Rat 9.8 pKd = 9.8 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00025a012
164612037 184785 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 184785 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 192356 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192356 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192356 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 192407 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192407 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192407 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 192419 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192419 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192419 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]prazosin from human alpha-1A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
44363762 39895 0 None - 1 Rat 9.2 pKd = 9.2 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 497 6 1 11 1.8 COc1cc2nc(N3CCN(S(=O)(=O)c4nonc4-c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm00025a012
CHEMBL147984 39895 0 None - 1 Rat 9.2 pKd = 9.2 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 497 6 1 11 1.8 COc1cc2nc(N3CCN(S(=O)(=O)c4nonc4-c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm00025a012
10250895 189738 0 None 1 6 Human 9.1 pKd = 9.1 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin)Binding affinity to alpha-1A adrenergic receptor (unknown origin)
ChEMBL 408 7 0 6 3.7 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2)CC1 10.1021/jm400408r
CHEMBL51767 189738 0 None 1 6 Human 9.1 pKd = 9.1 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin)Binding affinity to alpha-1A adrenergic receptor (unknown origin)
ChEMBL 408 7 0 6 3.7 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2)CC1 10.1021/jm400408r
10250895 189738 0 None -1 6 Rat 9.1 pKd = 9.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 408 7 0 6 3.7 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2)CC1 10.1016/s0960-894x(02)00933-2
CHEMBL51767 189738 0 None -1 6 Rat 9.1 pKd = 9.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 408 7 0 6 3.7 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2)CC1 10.1016/s0960-894x(02)00933-2
44364207 37549 0 None - 1 Rat 9.0 pKd = 9.0 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 513 6 1 11 1.0 COc1cc2nc(N3CCN(S(=O)(=O)c4no[n+]([O-])c4-c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm00025a012
CHEMBL145838 37549 0 None - 1 Rat 9.0 pKd = 9.0 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 513 6 1 11 1.0 COc1cc2nc(N3CCN(S(=O)(=O)c4no[n+]([O-])c4-c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm00025a012
71817386 102100 0 None -6 7 Rat 8.7 pKd = 8.7 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL2419769 102100 0 None -6 7 Rat 8.7 pKd = 8.7 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL3040851 102100 0 None -6 7 Rat 8.7 pKd = 8.7 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
2419 687 22 None -288 12 Rat 6.0 pKd = 6.0 Binding
In vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferensIn vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
9 687 22 None -288 12 Rat 6.0 pKd = 6.0 Binding
In vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferensIn vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
CHEMBL13647 687 22 None -288 12 Rat 6.0 pKd = 6.0 Binding
In vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferensIn vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
10317514 191921 0 None -14 7 Rat 7.9 pKd = 7.9 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 378 6 0 5 3.7 Cc1cc(=O)oc2cc(OCCCN3CCN(c4ccccc4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
CHEMBL52096 191921 0 None -14 7 Rat 7.9 pKd = 7.9 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 378 6 0 5 3.7 Cc1cc(=O)oc2cc(OCCCN3CCN(c4ccccc4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
2419 687 22 None -288 12 Rat 6.9 pKd = 6.9 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm400867d
9 687 22 None -288 12 Rat 6.9 pKd = 6.9 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm400867d
CHEMBL13647 687 22 None -288 12 Rat 6.9 pKd = 6.9 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm400867d
3584 3706 60 None -2 14 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.ejmech.2015.04.005
5401 3706 60 None -2 14 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.ejmech.2015.04.005
7302 3706 60 None -2 14 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.ejmech.2015.04.005
CHEMBL611 3706 60 None -2 14 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.ejmech.2015.04.005
DB01162 3706 60 None -2 14 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/j.ejmech.2015.04.005
73437674 118013 0 None -2 3 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 434 10 2 4 3.8 COc1ccccc1N1CCN(CCCNC(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.ejmech.2015.04.005
CHEMBL3415014 118013 0 None -2 3 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 434 10 2 4 3.8 COc1ccccc1N1CCN(CCCNC(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.ejmech.2015.04.005
14348818 109273 0 None 5 3 Rat 4.9 pKd = 4.9 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 415 7 4 7 2.9 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
CHEMBL323176 109273 0 None 5 3 Rat 4.9 pKd = 4.9 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 415 7 4 7 2.9 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
71817545 91678 0 None -2 7 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 354 7 2 5 3.0 COc1ccc2cc[nH]c2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL2419765 91678 0 None -2 7 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 354 7 2 5 3.0 COc1ccc2cc[nH]c2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
71817547 102092 0 None -81 7 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
CHEMBL2419771 102092 0 None -81 7 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
CHEMBL3040800 102092 0 None -81 7 Rat 7.9 pKd = 7.9 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
76308474 105740 0 None -162 5 Rat 6.9 pKd = 6.9 Binding
Competitive antagonist activity at alpha1A adrenergic receptor in Rattus norvegicus (rat) vas deferens assessed as inhibition of (-)-noradrenaline-induced contractionCompetitive antagonist activity at alpha1A adrenergic receptor in Rattus norvegicus (rat) vas deferens assessed as inhibition of (-)-noradrenaline-induced contraction
ChEMBL 467 5 1 9 3.1 COc1ccc(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)[C@H]3CCCC[C@@H]32)o1 10.1007/s00044-004-0024-8
CHEMBL2261607 105740 0 None -162 5 Rat 6.9 pKd = 6.9 Binding
Competitive antagonist activity at alpha1A adrenergic receptor in Rattus norvegicus (rat) vas deferens assessed as inhibition of (-)-noradrenaline-induced contractionCompetitive antagonist activity at alpha1A adrenergic receptor in Rattus norvegicus (rat) vas deferens assessed as inhibition of (-)-noradrenaline-induced contraction
ChEMBL 467 5 1 9 3.1 COc1ccc(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)[C@H]3CCCC[C@@H]32)o1 10.1007/s00044-004-0024-8
CHEMBL3138856 105740 0 None -162 5 Rat 6.9 pKd = 6.9 Binding
Competitive antagonist activity at alpha1A adrenergic receptor in Rattus norvegicus (rat) vas deferens assessed as inhibition of (-)-noradrenaline-induced contractionCompetitive antagonist activity at alpha1A adrenergic receptor in Rattus norvegicus (rat) vas deferens assessed as inhibition of (-)-noradrenaline-induced contraction
ChEMBL 467 5 1 9 3.1 COc1ccc(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)[C@H]3CCCC[C@@H]32)o1 10.1007/s00044-004-0024-8
10252540 84919 1 None -83 6 Rat 7.8 pKd = 7.8 Binding
Antagonist activity at alpha1A adrenoreceptor in Rattus norvegicus (rat) small mesenteric arteryAntagonist activity at alpha1A adrenoreceptor in Rattus norvegicus (rat) small mesenteric artery
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
CHEMBL2261604 84919 1 None -83 6 Rat 7.8 pKd = 7.8 Binding
Antagonist activity at alpha1A adrenoreceptor in Rattus norvegicus (rat) small mesenteric arteryAntagonist activity at alpha1A adrenoreceptor in Rattus norvegicus (rat) small mesenteric artery
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
10252540 84919 1 None -83 6 Rat 7.8 pKd = 7.8 Binding
Competitive antagonist activity at alpha1A adrenergic receptor in Rattus norvegicus (rat) vas deferens assessed as inhibition of (-)-noradrenaline-induced contractionCompetitive antagonist activity at alpha1A adrenergic receptor in Rattus norvegicus (rat) vas deferens assessed as inhibition of (-)-noradrenaline-induced contraction
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
CHEMBL2261604 84919 1 None -83 6 Rat 7.8 pKd = 7.8 Binding
Competitive antagonist activity at alpha1A adrenergic receptor in Rattus norvegicus (rat) vas deferens assessed as inhibition of (-)-noradrenaline-induced contractionCompetitive antagonist activity at alpha1A adrenergic receptor in Rattus norvegicus (rat) vas deferens assessed as inhibition of (-)-noradrenaline-induced contraction
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
1353 1872 85 None -10 86 Rat 7.8 pKd = 7.8 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00933-2
3559 1872 85 None -10 86 Rat 7.8 pKd = 7.8 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00933-2
86 1872 85 None -10 86 Rat 7.8 pKd = 7.8 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00933-2
CHEMBL54 1872 85 None -10 86 Rat 7.8 pKd = 7.8 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00933-2
DB00502 1872 85 None -10 86 Rat 7.8 pKd = 7.8 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00933-2
155559152 174198 0 None -21 3 Rat 5.7 pKd = 5.7 Binding
Antagonistic activity at alpha1A adrenoceptor in Sprague-Dawley rat vas deferens assessed as inhibition of noradrenaline-induced contractions after 0.5 hrs in presence of alpha2/beta adrenoceptor blocker yohimbine, propranolol by Schild plot analysisAntagonistic activity at alpha1A adrenoceptor in Sprague-Dawley rat vas deferens assessed as inhibition of noradrenaline-induced contractions after 0.5 hrs in presence of alpha2/beta adrenoceptor blocker yohimbine, propranolol by Schild plot analysis
ChEMBL 431 7 2 5 3.9 COc1ccc(N2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/j.bmc.2016.09.010
CHEMBL4561614 174198 0 None -21 3 Rat 5.7 pKd = 5.7 Binding
Antagonistic activity at alpha1A adrenoceptor in Sprague-Dawley rat vas deferens assessed as inhibition of noradrenaline-induced contractions after 0.5 hrs in presence of alpha2/beta adrenoceptor blocker yohimbine, propranolol by Schild plot analysisAntagonistic activity at alpha1A adrenoceptor in Sprague-Dawley rat vas deferens assessed as inhibition of noradrenaline-induced contractions after 0.5 hrs in presence of alpha2/beta adrenoceptor blocker yohimbine, propranolol by Schild plot analysis
ChEMBL 431 7 2 5 3.9 COc1ccc(N2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/j.bmc.2016.09.010
44294972 183426 0 None -1 3 Rat 6.7 pKd = 6.7 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 395 7 0 7 2.8 COc1cc(=O)oc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
CHEMBL48205 183426 0 None -1 3 Rat 6.7 pKd = 6.7 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 395 7 0 7 2.8 COc1cc(=O)oc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
73437673 118012 0 None -5 3 Rat 6.7 pKd = 6.7 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 420 9 2 4 3.4 COc1ccccc1N1CCN(CCCNC(=O)CCc2c[nH]c3ccccc23)CC1 10.1016/j.ejmech.2015.04.005
CHEMBL3415013 118012 0 None -5 3 Rat 6.7 pKd = 6.7 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 420 9 2 4 3.4 COc1ccccc1N1CCN(CCCNC(=O)CCc2c[nH]c3ccccc23)CC1 10.1016/j.ejmech.2015.04.005
10527913 120997 0 None - 1 Rat 8.6 pKd = 8.6 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 459 5 1 12 -0.4 COC(=O)c1c(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)CC2)no[n+]1[O-] 10.1021/jm00025a012
CHEMBL358498 120997 0 None - 1 Rat 8.6 pKd = 8.6 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 459 5 1 12 -0.4 COC(=O)c1c(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)CC2)no[n+]1[O-] 10.1021/jm00025a012
155567902 175411 0 None -6 3 Rat 6.7 pKd = 6.7 Binding
Antagonist activity at alpha-1a adrenergic receptor in SPF rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractionsAntagonist activity at alpha-1a adrenergic receptor in SPF rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions
ChEMBL 448 7 1 8 0.9 COc1cc2c(cc1OCC(O)CN1CCN(C(=O)C3CCCO3)CC1)C(=O)C(C)OC2 10.1016/j.bmc.2019.05.004
CHEMBL4589115 175411 0 None -6 3 Rat 6.7 pKd = 6.7 Binding
Antagonist activity at alpha-1a adrenergic receptor in SPF rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractionsAntagonist activity at alpha-1a adrenergic receptor in SPF rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions
ChEMBL 448 7 1 8 0.9 COc1cc2c(cc1OCC(O)CN1CCN(C(=O)C3CCCO3)CC1)C(=O)C(C)OC2 10.1016/j.bmc.2019.05.004
92766 106047 30 None 1 6 Human 6.6 pKd = 6.6 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@H]12 10.1021/jm00370a011
CHEMBL31410 106047 30 None 1 6 Human 6.6 pKd = 6.6 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@H]12 10.1021/jm00370a011
2803 939 53 None -3 19 Rat 6.6 pKd = 6.6 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
516 939 53 None -3 19 Rat 6.6 pKd = 6.6 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
704 939 53 None -3 19 Rat 6.6 pKd = 6.6 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
CHEMBL134 939 53 None -3 19 Rat 6.6 pKd = 6.6 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
DB00575 939 53 None -3 19 Rat 6.6 pKd = 6.6 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
73438500 118010 0 None -2 3 Rat 7.6 pKd = 7.6 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 392 7 2 4 3.1 COc1ccccc1N1CCN(CCCNC(=O)c2ccc3[nH]ccc3c2)CC1 10.1016/j.ejmech.2015.04.005
CHEMBL3415011 118010 0 None -2 3 Rat 7.6 pKd = 7.6 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 392 7 2 4 3.1 COc1ccccc1N1CCN(CCCNC(=O)c2ccc3[nH]ccc3c2)CC1 10.1016/j.ejmech.2015.04.005
44294683 189265 0 None -3 3 Rat 6.6 pKd = 6.6 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 379 6 0 6 3.1 Cc1cc(=O)oc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
CHEMBL51681 189265 0 None -3 3 Rat 6.6 pKd = 6.6 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 379 6 0 6 3.1 Cc1cc(=O)oc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
44364190 39512 0 None - 1 Rat 8.5 pKd = 8.5 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 539 6 1 11 1.4 COc1cc2nc(N3CCN(S(=O)(=O)c4no[n+]([O-])c4C4=C/C=C\C=C/C=C\4)CC3)nc(N)c2cc1OC 10.1021/jm00025a012
CHEMBL147624 39512 0 None - 1 Rat 8.5 pKd = 8.5 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 539 6 1 11 1.4 COc1cc2nc(N3CCN(S(=O)(=O)c4no[n+]([O-])c4C4=C/C=C\C=C/C=C\4)CC3)nc(N)c2cc1OC 10.1021/jm00025a012
71817549 102094 0 None -7 7 Rat 8.4 pKd = 8.4 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
CHEMBL3040803 102094 0 None -7 7 Rat 8.4 pKd = 8.4 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
CHEMBL3216590 102094 0 None -7 7 Rat 8.4 pKd = 8.4 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
2142 3035 54 None -2 37 Human 7.5 pKd = 7.5 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00370a011
4920903 3035 54 None -2 37 Human 7.5 pKd = 7.5 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00370a011
502 3035 54 None -2 37 Human 7.5 pKd = 7.5 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00370a011
5775 3035 54 None -2 37 Human 7.5 pKd = 7.5 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00370a011
CHEMBL597 3035 54 None -2 37 Human 7.5 pKd = 7.5 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00370a011
DB00692 3035 54 None -2 37 Human 7.5 pKd = 7.5 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00370a011
4418 33985 80 None -10 7 Rat 7.5 pKd = 7.5 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.ejmech.2015.04.005
CHEMBL142635 33985 80 None -10 7 Rat 7.5 pKd = 7.5 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.ejmech.2015.04.005
71817547 102092 0 None -81 7 Rat 7.5 pKd = 7.5 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
CHEMBL2419771 102092 0 None -81 7 Rat 7.5 pKd = 7.5 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
CHEMBL3040800 102092 0 None -81 7 Rat 7.5 pKd = 7.5 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
44294973 183409 0 None 1 3 Rat 6.5 pKd = 6.5 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 394 7 0 6 3.4 COc1cc(=O)oc2cc(OCCCN3CCN(c4ccccc4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
CHEMBL48194 183409 0 None 1 3 Rat 6.5 pKd = 6.5 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 394 7 0 6 3.4 COc1cc(=O)oc2cc(OCCCN3CCN(c4ccccc4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
135398737 942 89 None -5 92 Human 7.4 pKd = 7.4 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00370a011
38 942 89 None -5 92 Human 7.4 pKd = 7.4 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00370a011
722 942 89 None -5 92 Human 7.4 pKd = 7.4 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00370a011
CHEMBL42 942 89 None -5 92 Human 7.4 pKd = 7.4 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00370a011
DB00363 942 89 None -5 92 Human 7.4 pKd = 7.4 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00370a011
86288949 112115 0 None -5 5 Rat 7.4 pKd = 7.4 Binding
Antagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 mins
ChEMBL 434 8 0 4 3.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3233665 112115 0 None -5 5 Rat 7.4 pKd = 7.4 Binding
Antagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 mins
ChEMBL 434 8 0 4 3.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3302599 112115 0 None -5 5 Rat 7.4 pKd = 7.4 Binding
Antagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 mins
ChEMBL 434 8 0 4 3.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
2419 687 22 None -275 12 Human 6.4 pKd = 6.4 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm011066n
9 687 22 None -275 12 Human 6.4 pKd = 6.4 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm011066n
CHEMBL13647 687 22 None -275 12 Human 6.4 pKd = 6.4 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm011066n
102 4051 44 None -346 50 Human 6.4 pKd = 6.4 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00370a011
3659 4051 44 None -346 50 Human 6.4 pKd = 6.4 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00370a011
8969 4051 44 None -346 50 Human 6.4 pKd = 6.4 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00370a011
CHEMBL15245 4051 44 None -346 50 Human 6.4 pKd = 6.4 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00370a011
DB01392 4051 44 None -346 50 Human 6.4 pKd = 6.4 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00370a011
15112598 9216 0 None -2 3 Rat 5.4 pKd = 5.4 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 444 9 3 7 3.3 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(OC(C)C2=NCCN2)c(Cl)c1 10.1021/jm00115a008
CHEMBL111090 9216 0 None -2 3 Rat 5.4 pKd = 5.4 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 444 9 3 7 3.3 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(OC(C)C2=NCCN2)c(Cl)c1 10.1021/jm00115a008
134149596 147921 0 None -10 4 Rat 8.4 pKd = 8.4 Binding
Competitive antagonist activity at alpha1A-adrenoceptor in Wistar rat prostatic vas deference assessed as inhibition of (-)-NE-induced contractions preincubated for 60 mins before (-)-NE challenge measured after 45 mins by Schild plot analysisCompetitive antagonist activity at alpha1A-adrenoceptor in Wistar rat prostatic vas deference assessed as inhibition of (-)-NE-induced contractions preincubated for 60 mins before (-)-NE challenge measured after 45 mins by Schild plot analysis
ChEMBL 368 6 0 5 3.6 CC(C)Oc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2016.06.052
CHEMBL3938038 147921 0 None -10 4 Rat 8.4 pKd = 8.4 Binding
Competitive antagonist activity at alpha1A-adrenoceptor in Wistar rat prostatic vas deference assessed as inhibition of (-)-NE-induced contractions preincubated for 60 mins before (-)-NE challenge measured after 45 mins by Schild plot analysisCompetitive antagonist activity at alpha1A-adrenoceptor in Wistar rat prostatic vas deference assessed as inhibition of (-)-NE-induced contractions preincubated for 60 mins before (-)-NE challenge measured after 45 mins by Schild plot analysis
ChEMBL 368 6 0 5 3.6 CC(C)Oc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2016.06.052
491 191 4 None -44 12 Rat 8.4 pKd = 8.4 Binding
In vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferensIn vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
9891167 191 4 None -44 12 Rat 8.4 pKd = 8.4 Binding
In vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferensIn vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
CHEMBL13856 191 4 None -44 12 Rat 8.4 pKd = 8.4 Binding
In vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferensIn vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
71817545 91678 0 None -2 7 Rat 8.3 pKd = 8.3 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 354 7 2 5 3.0 COc1ccc2cc[nH]c2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL2419765 91678 0 None -2 7 Rat 8.3 pKd = 8.3 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 354 7 2 5 3.0 COc1ccc2cc[nH]c2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
14348818 109273 0 None 5 3 Rat 5.4 pKd = 5.4 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 415 7 4 7 2.9 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
CHEMBL323176 109273 0 None 5 3 Rat 5.4 pKd = 5.4 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 415 7 4 7 2.9 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
44294687 96446 0 None 7 3 Rat 7.4 pKd = 7.4 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 380 6 0 7 2.5 Cc1cc(=O)oc2cc(OCCCN3CCN(c4ncccn4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
CHEMBL265805 96446 0 None 7 3 Rat 7.4 pKd = 7.4 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 380 6 0 7 2.5 Cc1cc(=O)oc2cc(OCCCN3CCN(c4ncccn4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
155534921 171411 0 None -5 3 Rat 6.4 pKd = 6.4 Binding
Antagonistic activity at alpha1A adrenoceptor in Sprague-Dawley rat vas deferens assessed as inhibition of noradrenaline-induced contractions after 0.5 hrs in presence of alpha2/beta adrenoceptor blocker yohimbine, propranolol by Schild plot analysisAntagonistic activity at alpha1A adrenoceptor in Sprague-Dawley rat vas deferens assessed as inhibition of noradrenaline-induced contractions after 0.5 hrs in presence of alpha2/beta adrenoceptor blocker yohimbine, propranolol by Schild plot analysis
ChEMBL 461 8 2 6 3.9 COc1ccc(OC)c(N2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)c1 10.1016/j.bmc.2016.09.010
CHEMBL4471070 171411 0 None -5 3 Rat 6.4 pKd = 6.4 Binding
Antagonistic activity at alpha1A adrenoceptor in Sprague-Dawley rat vas deferens assessed as inhibition of noradrenaline-induced contractions after 0.5 hrs in presence of alpha2/beta adrenoceptor blocker yohimbine, propranolol by Schild plot analysisAntagonistic activity at alpha1A adrenoceptor in Sprague-Dawley rat vas deferens assessed as inhibition of noradrenaline-induced contractions after 0.5 hrs in presence of alpha2/beta adrenoceptor blocker yohimbine, propranolol by Schild plot analysis
ChEMBL 461 8 2 6 3.9 COc1ccc(OC)c(N2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)c1 10.1016/j.bmc.2016.09.010
44294988 192647 0 None 1 3 Rat 7.4 pKd = 7.4 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 396 7 0 8 2.2 COc1cc(=O)oc2cc(OCCCN3CCN(c4ncccn4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
CHEMBL52384 192647 0 None 1 3 Rat 7.4 pKd = 7.4 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 396 7 0 8 2.2 COc1cc(=O)oc2cc(OCCCN3CCN(c4ncccn4)CC3)ccc12 10.1016/s0960-894x(02)00933-2
73437729 118017 0 None -2 3 Rat 7.3 pKd = 7.3 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 426 7 2 4 3.8 COc1ccccc1N1CCN(CCCNC(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2015.04.005
CHEMBL3415018 118017 0 None -2 3 Rat 7.3 pKd = 7.3 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 426 7 2 4 3.8 COc1ccccc1N1CCN(CCCNC(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2015.04.005
86288950 112133 0 None -15 6 Rat 7.3 pKd = 7.3 Binding
Antagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 mins
ChEMBL 452 8 0 4 3.9 CN1C(=O)N(CCCCCN2CCN(c3ccccc3F)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3233666 112133 0 None -15 6 Rat 7.3 pKd = 7.3 Binding
Antagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 mins
ChEMBL 452 8 0 4 3.9 CN1C(=O)N(CCCCCN2CCN(c3ccccc3F)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3302931 112133 0 None -15 6 Rat 7.3 pKd = 7.3 Binding
Antagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar (Krf:(WI) WU) rat endothelium-denuded tail artery assessed as inhibition of noradrenaline-induced contraction after 30 mins
ChEMBL 452 8 0 4 3.9 CN1C(=O)N(CCCCCN2CCN(c3ccccc3F)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
71817386 102100 0 None -6 7 Rat 8.3 pKd = 8.3 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL2419769 102100 0 None -6 7 Rat 8.3 pKd = 8.3 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL3040851 102100 0 None -6 7 Rat 8.3 pKd = 8.3 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
10694582 38316 0 None - 1 Rat 8.3 pKd = 8.3 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 444 5 2 11 -1.1 COc1cc2nc(N3CCN(C(=O)c4no[n+]([O-])c4C(N)=O)CC3)nc(N)c2cc1OC 10.1021/jm00025a012
CHEMBL146481 38316 0 None - 1 Rat 8.3 pKd = 8.3 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 444 5 2 11 -1.1 COc1cc2nc(N3CCN(C(=O)c4no[n+]([O-])c4C(N)=O)CC3)nc(N)c2cc1OC 10.1021/jm00025a012
73437677 118018 0 None -9 3 Rat 7.3 pKd = 7.3 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 406 7 1 5 3.1 COc1ccccc1N1CCN(CCCNC(=O)c2cn(C)c3ccccc23)CC1 10.1016/j.ejmech.2015.04.005
CHEMBL3415019 118018 0 None -9 3 Rat 7.3 pKd = 7.3 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 406 7 1 5 3.1 COc1ccccc1N1CCN(CCCNC(=O)c2cn(C)c3ccccc23)CC1 10.1016/j.ejmech.2015.04.005
73437675 118014 0 None -2 3 Rat 7.3 pKd = 7.3 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 408 7 3 5 2.8 COc1ccccc1N1CCN(CCCNC(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1016/j.ejmech.2015.04.005
CHEMBL3415015 118014 0 None -2 3 Rat 7.3 pKd = 7.3 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 408 7 3 5 2.8 COc1ccccc1N1CCN(CCCNC(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1016/j.ejmech.2015.04.005
73437730 118015 0 None -2 3 Rat 7.2 pKd = 7.2 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 437 8 2 6 3.0 COc1ccccc1N1CCN(CCCNC(=O)c2cc3cccc([N+](=O)[O-])c3[nH]2)CC1 10.1016/j.ejmech.2015.04.005
CHEMBL3415016 118015 0 None -2 3 Rat 7.2 pKd = 7.2 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 437 8 2 6 3.0 COc1ccccc1N1CCN(CCCNC(=O)c2cc3cccc([N+](=O)[O-])c3[nH]2)CC1 10.1016/j.ejmech.2015.04.005
73437678 118016 0 None -4 3 Rat 7.2 pKd = 7.2 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 470 7 2 4 3.9 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccc(Br)cc3[nH]2)CC1 10.1016/j.ejmech.2015.04.005
CHEMBL3415017 118016 0 None -4 3 Rat 7.2 pKd = 7.2 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 470 7 2 4 3.9 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccc(Br)cc3[nH]2)CC1 10.1016/j.ejmech.2015.04.005
9871544 14086 1 None -141 11 Human 6.2 pKd = 6.2 Binding
Binding affinity to Alpha-1A adrenergic receptorBinding affinity to Alpha-1A adrenergic receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1076624 14086 1 None -141 11 Human 6.2 pKd = 6.2 Binding
Binding affinity to Alpha-1A adrenergic receptorBinding affinity to Alpha-1A adrenergic receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1198948 14086 1 None -141 11 Human 6.2 pKd = 6.2 Binding
Binding affinity to Alpha-1A adrenergic receptorBinding affinity to Alpha-1A adrenergic receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
118733023 118019 0 None -2 3 Rat 8.1 pKd = 8.1 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 482 9 1 5 4.6 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccc3n2Cc2ccccc2)CC1 10.1016/j.ejmech.2015.04.005
CHEMBL3415020 118019 0 None -2 3 Rat 8.1 pKd = 8.1 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 482 9 1 5 4.6 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccc3n2Cc2ccccc2)CC1 10.1016/j.ejmech.2015.04.005
73438501 118011 0 None -1 3 Rat 8.1 pKd = 8.1 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 406 8 2 4 3.0 COc1ccccc1N1CCN(CCCNC(=O)Cc2c[nH]c3ccccc23)CC1 10.1016/j.ejmech.2015.04.005
CHEMBL3415012 118011 0 None -1 3 Rat 8.1 pKd = 8.1 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 406 8 2 4 3.0 COc1ccccc1N1CCN(CCCNC(=O)Cc2c[nH]c3ccccc23)CC1 10.1016/j.ejmech.2015.04.005
44294991 101040 0 None 2 3 Rat 8.1 pKd = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 424 8 0 7 3.4 COc1ccccc1N1CCN(CCCOc2ccc3c(OC)cc(=O)oc3c2)CC1 10.1016/s0960-894x(02)00933-2
CHEMBL298108 101040 0 None 2 3 Rat 8.1 pKd = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
ChEMBL 424 8 0 7 3.4 COc1ccccc1N1CCN(CCCOc2ccc3c(OC)cc(=O)oc3c2)CC1 10.1016/s0960-894x(02)00933-2
73437676 117979 0 None -1 3 Rat 7.1 pKd = 7.1 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 422 8 2 5 3.1 COc1ccc2[nH]c(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)cc2c1 10.1016/j.ejmech.2015.04.005
CHEMBL3414578 117979 0 None -1 3 Rat 7.1 pKd = 7.1 Binding
Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 minsAntagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins
ChEMBL 422 8 2 5 3.1 COc1ccc2[nH]c(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)cc2c1 10.1016/j.ejmech.2015.04.005
14348818 109273 0 None 5 3 Rat 5.1 pKd = 5.1 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 415 7 4 7 2.9 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
CHEMBL323176 109273 0 None 5 3 Rat 5.1 pKd = 5.1 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
ChEMBL 415 7 4 7 2.9 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
490 190 5 None -36 12 Rat 8.1 pKd = 8.1 Binding
In vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferensIn vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
9890547 190 5 None -36 12 Rat 8.1 pKd = 8.1 Binding
In vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferensIn vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
CHEMBL268758 190 5 None -36 12 Rat 8.1 pKd = 8.1 Binding
In vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferensIn vitro functional activity at Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
10550345 118676 0 None - 1 Rat 8.0 pKd = 8.0 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 426 4 1 11 -0.3 COc1cc2nc(N3CCN(C(=O)c4no[n+]([O-])c4C#N)CC3)nc(N)c2cc1OC 10.1021/jm00025a012
CHEMBL343188 118676 0 None - 1 Rat 8.0 pKd = 8.0 Binding
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic stripsPartial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
ChEMBL 426 4 1 11 -0.3 COc1cc2nc(N3CCN(C(=O)c4no[n+]([O-])c4C#N)CC3)nc(N)c2cc1OC 10.1021/jm00025a012
71817549 102094 0 None -7 7 Rat 8.0 pKd = 8.0 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
CHEMBL3040803 102094 0 None -7 7 Rat 8.0 pKd = 8.0 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
CHEMBL3216590 102094 0 None -7 7 Rat 8.0 pKd = 8.0 Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysisAntagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
10531157 37554 0 None 2290 3 Human 11.0 pKi = 11 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 572 8 2 8 3.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3[N+](=O)[O-])CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145843 37554 0 None 2290 3 Human 11.0 pKi = 11 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 572 8 2 8 3.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3[N+](=O)[O-])CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
60820 4228 12 None 1 13 Human 10.7 pKi = 10.7 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1016/j.bmc.2008.02.091
CHEMBL10085 4228 12 None 1 13 Human 10.7 pKi = 10.7 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1016/j.bmc.2008.02.091
10745901 37216 0 None 1698 3 Human 10.7 pKi = 10.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 586 8 2 8 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3[N+](=O)[O-])C[C@@H]2C)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145547 37216 0 None 1698 3 Human 10.7 pKi = 10.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 586 8 2 8 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3[N+](=O)[O-])C[C@@H]2C)C1c1ccc(F)c(F)c1 10.1021/jm990202+
129211 3680 75 None -1 16 Human 10.5 pKi = 10.5 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
2562 3680 75 None -1 16 Human 10.5 pKi = 10.5 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
488 3680 75 None -1 16 Human 10.5 pKi = 10.5 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
CHEMBL836 3680 75 None -1 16 Human 10.5 pKi = 10.5 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
DB00706 3680 75 None -1 16 Human 10.5 pKi = 10.5 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
164089 109851 20 None -1 5 Bovine 10.5 pKi = 10.5 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 395 5 1 7 3.4 COc1cc2c(cc1OC)CN(c1cc(N)c3cc(OC)c(OC)cc3n1)CC2 10.1021/jm00018a001
CHEMBL324090 109851 20 None -1 5 Bovine 10.5 pKi = 10.5 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 395 5 1 7 3.4 COc1cc2c(cc1OC)CN(c1cc(N)c3cc(OC)c(OC)cc3n1)CC2 10.1021/jm00018a001
129211 3680 75 None -2 16 Rat 10.5 pKi = 10.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm990567u
2562 3680 75 None -2 16 Rat 10.5 pKi = 10.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm990567u
488 3680 75 None -2 16 Rat 10.5 pKi = 10.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm990567u
CHEMBL836 3680 75 None -2 16 Rat 10.5 pKi = 10.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm990567u
DB00706 3680 75 None -2 16 Rat 10.5 pKi = 10.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm990567u
4151 3537 85 None 16 3 Human 10.4 pKi = 10.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1016/j.bmcl.2004.11.032
493 3537 85 None 16 3 Human 10.4 pKi = 10.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1016/j.bmcl.2004.11.032
5312125 3537 85 None 16 3 Human 10.4 pKi = 10.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1016/j.bmcl.2004.11.032
CHEMBL24778 3537 85 None 16 3 Human 10.4 pKi = 10.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1016/j.bmcl.2004.11.032
DB06207 3537 85 None 16 3 Human 10.4 pKi = 10.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1016/j.bmcl.2004.11.032
4151 3537 85 None 16 3 Human 10.4 pKi = 10.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/jm960697s
493 3537 85 None 16 3 Human 10.4 pKi = 10.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/jm960697s
5312125 3537 85 None 16 3 Human 10.4 pKi = 10.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/jm960697s
CHEMBL24778 3537 85 None 16 3 Human 10.4 pKi = 10.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/jm960697s
DB06207 3537 85 None 16 3 Human 10.4 pKi = 10.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/jm960697s
44298611 100173 0 None 125 3 Human 10.4 pKi = 10.4 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 440 7 1 6 2.3 Cc1[nH]c(=O)n(CCCN2CCN(c3ccccc3OCC(F)(F)F)CC2)c(=O)c1C 10.1016/s0960-894x(03)00305-6
CHEMBL292189 100173 0 None 125 3 Human 10.4 pKi = 10.4 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 440 7 1 6 2.3 Cc1[nH]c(=O)n(CCCN2CCN(c3ccccc3OCC(F)(F)F)CC2)c(=O)c1C 10.1016/s0960-894x(03)00305-6
164089 109851 20 None -1 5 Human 10.4 pKi = 10.4 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 395 5 1 7 3.4 COc1cc2c(cc1OC)CN(c1cc(N)c3cc(OC)c(OC)cc3n1)CC2 10.1021/jm00018a001
CHEMBL324090 109851 20 None -1 5 Human 10.4 pKi = 10.4 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 395 5 1 7 3.4 COc1cc2c(cc1OC)CN(c1cc(N)c3cc(OC)c(OC)cc3n1)CC2 10.1021/jm00018a001
10789770 100405 0 None 1 5 Rat 10.4 pKi = 10.4 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 451 6 1 7 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)c(OC)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL293695 100405 0 None 1 5 Rat 10.4 pKi = 10.4 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 451 6 1 7 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)c(OC)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
10622402 201063 0 None 6 3 Rat 10.4 pKi = 10.4 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 427 5 1 7 2.4 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2s1 10.1021/jm000541z
CHEMBL62028 201063 0 None 6 3 Rat 10.4 pKi = 10.4 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 427 5 1 7 2.4 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2s1 10.1021/jm000541z
4209 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2014.12.045
4893 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2014.12.045
503 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2014.12.045
5385 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2014.12.045
CHEMBL2 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2014.12.045
DB00457 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2014.12.045
4209 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm401895u
4893 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm401895u
503 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm401895u
5385 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm401895u
CHEMBL2 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm401895u
DB00457 3102 71 None -2 34 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm401895u
76333279 84378 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 405 8 1 5 4.6 COc1cccc(OC)c1OCCN[C@H]1C[C@@H](c2ccccc2)c2ccccc2O1 10.1007/s00044-010-9379-1
CHEMBL2234441 84378 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 405 8 1 5 4.6 COc1cccc(OC)c1OCCN[C@H]1C[C@@H](c2ccccc2)c2ccccc2O1 10.1007/s00044-010-9379-1
10698570 118240 0 None 257 3 Human 10.3 pKi = 10.3 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 586 8 2 8 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3[N+](=O)[O-])C[C@H]2C)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL341849 118240 0 None 257 3 Human 10.3 pKi = 10.3 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 586 8 2 8 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3[N+](=O)[O-])C[C@H]2C)C1c1ccc(F)c(F)c1 10.1021/jm990202+
11742834 165206 0 None -1 7 Human 10.3 pKi = 10.3 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 419 9 1 5 4.7 COc1cccc(OC)c1OCCNC[C@@H]1C[C@H](c2ccccc2)c2ccccc2O1 10.1021/jm011066n
CHEMBL42472 165206 0 None -1 7 Human 10.3 pKi = 10.3 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 419 9 1 5 4.7 COc1cccc(OC)c1OCCNC[C@@H]1C[C@H](c2ccccc2)c2ccccc2O1 10.1021/jm011066n
76333279 84378 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 405 8 1 5 4.6 COc1cccc(OC)c1OCCN[C@H]1C[C@@H](c2ccccc2)c2ccccc2O1 10.1007/s00044-010-9379-1
CHEMBL2234441 84378 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 405 8 1 5 4.6 COc1cccc(OC)c1OCCN[C@H]1C[C@@H](c2ccccc2)c2ccccc2O1 10.1007/s00044-010-9379-1
129211 3680 75 None -1 16 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2010.09.042
2562 3680 75 None -1 16 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2010.09.042
488 3680 75 None -1 16 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2010.09.042
CHEMBL836 3680 75 None -1 16 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2010.09.042
DB00706 3680 75 None -1 16 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2010.09.042
19085858 103662 0 None 173 3 Human 10.2 pKi = 10.2 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in CHO cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in CHO cells
ChEMBL 501 7 0 8 3.6 CSc1ccc2c(c1)C(=O)N(CCCCN1CCC(n3c(=O)oc4ccccc43)CC1)S2(=O)=O 10.1016/s0960-894x(98)00446-6
CHEMBL309518 103662 0 None 173 3 Human 10.2 pKi = 10.2 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in CHO cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in CHO cells
ChEMBL 501 7 0 8 3.6 CSc1ccc2c(c1)C(=O)N(CCCCN1CCC(n3c(=O)oc4ccccc43)CC1)S2(=O)=O 10.1016/s0960-894x(98)00446-6
10817365 36468 0 None 501 3 Human 10.2 pKi = 10.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 599 9 2 7 3.9 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL144933 36468 0 None 501 3 Human 10.2 pKi = 10.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 599 9 2 7 3.9 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)C(=O)N1 10.1021/jm990201h
10651636 37613 0 None 1318 3 Human 10.2 pKi = 10.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 630 8 2 5 6.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccc(C)cc3)(c3ccccc3C)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL145894 37613 0 None 1318 3 Human 10.2 pKi = 10.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 630 8 2 5 6.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccc(C)cc3)(c3ccccc3C)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
44298664 195600 0 None 31 3 Human 10.2 pKi = 10.2 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 462 7 1 6 2.8 O=c1[nH]c2ccccc2c(=O)n1CCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
CHEMBL56863 195600 0 None 31 3 Human 10.2 pKi = 10.2 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 462 7 1 6 2.8 O=c1[nH]c2ccccc2c(=O)n1CCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
19085914 204101 0 None 234 3 Human 10.2 pKi = 10.2 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 485 7 0 8 2.9 COc1ccc2c(c1)C(=O)N(CCCCN1CCC(n3c(=O)oc4ccccc43)CC1)S2(=O)=O 10.1016/s0960-894x(98)00446-6
CHEMBL83340 204101 0 None 234 3 Human 10.2 pKi = 10.2 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 485 7 0 8 2.9 COc1ccc2c(c1)C(=O)N(CCCCN1CCC(n3c(=O)oc4ccccc43)CC1)S2(=O)=O 10.1016/s0960-894x(98)00446-6
49781233 17728 0 None 5 3 Bovine 10.2 pKi = 10.2 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 392 2 0 7 2.9 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4nnnn4C)cc32)CC1 10.1021/jm100652h
CHEMBL1259217 17728 0 None 5 3 Bovine 10.2 pKi = 10.2 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 392 2 0 7 2.9 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4nnnn4C)cc32)CC1 10.1021/jm100652h
44324405 205024 0 None 117 3 Human 10.2 pKi = 10.2 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 511 7 2 4 3.9 CN1C=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC1=O 10.1021/jm990612y
CHEMBL90086 205024 0 None 117 3 Human 10.2 pKi = 10.2 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 511 7 2 4 3.9 CN1C=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC1=O 10.1021/jm990612y
10767606 205708 0 None 371 3 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 497 7 3 4 3.6 N#Cc1cc(F)ccc1C1CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2017.03.025
CHEMBL94188 205708 0 None 371 3 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 497 7 3 4 3.6 N#Cc1cc(F)ccc1C1CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2017.03.025
10767606 205708 0 None 371 3 Human 10.2 pKi = 10.2 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 497 7 3 4 3.6 N#Cc1cc(F)ccc1C1CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
CHEMBL94188 205708 0 None 371 3 Human 10.2 pKi = 10.2 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 497 7 3 4 3.6 N#Cc1cc(F)ccc1C1CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
4209 3102 71 None -3 34 Rat 10.2 pKi = 10.2 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990277d
4893 3102 71 None -3 34 Rat 10.2 pKi = 10.2 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990277d
503 3102 71 None -3 34 Rat 10.2 pKi = 10.2 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990277d
5385 3102 71 None -3 34 Rat 10.2 pKi = 10.2 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990277d
CHEMBL2 3102 71 None -3 34 Rat 10.2 pKi = 10.2 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990277d
DB00457 3102 71 None -3 34 Rat 10.2 pKi = 10.2 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990277d
9913449 105958 0 None 13 3 Human 10.1 pKi = 10.1 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 489 6 0 7 3.5 O=C1c2cc(Cl)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL313990 105958 0 None 13 3 Human 10.1 pKi = 10.1 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 489 6 0 7 3.5 O=C1c2cc(Cl)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
10526964 205227 0 None 1 3 Bovine 10.1 pKi = 10.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 437 10 1 6 3.2 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC2CC2)CC1 10.1021/jm970166j
CHEMBL91278 205227 0 None 1 3 Bovine 10.1 pKi = 10.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 437 10 1 6 3.2 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC2CC2)CC1 10.1021/jm970166j
76315111 84380 0 None - 1 Human 10.1 pKi = 10.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 421 8 1 5 5.3 COc1cccc(OC)c1OCCN[C@H]1C[C@@H](c2ccccc2)c2ccccc2S1 10.1007/s00044-010-9379-1
CHEMBL2234443 84380 0 None - 1 Human 10.1 pKi = 10.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 421 8 1 5 5.3 COc1cccc(OC)c1OCCN[C@H]1C[C@@H](c2ccccc2)c2ccccc2S1 10.1007/s00044-010-9379-1
10699164 36782 0 None 151 3 Human 10.1 pKi = 10.1 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 552 7 2 7 3.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C#N)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145190 36782 0 None 151 3 Human 10.1 pKi = 10.1 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 552 7 2 7 3.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C#N)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
499 4002 15 None -1 15 Rat 10.1 pKi = 10.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
5685 4002 15 None -1 15 Rat 10.1 pKi = 10.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
CHEMBL25554 4002 15 None -1 15 Rat 10.1 pKi = 10.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
52942381 17695 0 None -2 4 Bovine 10.1 pKi = 10.1 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 339 2 1 4 3.1 CN1CCN(C2Cc3ccccc3Sc3ccc(CN)cc32)CC1 10.1021/jm100652h
CHEMBL1259113 17695 0 None -2 4 Bovine 10.1 pKi = 10.1 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 339 2 1 4 3.1 CN1CCN(C2Cc3ccccc3Sc3ccc(CN)cc32)CC1 10.1021/jm100652h
19085876 204090 0 None 87 3 Human 10.1 pKi = 10.1 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 473 6 0 7 3.0 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3cc(F)ccc32)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL83272 204090 0 None 87 3 Human 10.1 pKi = 10.1 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 473 6 0 7 3.0 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3cc(F)ccc32)CC1 10.1016/s0960-894x(98)00446-6
49781447 17647 0 None 3 4 Bovine 10.1 pKi = 10.1 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 391 2 0 6 3.5 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ncn(C)n4)cc32)CC1 10.1021/jm100652h
CHEMBL1258988 17647 0 None 3 4 Bovine 10.1 pKi = 10.1 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 391 2 0 6 3.5 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ncn(C)n4)cc32)CC1 10.1021/jm100652h
4209 3102 71 None -3 34 Rat 10.1 pKi = 10.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
4893 3102 71 None -3 34 Rat 10.1 pKi = 10.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
503 3102 71 None -3 34 Rat 10.1 pKi = 10.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
5385 3102 71 None -3 34 Rat 10.1 pKi = 10.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL2 3102 71 None -3 34 Rat 10.1 pKi = 10.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
DB00457 3102 71 None -3 34 Rat 10.1 pKi = 10.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
49781892 17704 0 None -1 4 Bovine 10.1 pKi = 10.1 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 381 3 1 4 3.3 CC(=O)NCc1ccc2c(c1)C(N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259144 17704 0 None -1 4 Bovine 10.1 pKi = 10.1 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 381 3 1 4 3.3 CC(=O)NCc1ccc2c(c1)C(N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
44289248 168399 0 None 4 7 Human 10.1 pKi = 10.1 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2S1 10.1021/jm011066n
CHEMBL43905 168399 0 None 4 7 Human 10.1 pKi = 10.1 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2S1 10.1021/jm011066n
76315111 84380 0 None - 1 Human 10.1 pKi = 10.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 421 8 1 5 5.3 COc1cccc(OC)c1OCCN[C@H]1C[C@@H](c2ccccc2)c2ccccc2S1 10.1007/s00044-010-9379-1
CHEMBL2234443 84380 0 None - 1 Human 10.1 pKi = 10.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 421 8 1 5 5.3 COc1cccc(OC)c1OCCN[C@H]1C[C@@H](c2ccccc2)c2ccccc2S1 10.1007/s00044-010-9379-1
10716965 167386 0 None 10 3 Rat 10.1 pKi = 10.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 419 4 1 5 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(C)c(C)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL431720 167386 0 None 10 3 Rat 10.1 pKi = 10.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 419 4 1 5 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(C)c(C)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
10812130 197492 0 None 2 3 Rat 10.1 pKi = 10.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 421 5 1 6 2.4 COc1ccc2c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)[nH]c2c1 10.1021/jm000541z
CHEMBL58956 197492 0 None 2 3 Rat 10.1 pKi = 10.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 421 5 1 6 2.4 COc1ccc2c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)[nH]c2c1 10.1021/jm000541z
10693231 201065 0 None -2 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 416 4 1 6 2.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C#N)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL62033 201065 0 None -2 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 416 4 1 6 2.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C#N)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
11039289 116327 0 None 12 5 Human 10.0 pKi = 10.0 Binding
Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)
ChEMBL 600 13 1 9 4.7 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCCCO[N+](=O)[O-])CC3)cccc2c1=O 10.1021/jm030825u
CHEMBL338029 116327 0 None 12 5 Human 10.0 pKi = 10.0 Binding
Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)
ChEMBL 600 13 1 9 4.7 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCCCO[N+](=O)[O-])CC3)cccc2c1=O 10.1021/jm030825u
34580 17694 2 None -1 4 Bovine 10.0 pKi = 10.0 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 335 1 0 4 3.6 CN1CCN(C2Cc3ccccc3Sc3ccc(C#N)cc32)CC1 10.1021/jm100652h
CHEMBL1259112 17694 2 None -1 4 Bovine 10.0 pKi = 10.0 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 335 1 0 4 3.6 CN1CCN(C2Cc3ccccc3Sc3ccc(C#N)cc32)CC1 10.1021/jm100652h
19085926 203822 0 None 199 3 Human 10.0 pKi = 10 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 469 6 0 7 3.2 Cc1ccc2c(c1)C(=O)N(CCCCN1CCC(n3c(=O)oc4ccccc43)CC1)S2(=O)=O 10.1016/s0960-894x(98)00446-6
CHEMBL81006 203822 0 None 199 3 Human 10.0 pKi = 10 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 469 6 0 7 3.2 Cc1ccc2c(c1)C(=O)N(CCCCN1CCC(n3c(=O)oc4ccccc43)CC1)S2(=O)=O 10.1016/s0960-894x(98)00446-6
9959671 32437 0 None 363 3 Human 10.0 pKi = 10 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 0 7 5.6 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL141322 32437 0 None 363 3 Human 10.0 pKi = 10 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 0 7 5.6 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10721751 34392 0 None 1412 3 Human 10.0 pKi = 10 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 569 10 1 6 4.9 COC(=O)C1=C(C)NC(=O)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL142981 34392 0 None 1412 3 Human 10.0 pKi = 10 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 569 10 1 6 4.9 COC(=O)C1=C(C)NC(=O)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10031709 37064 0 None 2511 3 Human 10.0 pKi = 10 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 613 10 0 5 8.1 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccc(C)cc3)(c3ccccc3C)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL145411 37064 0 None 2511 3 Human 10.0 pKi = 10 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 613 10 0 5 8.1 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccc(C)cc3)(c3ccccc3C)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10651219 33501 0 None 1000 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 600 10 3 8 2.1 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C(=O)N1 10.1021/jm990202+
CHEMBL142236 33501 0 None 1000 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 600 10 3 8 2.1 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C(=O)N1 10.1021/jm990202+
10650726 33521 0 None 87 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 571 9 2 7 3.8 CCOc1ccccc1N1CCN(CCCNC(=O)N2C(=O)NC(C)=C(C(=O)OC)C2c2ccc(F)c(F)c2)CC1 10.1021/jm990202+
CHEMBL142251 33521 0 None 87 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 571 9 2 7 3.8 CCOc1ccccc1N1CCN(CCCNC(=O)N2C(=O)NC(C)=C(C(=O)OC)C2c2ccc(F)c(F)c2)CC1 10.1021/jm990202+
10531476 34107 0 None 269 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 590 8 2 10 3.0 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc2nonc2c1 10.1021/jm990200p
CHEMBL142743 34107 0 None 269 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 590 8 2 10 3.0 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc2nonc2c1 10.1021/jm990200p
10747201 36636 0 None 1288 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 618 10 3 8 2.3 COCC1=C(C(=O)OC)C(c2cc(F)c(F)cc2F)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C(=O)N1 10.1021/jm990202+
CHEMBL145072 36636 0 None 1288 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 618 10 3 8 2.3 COCC1=C(C(=O)OC)C(c2cc(F)c(F)cc2F)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C(=O)N1 10.1021/jm990202+
10699164 36782 0 None 151 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 552 7 2 7 3.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C#N)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145190 36782 0 None 151 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 552 7 2 7 3.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C#N)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
10745380 38540 0 None 177 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 557 8 2 7 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL146654 38540 0 None 177 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 557 8 2 7 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
10438280 101114 0 None 446 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 584 8 2 7 3.8 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990200p
CHEMBL298713 101114 0 None 446 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 584 8 2 7 3.8 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990200p
11802456 170383 0 None 316 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 584 9 3 7 2.9 CCC1=C(C(=O)OC)C(c2ccc(F)cc2F)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C(=O)N1 10.1021/jm990202+
CHEMBL445577 170383 0 None 316 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 584 9 3 7 2.9 CCC1=C(C(=O)OC)C(c2ccc(F)cc2F)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C(=O)N1 10.1021/jm990202+
10627090 34323 0 None 1288 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 581 9 2 7 3.8 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL142929 34323 0 None 1288 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 581 9 2 7 3.8 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
10721751 34392 0 None 1412 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 569 10 1 6 4.9 COC(=O)C1=C(C)NC(=O)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL142981 34392 0 None 1412 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 569 10 1 6 4.9 COC(=O)C1=C(C)NC(=O)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
10438280 101114 0 None 446 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 584 8 2 7 3.8 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL298713 101114 0 None 446 3 Human 10.0 pKi = 10 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 584 8 2 7 3.8 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
10578715 102189 0 None 144 3 Human 10.0 pKi = 10.0 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 556 10 1 7 4.2 COc1ccc(N2C(=O)c3ccc(C(=O)NCCCN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
CHEMBL304591 102189 0 None 144 3 Human 10.0 pKi = 10.0 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 556 10 1 7 4.2 COc1ccc(N2C(=O)c3ccc(C(=O)NCCCN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
10815593 205300 0 None 436 3 Human 9.9 pKi = 9.9 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 511 7 2 4 3.7 CN1C=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC1=O 10.1021/jm990612y
CHEMBL91616 205300 0 None 436 3 Human 9.9 pKi = 9.9 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 511 7 2 4 3.7 CN1C=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC1=O 10.1021/jm990612y
19085866 104925 0 None 117 3 Human 9.9 pKi = 9.9 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 455 6 0 7 2.9 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL311890 104925 0 None 117 3 Human 9.9 pKi = 9.9 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 455 6 0 7 2.9 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
49781893 17705 0 None 1 4 Bovine 9.9 pKi = 9.9 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 409 4 1 4 4.0 CC(C)C(=O)NCc1ccc2c(c1)C(N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259145 17705 0 None 1 4 Bovine 9.9 pKi = 9.9 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 409 4 1 4 4.0 CC(C)C(=O)NCc1ccc2c(c1)C(N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
10673657 204996 0 None 1071 3 Human 9.9 pKi = 9.9 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 525 7 2 4 4.3 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1021/jm990612y
CHEMBL89927 204996 0 None 1071 3 Human 9.9 pKi = 9.9 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 525 7 2 4 4.3 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1021/jm990612y
9985476 37038 0 None 912 3 Human 9.9 pKi = 9.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 570 8 3 7 2.5 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145394 37038 0 None 912 3 Human 9.9 pKi = 9.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 570 8 3 7 2.5 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
4209 3102 71 None -4 34 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
4893 3102 71 None -4 34 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
503 3102 71 None -4 34 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
5385 3102 71 None -4 34 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
CHEMBL2 3102 71 None -4 34 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
DB00457 3102 71 None -4 34 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970166j
129211 3680 75 None -7 16 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
2562 3680 75 None -7 16 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
488 3680 75 None -7 16 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
CHEMBL836 3680 75 None -7 16 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
DB00706 3680 75 None -7 16 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
10499343 204789 0 None 79 2 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 369 8 2 6 1.8 COc1ccccc1N1CCN(CCCNc2ncccc2C(N)=O)CC1 10.1021/jm970166j
CHEMBL88512 204789 0 None 79 2 Bovine 9.9 pKi = 9.9 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 369 8 2 6 1.8 COc1ccccc1N1CCN(CCCNc2ncccc2C(N)=O)CC1 10.1021/jm970166j
19085820 204080 0 None 1023 3 Human 9.9 pKi = 9.9 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 500 7 0 9 2.8 O=C1c2cc([N+](=O)[O-])ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL83226 204080 0 None 1023 3 Human 9.9 pKi = 9.9 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 500 7 0 9 2.8 O=C1c2cc([N+](=O)[O-])ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
129211 3680 75 None -1 16 Human 9.9 pKi = 9.9 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm9905918
2562 3680 75 None -1 16 Human 9.9 pKi = 9.9 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm9905918
488 3680 75 None -1 16 Human 9.9 pKi = 9.9 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm9905918
CHEMBL836 3680 75 None -1 16 Human 9.9 pKi = 9.9 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm9905918
DB00706 3680 75 None -1 16 Human 9.9 pKi = 9.9 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm9905918
10576661 205121 0 None 1230 3 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 479 7 3 4 3.5 N#Cc1ccccc1C1CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2017.03.025
CHEMBL90652 205121 0 None 1230 3 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 479 7 3 4 3.5 N#Cc1ccccc1C1CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2017.03.025
129211 3680 75 None -2 16 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2011.04.032
2562 3680 75 None -2 16 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2011.04.032
488 3680 75 None -2 16 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2011.04.032
CHEMBL836 3680 75 None -2 16 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2011.04.032
DB00706 3680 75 None -2 16 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2011.04.032
10576661 205121 0 None 1230 3 Human 9.9 pKi = 9.9 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 479 7 3 4 3.5 N#Cc1ccccc1C1CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
CHEMBL90652 205121 0 None 1230 3 Human 9.9 pKi = 9.9 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 479 7 3 4 3.5 N#Cc1ccccc1C1CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
10649481 205081 0 None 123 3 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 514 7 1 3 4.8 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N(C)C(=O)N1C 10.1016/j.ejmech.2017.03.025
CHEMBL90420 205081 0 None 123 3 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 514 7 1 3 4.8 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N(C)C(=O)N1C 10.1016/j.ejmech.2017.03.025
11638677 84152 0 None -5 6 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
ChEMBL 340 5 0 5 2.8 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2011.04.032
CHEMBL2153423 84152 0 None -5 6 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
ChEMBL 340 5 0 5 2.8 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2011.04.032
CHEMBL2220978 84152 0 None -5 6 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
ChEMBL 340 5 0 5 2.8 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2011.04.032
10840194 111323 0 None 245 3 Human 9.9 pKi = 9.9 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 541 9 3 5 3.6 COCC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
CHEMBL328763 111323 0 None 245 3 Human 9.9 pKi = 9.9 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 541 9 3 5 3.6 COCC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
10815240 205115 0 None 33 3 Human 9.9 pKi = 9.9 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 500 7 2 3 4.5 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N(C)C(=O)N1 10.1021/jm990612y
CHEMBL90606 205115 0 None 33 3 Human 9.9 pKi = 9.9 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 500 7 2 3 4.5 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N(C)C(=O)N1 10.1021/jm990612y
4209 3102 71 None -2 34 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting methodDisplacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting method
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.12.063
4893 3102 71 None -2 34 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting methodDisplacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting method
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.12.063
503 3102 71 None -2 34 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting methodDisplacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting method
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.12.063
5385 3102 71 None -2 34 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting methodDisplacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting method
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.12.063
CHEMBL2 3102 71 None -2 34 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting methodDisplacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting method
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.12.063
DB00457 3102 71 None -2 34 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting methodDisplacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting method
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.12.063
463 1373 17 None 5 13 Human 9.8 pKi = 9.8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960697s
6918097 1373 17 None 5 13 Human 9.8 pKi = 9.8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960697s
837 1373 17 None 5 13 Human 9.8 pKi = 9.8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960697s
CHEMBL2051956 1373 17 None 5 13 Human 9.8 pKi = 9.8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960697s
DB14068 1373 17 None 5 13 Human 9.8 pKi = 9.8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960697s
499 4002 15 None 1 15 Human 9.8 pKi = 9.8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm960697s
5685 4002 15 None 1 15 Human 9.8 pKi = 9.8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm960697s
CHEMBL25554 4002 15 None 1 15 Human 9.8 pKi = 9.8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm960697s
44298624 194024 0 None 63 2 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 458 8 1 6 2.5 Cc1c[nH]c(=O)n(CCCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
CHEMBL55695 194024 0 None 63 2 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 458 8 1 6 2.5 Cc1c[nH]c(=O)n(CCCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
487 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
60602 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
CHEMBL405355 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
DB09239 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
19085881 204044 0 None 478 3 Human 9.8 pKi = 9.8 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in CHO cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in CHO cells
ChEMBL 500 7 0 9 2.8 O=C1c2ccc([N+](=O)[O-])cc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL82877 204044 0 None 478 3 Human 9.8 pKi = 9.8 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in CHO cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in CHO cells
ChEMBL 500 7 0 9 2.8 O=C1c2ccc([N+](=O)[O-])cc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
10530491 102119 0 None 234 2 Human 9.8 pKi = 9.8 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 540 9 1 6 4.5 Cc1ccc(N2C(=O)c3ccc(C(=O)NCCCN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
CHEMBL304132 102119 0 None 234 2 Human 9.8 pKi = 9.8 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 540 9 1 6 4.5 Cc1ccc(N2C(=O)c3ccc(C(=O)NCCCN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
487 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Binding affinity towards recombinant human alpha-1A adrenergic receptorBinding affinity towards recombinant human alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm030480f
60602 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Binding affinity towards recombinant human alpha-1A adrenergic receptorBinding affinity towards recombinant human alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm030480f
CHEMBL405355 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Binding affinity towards recombinant human alpha-1A adrenergic receptorBinding affinity towards recombinant human alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm030480f
DB09239 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Binding affinity towards recombinant human alpha-1A adrenergic receptorBinding affinity towards recombinant human alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm030480f
487 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2004.11.032
60602 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2004.11.032
CHEMBL405355 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2004.11.032
DB09239 3564 17 None -1 12 Human 9.8 pKi = 9.8 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2004.11.032
137659584 158823 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 548 9 3 6 3.2 COCC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(C#N)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1016/j.ejmech.2017.03.025
CHEMBL4100620 158823 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 548 9 3 6 3.2 COCC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(C#N)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1016/j.ejmech.2017.03.025
499 4002 15 None 1 15 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/acs.jmedchem.9b01465
5685 4002 15 None 1 15 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/acs.jmedchem.9b01465
CHEMBL25554 4002 15 None 1 15 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/acs.jmedchem.9b01465
71508712 86626 0 None 40 5 Bovine 9.8 pKi = 9.8 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 389 3 0 5 4.4 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncn(C)n4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2326175 86626 0 None 40 5 Bovine 9.8 pKi = 9.8 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 389 3 0 5 4.4 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncn(C)n4)cc23)CC1 10.1016/j.bmc.2012.10.049
49782998 17720 0 None 1 6 Bovine 9.8 pKi = 9.8 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 409 4 1 4 4.0 CC(C)C(=O)NCc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259190 17720 0 None 1 6 Bovine 9.8 pKi = 9.8 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 409 4 1 4 4.0 CC(C)C(=O)NCc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
10696866 205196 0 None 6165 3 Human 9.8 pKi = 9.8 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 504 7 3 5 3.1 N#Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
CHEMBL91091 205196 0 None 6165 3 Human 9.8 pKi = 9.8 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 504 7 3 5 3.1 N#Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
10974101 116440 0 None 10 5 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)
ChEMBL 609 10 1 9 4.2 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C)CC3)cccc2c1=O 10.1021/jm030825u
CHEMBL338608 116440 0 None 10 5 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)
ChEMBL 609 10 1 9 4.2 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C)CC3)cccc2c1=O 10.1021/jm030825u
14423371 96992 1 None -1 7 Human 9.8 pKi = 9.8 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 441 11 1 8 3.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL27013 96992 1 None -1 7 Human 9.8 pKi = 9.8 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 441 11 1 8 3.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1021/jm9810654
4209 3102 71 None -4 34 Bovine 9.8 pKi = 9.8 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
4893 3102 71 None -4 34 Bovine 9.8 pKi = 9.8 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
503 3102 71 None -4 34 Bovine 9.8 pKi = 9.8 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
5385 3102 71 None -4 34 Bovine 9.8 pKi = 9.8 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
CHEMBL2 3102 71 None -4 34 Bovine 9.8 pKi = 9.8 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
DB00457 3102 71 None -4 34 Bovine 9.8 pKi = 9.8 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
9830741 206110 1 None 1 7 Human 9.8 pKi = 9.8 Binding
Binding affinity towards Alpha1A human adrenergic receptors, using [125I]-HEAT as radioligand.Binding affinity towards Alpha1A human adrenergic receptors, using [125I]-HEAT as radioligand.
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm000085e
CHEMBL96467 206110 1 None 1 7 Human 9.8 pKi = 9.8 Binding
Binding affinity towards Alpha1A human adrenergic receptors, using [125I]-HEAT as radioligand.Binding affinity towards Alpha1A human adrenergic receptors, using [125I]-HEAT as radioligand.
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm000085e
9830741 206110 1 None 1 7 Human 9.8 pKi = 9.8 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1016/j.bmcl.2004.11.032
CHEMBL96467 206110 1 None 1 7 Human 9.8 pKi = 9.8 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1016/j.bmcl.2004.11.032
9913449 105958 0 None 13 3 Human 9.8 pKi = 9.8 Binding
Compound was evaluated for its affinity for alpha 1a receptor in human prostate tissue preparationsCompound was evaluated for its affinity for alpha 1a receptor in human prostate tissue preparations
ChEMBL 489 6 0 7 3.5 O=C1c2cc(Cl)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL313990 105958 0 None 13 3 Human 9.8 pKi = 9.8 Binding
Compound was evaluated for its affinity for alpha 1a receptor in human prostate tissue preparationsCompound was evaluated for its affinity for alpha 1a receptor in human prostate tissue preparations
ChEMBL 489 6 0 7 3.5 O=C1c2cc(Cl)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
137637836 155528 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 509 9 3 6 3.1 COCC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)cc2)NCN1 10.1016/j.ejmech.2017.03.025
CHEMBL4062896 155528 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 509 9 3 6 3.1 COCC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)cc2)NCN1 10.1016/j.ejmech.2017.03.025
10719222 205704 0 None 141 3 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 472 7 3 3 3.7 O=C1NC=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1016/j.ejmech.2017.03.025
CHEMBL94167 205704 0 None 141 3 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 472 7 3 3 3.7 O=C1NC=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1016/j.ejmech.2017.03.025
49781232 17727 0 None -1 5 Bovine 9.8 pKi = 9.8 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 392 2 0 7 2.9 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4nnn(C)n4)cc32)CC1 10.1021/jm100652h
CHEMBL1259216 17727 0 None -1 5 Bovine 9.8 pKi = 9.8 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 392 2 0 7 2.9 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4nnn(C)n4)cc32)CC1 10.1021/jm100652h
10767607 106632 0 None 831 3 Human 9.8 pKi = 9.8 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 497 7 3 4 3.4 N#CC1(c2ccc(F)cc2)CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
CHEMBL316100 106632 0 None 831 3 Human 9.8 pKi = 9.8 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 497 7 3 4 3.4 N#CC1(c2ccc(F)cc2)CCN(CCCNC(=O)C2=CNC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
10791844 205418 0 None 512 3 Human 9.8 pKi = 9.8 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 511 7 3 4 4.0 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
CHEMBL92328 205418 0 None 512 3 Human 9.8 pKi = 9.8 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 511 7 3 4 4.0 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
10719222 205704 0 None 141 3 Human 9.8 pKi = 9.8 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 472 7 3 3 3.7 O=C1NC=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1021/jm990612y
CHEMBL94167 205704 0 None 141 3 Human 9.8 pKi = 9.8 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 472 7 3 3 3.7 O=C1NC=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1021/jm990612y
9830741 206110 1 None 1 7 Human 9.8 pKi = 9.8 Binding
Tested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assayTested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assay
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1016/s0960-894x(00)00524-2
CHEMBL96467 206110 1 None 1 7 Human 9.8 pKi = 9.8 Binding
Tested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assayTested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assay
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1016/s0960-894x(00)00524-2
10649481 205081 0 None 123 3 Human 9.7 pKi = 9.7 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 514 7 1 3 4.8 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N(C)C(=O)N1C 10.1021/jm990612y
CHEMBL90420 205081 0 None 123 3 Human 9.7 pKi = 9.7 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 514 7 1 3 4.8 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N(C)C(=O)N1C 10.1021/jm990612y
10839105 205082 0 None 660 3 Human 9.7 pKi = 9.7 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 500 7 2 3 4.5 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1021/jm990612y
CHEMBL90421 205082 0 None 660 3 Human 9.7 pKi = 9.7 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 500 7 2 3 4.5 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1021/jm990612y
CHEMBL179334 62958 0 None 977 6 Human 9.7 pKi = 9.7 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 608 10 2 7 6.4 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)[C@H]1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
10674564 202230 0 None 83 3 Human 9.7 pKi = 9.7 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 569 10 1 7 4.3 CC(C)Oc1ccccc1N1CCN(CCCNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(N(C)C)cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL69264 202230 0 None 83 3 Human 9.7 pKi = 9.7 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 569 10 1 7 4.3 CC(C)Oc1ccccc1N1CCN(CCCNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(N(C)C)cc2)C3=O)CC1 10.1021/jm9905918
10074286 203783 0 None 2 4 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 489 9 1 8 3.5 COc1ccccc1N1CCN(CCNc2c(C(=O)C(C)C)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL80730 203783 0 None 2 4 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 489 9 1 8 3.5 COc1ccccc1N1CCN(CCNc2c(C(=O)C(C)C)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL179334 62958 0 None 977 6 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 608 10 2 7 6.4 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)[C@H]1c1ccc([N+](=O)[O-])cc1 10.1016/j.bmcl.2004.11.032
137646446 157118 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 518 7 2 3 4.6 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)c(F)c3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1016/j.ejmech.2017.03.025
CHEMBL4081581 157118 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 518 7 2 3 4.6 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)c(F)c3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1016/j.ejmech.2017.03.025
9932698 17712 0 None 3 6 Bovine 9.7 pKi = 9.7 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 435 6 2 4 3.4 NCc1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm100652h
CHEMBL1259172 17712 0 None 3 6 Bovine 9.7 pKi = 9.7 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 435 6 2 4 3.4 NCc1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm100652h
10697623 106670 0 None 2398 3 Human 9.7 pKi = 9.7 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 536 7 2 5 3.6 CN1C=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC1=O 10.1021/jm990612y
CHEMBL316358 106670 0 None 2398 3 Human 9.7 pKi = 9.7 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 536 7 2 5 3.6 CN1C=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC1=O 10.1021/jm990612y
13911290 27945 0 None 1 6 Bovine 9.7 pKi = 9.7 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 386 5 1 7 1.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sccc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL13735 27945 0 None 1 6 Bovine 9.7 pKi = 9.7 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 386 5 1 7 1.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sccc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
129211 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.04.008
2562 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.04.008
488 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.04.008
CHEMBL836 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.04.008
DB00706 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.04.008
129211 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.04.098
2562 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.04.098
488 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.04.098
CHEMBL836 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.04.098
DB00706 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.04.098
10005161 203528 0 None 1 4 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 475 9 1 8 3.3 CCC(=O)c1c(-c2ccccc2)nn(C)c(=O)c1NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm0009336
CHEMBL78874 203528 0 None 1 4 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 475 9 1 8 3.3 CCC(=O)c1c(-c2ccccc2)nn(C)c(=O)c1NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm0009336
129211 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.11.068
2562 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.11.068
488 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.11.068
CHEMBL836 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.11.068
DB00706 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2007.11.068
49781450 17660 0 None 1 4 Bovine 9.7 pKi = 9.7 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 387 2 0 4 4.7 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4cccnc4)cc32)CC1 10.1021/jm100652h
CHEMBL1259023 17660 0 None 1 4 Bovine 9.7 pKi = 9.7 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 387 2 0 4 4.7 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4cccnc4)cc32)CC1 10.1021/jm100652h
9916549 121037 0 None 1 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of humanIn vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of human
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL358595 121037 0 None 1 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of humanIn vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of human
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
463 1373 17 None 5 13 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960697s
6918097 1373 17 None 5 13 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960697s
837 1373 17 None 5 13 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960697s
CHEMBL2051956 1373 17 None 5 13 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960697s
DB14068 1373 17 None 5 13 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960697s
4209 3102 71 None -2 34 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960697s
4893 3102 71 None -2 34 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960697s
503 3102 71 None -2 34 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960697s
5385 3102 71 None -2 34 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960697s
CHEMBL2 3102 71 None -2 34 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960697s
DB00457 3102 71 None -2 34 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960697s
129211 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm960697s
2562 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm960697s
488 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm960697s
CHEMBL836 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm960697s
DB00706 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm960697s
9872851 96625 1 None 79 3 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 571 10 1 7 4.6 COc1ccc(CCN2CCC(c3nc(COCC(F)(F)F)c(-c4ccc(F)cc4)o3)CC2)cc1S(N)(=O)=O 10.1021/jm960697s
CHEMBL267336 96625 1 None 79 3 Human 9.7 pKi = 9.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 571 10 1 7 4.6 COc1ccc(CCN2CCC(c3nc(COCC(F)(F)F)c(-c4ccc(F)cc4)o3)CC2)cc1S(N)(=O)=O 10.1021/jm960697s
9809007 171986 6 None 134 6 Human 9.7 pKi = 9.7 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm9902032
CHEMBL448620 171986 6 None 134 6 Human 9.7 pKi = 9.7 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm9902032
60820 4228 12 None -10 13 Rat 9.7 pKi = 9.7 Binding
Binding affinity towards alpha-1A adrenergic receptors using alpha-1A ligand WB-4101Binding affinity towards alpha-1A adrenergic receptors using alpha-1A ligand WB-4101
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1021/jm00034a003
CHEMBL10085 4228 12 None -10 13 Rat 9.7 pKi = 9.7 Binding
Binding affinity towards alpha-1A adrenergic receptors using alpha-1A ligand WB-4101Binding affinity towards alpha-1A adrenergic receptors using alpha-1A ligand WB-4101
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1021/jm00034a003
10674055 202506 0 None 50 3 Human 9.7 pKi = 9.7 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 542 9 2 7 3.9 CC(C)Oc1ccccc1N1CCN(CCCNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(O)cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL70892 202506 0 None 50 3 Human 9.7 pKi = 9.7 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 542 9 2 7 3.9 CC(C)Oc1ccccc1N1CCN(CCCNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(O)cc2)C3=O)CC1 10.1021/jm9905918
129211 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2004.11.032
2562 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2004.11.032
488 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2004.11.032
CHEMBL836 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2004.11.032
DB00706 3680 75 None -1 16 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.bmcl.2004.11.032
44390739 63996 1 None - 1 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 361 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1CSc2ccccc2O1 10.1016/j.bmcl.2004.11.032
CHEMBL181215 63996 1 None - 1 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 361 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1CSc2ccccc2O1 10.1016/j.bmcl.2004.11.032
10099811 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1016/j.bmcl.2004.11.032
CHEMBL356584 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1016/j.bmcl.2004.11.032
18738386 202331 0 None 125 3 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 413 7 0 5 4.0 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCC3=O)cs2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL69848 202331 0 None 125 3 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 413 7 0 5 4.0 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCC3=O)cs2)CC1 10.1016/s0960-894x(02)00347-5
11984570 92358 0 None 2 3 Human 9.7 pKi = 9.7 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 465 5 0 5 4.3 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4cccc(F)c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
CHEMBL243694 92358 0 None 2 3 Human 9.7 pKi = 9.7 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 465 5 0 5 4.3 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4cccc(F)c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
49781452 17669 0 None -1 4 Bovine 9.7 pKi = 9.7 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 388 2 0 5 4.1 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4cncnc4)cc32)CC1 10.1021/jm100652h
CHEMBL1259042 17669 0 None -1 4 Bovine 9.7 pKi = 9.7 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 388 2 0 5 4.1 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4cncnc4)cc32)CC1 10.1021/jm100652h
10722045 32581 0 None 436 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 584 8 2 7 3.8 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)cc1F 10.1021/jm990200p
CHEMBL141444 32581 0 None 436 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 584 8 2 7 3.8 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)cc1F 10.1021/jm990200p
10626726 33707 0 None 70 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 561 7 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3Cl)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL142398 33707 0 None 70 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 561 7 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3Cl)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
10371061 36456 0 None 1380 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)cc2F)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL144925 36456 0 None 1380 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)cc2F)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
10627155 36973 0 None 125 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 585 8 2 8 3.2 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(=O)OC)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145338 36973 0 None 125 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 585 8 2 8 3.2 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(=O)OC)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
10554140 118599 0 None 38 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 527 7 2 6 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL342731 118599 0 None 38 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 527 7 2 6 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
10099811 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
10099811 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990202+
CHEMBL356584 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL356584 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990202+
9916549 121037 0 None 1 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL358595 121037 0 None 1 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
10371061 36456 0 None 1380 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)cc2F)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL144925 36456 0 None 1380 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)cc2F)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
10745870 36473 0 None 3090 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 584 9 2 7 2.8 COC(=O)C1=C(C)NC(=O)N(CC(=O)NCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL144938 36473 0 None 3090 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 584 9 2 7 2.8 COC(=O)C1=C(C)NC(=O)N(CC(=O)NCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
10720893 37121 0 None 181 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 526 7 2 5 4.5 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL145459 37121 0 None 181 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 526 7 2 5 4.5 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
10675068 95990 0 None 758 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 599 9 2 7 3.9 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C#N)(c3cccc(F)c3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL262217 95990 0 None 758 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 599 9 2 7 3.9 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C#N)(c3cccc(F)c3)CC2)C(=O)N1 10.1021/jm990201h
10508330 118276 0 None 99 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 638 8 2 5 5.9 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)(c3ccc(F)cc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL342126 118276 0 None 99 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 638 8 2 5 5.9 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)(c3ccc(F)cc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
10099811 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL356584 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
10507500 121167 0 None 1258 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 582 6 2 7 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CC2)OC(=O)Cc2ccccc23)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL358785 121167 0 None 1258 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 582 6 2 7 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CC2)OC(=O)Cc2ccccc23)C1c1ccc(F)c(F)c1 10.1021/jm990201h
10555024 121362 0 None 2454 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 568 6 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CC2)OCCc2ccccc23)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL359012 121362 0 None 2454 3 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 568 6 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CC2)OCCc2ccccc23)C1c1ccc(F)c(F)c1 10.1021/jm990201h
10099811 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity radioligandIn vitro binding affinity radioligand
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL356584 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity radioligandIn vitro binding affinity radioligand
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
4013695 101532 19 None 1 5 Rat 9.7 pKi = 9.7 Binding
Binding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranesBinding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranes
ChEMBL 419 5 2 6 2.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1021/jm00110a014
CHEMBL301707 101532 19 None 1 5 Rat 9.7 pKi = 9.7 Binding
Binding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranesBinding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranes
ChEMBL 419 5 2 6 2.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1021/jm00110a014
10099811 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of humanIn vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of human
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL356584 120497 1 None 676 4 Human 9.7 pKi = 9.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of humanIn vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of human
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
10527469 155712 1 None 1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
CHEMBL40650 155712 1 None 1 16 Human 9.7 pKi = 9.7 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
10916771 104722 0 None 9 4 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 419 7 1 7 2.7 COc1ccccc1N1CCN(CCNc2cc(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL311479 104722 0 None 9 4 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 419 7 1 7 2.7 COc1ccccc1N1CCN(CCNc2cc(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
10527469 155712 1 None 1 16 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1016/j.bmcl.2004.11.032
CHEMBL40650 155712 1 None 1 16 Human 9.7 pKi = 9.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1016/j.bmcl.2004.11.032
9828476 205187 0 None 58 6 Human 9.6 pKi = 9.6 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 532 9 2 7 5.2 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL91022 205187 0 None 58 6 Human 9.6 pKi = 9.6 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 532 9 2 7 5.2 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
9828476 84844 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 532 9 2 7 4.4 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL2260360 84844 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 532 9 2 7 4.4 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
9830741 206110 1 None 1 7 Human 9.6 pKi = 9.6 Binding
Binding affinity towards Alpha1A dog adrenergic receptors, using [125I]HEAT as radioligand.Binding affinity towards Alpha1A dog adrenergic receptors, using [125I]HEAT as radioligand.
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm000085e
CHEMBL96467 206110 1 None 1 7 Human 9.6 pKi = 9.6 Binding
Binding affinity towards Alpha1A dog adrenergic receptors, using [125I]HEAT as radioligand.Binding affinity towards Alpha1A dog adrenergic receptors, using [125I]HEAT as radioligand.
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm000085e
10626910 202078 0 None 537 2 Human 9.6 pKi = 9.6 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 572 10 2 8 3.2 COc1ccc(N2C(=O)c3ccc(C(=O)NC[C@H](O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
CHEMBL68203 202078 0 None 537 2 Human 9.6 pKi = 9.6 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 572 10 2 8 3.2 COc1ccc(N2C(=O)c3ccc(C(=O)NC[C@H](O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
9826801 107438 0 None 4 13 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL319352 107438 0 None 4 13 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
135418497 62695 0 None 1 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(C[C@H]2CN=C3c4ccccc4NC(=O)N32)CC1 10.1021/jm970159v
CHEMBL1788222 62695 0 None 1 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(C[C@H]2CN=C3c4ccccc4NC(=O)N32)CC1 10.1021/jm970159v
4209 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2006.05.002
4893 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2006.05.002
503 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2006.05.002
5385 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2006.05.002
CHEMBL2 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2006.05.002
DB00457 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2006.05.002
9826801 107438 0 None 4 13 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1016/j.bmc.2012.10.049
CHEMBL319352 107438 0 None 4 13 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1016/j.bmc.2012.10.049
9826801 107438 0 None 4 13 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm100652h
CHEMBL319352 107438 0 None 4 13 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm100652h
9809007 171986 6 None 134 6 Human 9.6 pKi = 9.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm960697s
CHEMBL448620 171986 6 None 134 6 Human 9.6 pKi = 9.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm960697s
10369288 205517 0 None 169 3 Human 9.6 pKi = 9.6 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 516 9 3 4 3.7 COCC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
CHEMBL92951 205517 0 None 169 3 Human 9.6 pKi = 9.6 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 516 9 3 4 3.7 COCC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
10456471 100054 0 None 1 5 Rat 9.6 pKi = 9.6 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 451 6 1 7 2.4 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
CHEMBL291303 100054 0 None 1 5 Rat 9.6 pKi = 9.6 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 451 6 1 7 2.4 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
9913449 105958 0 None 13 3 Human 9.6 pKi = 9.6 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparations
ChEMBL 489 6 0 7 3.5 O=C1c2cc(Cl)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL313990 105958 0 None 13 3 Human 9.6 pKi = 9.6 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparations
ChEMBL 489 6 0 7 3.5 O=C1c2cc(Cl)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
44300165 101368 0 None 66 3 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.5 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@H](N3CCC(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL300540 101368 0 None 66 3 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.5 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@H](N3CCC(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
10369288 205517 0 None 169 3 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 516 9 3 4 3.7 COCC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1016/j.ejmech.2017.03.025
CHEMBL92951 205517 0 None 169 3 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 516 9 3 4 3.7 COCC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1016/j.ejmech.2017.03.025
49781236 17646 0 None -1 4 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 390 2 0 5 4.1 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4cnn(C)c4)cc32)CC1 10.1021/jm100652h
CHEMBL1258987 17646 0 None -1 4 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 390 2 0 5 4.1 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4cnn(C)c4)cc32)CC1 10.1021/jm100652h
49781449 17654 0 None 2 4 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 387 2 0 4 4.7 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ccccn4)cc32)CC1 10.1021/jm100652h
CHEMBL1259006 17654 0 None 2 4 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 387 2 0 4 4.7 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ccccn4)cc32)CC1 10.1021/jm100652h
9847196 29952 0 None 1 5 Bovine 9.6 pKi = 9.6 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(-c4ccccc4)cc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL13903 29952 0 None 1 5 Bovine 9.6 pKi = 9.6 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(-c4ccccc4)cc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
10606670 197404 0 None 13 3 Rat 9.6 pKi = 9.6 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 465 6 0 8 2.4 COc1cc2c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)n(C)c2cc1OC 10.1021/jm000541z
CHEMBL58862 197404 0 None 13 3 Rat 9.6 pKi = 9.6 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 465 6 0 8 2.4 COc1cc2c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)n(C)c2cc1OC 10.1021/jm000541z
3567002 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 10.1016/j.bmcl.2004.11.032
7381 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 10.1016/j.bmcl.2004.11.032
CHEMBL56331 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 10.1016/j.bmcl.2004.11.032
10624993 111183 0 None 630 3 Human 9.6 pKi = 9.6 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 493 7 3 4 3.9 CC1=C(C(=O)NCCCN2CCC(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
CHEMBL328658 111183 0 None 630 3 Human 9.6 pKi = 9.6 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 493 7 3 4 3.9 CC1=C(C(=O)NCCCN2CCC(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
11626704 72094 0 None -5 4 Human 9.6 pKi = 9.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 457 13 1 6 5.0 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc(Cl)c1 10.1007/s00044-010-9379-1
CHEMBL198860 72094 0 None -5 4 Human 9.6 pKi = 9.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 457 13 1 6 5.0 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc(Cl)c1 10.1007/s00044-010-9379-1
44289437 169285 0 None -1 7 Human 9.6 pKi = 9.6 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 431 9 1 5 4.7 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2C1=O 10.1021/jm011066n
CHEMBL44403 169285 0 None -1 7 Human 9.6 pKi = 9.6 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 431 9 1 5 4.7 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2C1=O 10.1021/jm011066n
11626704 72094 0 None -5 4 Human 9.6 pKi = 9.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 457 13 1 6 5.0 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc(Cl)c1 10.1007/s00044-010-9379-1
CHEMBL198860 72094 0 None -5 4 Human 9.6 pKi = 9.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 457 13 1 6 5.0 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc(Cl)c1 10.1007/s00044-010-9379-1
11626704 72094 0 None -5 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 457 13 1 6 5.0 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc(Cl)c1 10.1021/jm0580398
CHEMBL198860 72094 0 None -5 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 457 13 1 6 5.0 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc(Cl)c1 10.1021/jm0580398
11583392 72554 1 None -7 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 457 13 1 6 5.0 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccc(Cl)cc1 10.1021/jm0580398
CHEMBL200446 72554 1 None -7 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 457 13 1 6 5.0 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccc(Cl)cc1 10.1021/jm0580398
3567002 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 10.1016/s0960-894x(03)00305-6
7381 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 10.1016/s0960-894x(03)00305-6
CHEMBL56331 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 10.1016/s0960-894x(03)00305-6
44298650 162593 0 None 100 3 Human 9.6 pKi = 9.6 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 448 7 1 6 2.0 O=c1[nH]cc(F)c(=O)n1CCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
CHEMBL417954 162593 0 None 100 3 Human 9.6 pKi = 9.6 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 448 7 1 6 2.0 O=c1[nH]cc(F)c(=O)n1CCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
4431 2679 18 None 1 12 Human 9.6 pKi = 9.6 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.bmcl.2006.12.111
73 2679 18 None 1 12 Human 9.6 pKi = 9.6 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.bmcl.2006.12.111
CHEMBL8618 2679 18 None 1 12 Human 9.6 pKi = 9.6 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.bmcl.2006.12.111
132891 5225 12 None 2 5 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(CC2CN=C3c4ccccc4NC(=O)N32)CC1 10.1021/jm970159v
CHEMBL106737 5225 12 None 2 5 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(CC2CN=C3c4ccccc4NC(=O)N32)CC1 10.1021/jm970159v
49781235 17733 0 None -1 4 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 390 2 0 5 4.1 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ccn(C)n4)cc32)CC1 10.1021/jm100652h
CHEMBL1259232 17733 0 None -1 4 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 390 2 0 5 4.1 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ccn(C)n4)cc32)CC1 10.1021/jm100652h
9985476 37038 0 None 912 3 Human 9.6 pKi = 9.6 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 570 8 3 7 2.5 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145394 37038 0 None 912 3 Human 9.6 pKi = 9.6 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 570 8 3 7 2.5 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
52949448 16467 0 None 3 4 Human 9.6 pKi = 9.6 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 430 6 0 5 4.1 COc1ccccc1N1CCN(CC2OCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242352 16467 0 None 3 4 Human 9.6 pKi = 9.6 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 430 6 0 5 4.1 COc1ccccc1N1CCN(CC2OCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
57393527 71199 0 None 3 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 430 6 0 5 4.1 COc1ccccc1N1CCN(CC2COC(c3ccccc3)(c3ccccc3)O2)CC1 10.1021/jm200421e
CHEMBL1946777 71199 0 None 3 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 430 6 0 5 4.1 COc1ccccc1N1CCN(CC2COC(c3ccccc3)(c3ccccc3)O2)CC1 10.1021/jm200421e
CHEMBL1963046 71199 0 None 3 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 430 6 0 5 4.1 COc1ccccc1N1CCN(CC2COC(c3ccccc3)(c3ccccc3)O2)CC1 10.1021/jm200421e
4013695 101532 19 None -1 5 Human 9.6 pKi = 9.6 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 419 5 2 6 2.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL301707 101532 19 None -1 5 Human 9.6 pKi = 9.6 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 419 5 2 6 2.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1016/j.ejmech.2011.03.054
4013695 101532 19 None -1 5 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 419 5 2 6 2.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL301707 101532 19 None -1 5 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 419 5 2 6 2.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1016/j.ejmech.2011.03.054
4209 3102 71 None -2 34 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
4893 3102 71 None -2 34 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
503 3102 71 None -2 34 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
5385 3102 71 None -2 34 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
CHEMBL2 3102 71 None -2 34 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
DB00457 3102 71 None -2 34 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
19085829 204121 0 None 186 3 Human 9.6 pKi = 9.6 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in HEK cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in HEK cells
ChEMBL 473 6 0 7 3.0 O=C1c2cc(F)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL83592 204121 0 None 186 3 Human 9.6 pKi = 9.6 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in HEK cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in HEK cells
ChEMBL 473 6 0 7 3.0 O=C1c2cc(F)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
10647175 130920 0 None 2 3 Rat 9.6 pKi = 9.6 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 449 5 1 7 2.1 COC(=O)c1ccc2c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)[nH]c2c1 10.1021/jm000541z
CHEMBL369154 130920 0 None 2 3 Rat 9.6 pKi = 9.6 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 449 5 1 7 2.1 COC(=O)c1ccc2c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)[nH]c2c1 10.1021/jm000541z
10478121 170225 0 None 1 5 Rat 9.6 pKi = 9.6 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 435 6 0 7 3.1 COc1cc2ncn(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
CHEMBL445325 170225 0 None 1 5 Rat 9.6 pKi = 9.6 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 435 6 0 7 3.1 COc1cc2ncn(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
10527469 155712 1 None -1 16 Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL40650 155712 1 None -1 16 Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm990567u
490 190 5 None -2 12 Bovine 9.6 pKi = 9.6 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
9890547 190 5 None -2 12 Bovine 9.6 pKi = 9.6 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
CHEMBL268758 190 5 None -2 12 Bovine 9.6 pKi = 9.6 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
18187410 104406 0 None 10 3 Human 9.6 pKi = 9.6 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 418 6 1 6 3.5 O=C1c2ccccc2C(=O)N1CCCCN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL311247 104406 0 None 10 3 Human 9.6 pKi = 9.6 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 418 6 1 6 3.5 O=C1c2ccccc2C(=O)N1CCCCN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
11092254 203745 0 None 1 4 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 495 8 1 8 3.5 COc1ccc(Cl)cc1N1CCN(CCNc2c(C(C)=O)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL80458 203745 0 None 1 4 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 495 8 1 8 3.5 COc1ccc(Cl)cc1N1CCN(CCNc2c(C(C)=O)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
4209 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
4893 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
503 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
5385 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
CHEMBL2 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
DB00457 3102 71 None -3 34 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.01.025
9843389 86615 0 None 245 2 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 390 3 0 6 3.8 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4nnn(C)n4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2325935 86615 0 None 245 2 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 390 3 0 6 3.8 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4nnn(C)n4)cc23)CC1 10.1016/j.bmc.2012.10.049
12765746 101797 3 None -3 11 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
CHEMBL303313 101797 3 None -3 11 Bovine 9.6 pKi = 9.6 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
10698013 99961 0 None 2 3 Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 518 5 1 7 3.3 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(C(=O)N(C)C)cc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL290519 99961 0 None 2 3 Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 518 5 1 7 3.3 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(C(=O)N(C)C)cc54)c3=O)C[C@@H]21 10.1021/jm990567u
4013695 101532 19 None -1 5 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 419 5 2 6 2.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
CHEMBL301707 101532 19 None -1 5 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 419 5 2 6 2.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
11430491 62657 0 None 1 6 Human 9.5 pKi = 9.5 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 435 5 1 9 2.4 COc1cc2nc(N3CCN(C(=O)CC4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
CHEMBL178673 62657 0 None 1 6 Human 9.5 pKi = 9.5 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 435 5 1 9 2.4 COc1cc2nc(N3CCN(C(=O)CC4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
10792897 167340 0 None 186 2 Human 9.5 pKi = 9.5 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 556 9 2 7 3.5 Cc1ccc(N2C(=O)c3ccc(C(=O)NC[C@H](O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
CHEMBL431362 167340 0 None 186 2 Human 9.5 pKi = 9.5 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 556 9 2 7 3.5 Cc1ccc(N2C(=O)c3ccc(C(=O)NC[C@H](O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
10673690 100023 0 None -1 3 Rat 9.5 pKi = 9.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 490 5 2 7 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cc(C(N)=O)ccc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL291073 100023 0 None -1 3 Rat 9.5 pKi = 9.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 490 5 2 7 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cc(C(N)=O)ccc54)c3=O)C[C@@H]21 10.1021/jm990567u
10721171 37462 0 None 398 3 Human 9.5 pKi = 9.5 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 539 10 0 6 6.2 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3OC)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL145770 37462 0 None 398 3 Human 9.5 pKi = 9.5 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 539 10 0 6 6.2 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3OC)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
11134424 104239 0 None -1 4 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 465 7 1 7 3.5 CC(=O)c1c(-c2ccccc2)nn(C)c(=O)c1NCCN1CCN(c2ccccc2Cl)CC1 10.1021/jm0009336
CHEMBL310599 104239 0 None -1 4 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 465 7 1 7 3.5 CC(=O)c1c(-c2ccccc2)nn(C)c(=O)c1NCCN1CCN(c2ccccc2Cl)CC1 10.1021/jm0009336
4209 3102 71 None -3 34 Rat 9.5 pKi = 9.5 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
4893 3102 71 None -3 34 Rat 9.5 pKi = 9.5 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
503 3102 71 None -3 34 Rat 9.5 pKi = 9.5 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
5385 3102 71 None -3 34 Rat 9.5 pKi = 9.5 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
CHEMBL2 3102 71 None -3 34 Rat 9.5 pKi = 9.5 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
DB00457 3102 71 None -3 34 Rat 9.5 pKi = 9.5 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
10836245 102261 0 None 10 5 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 427 7 0 5 4.4 CC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)s2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL305029 102261 0 None 10 5 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 427 7 0 5 4.4 CC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)s2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL552830 102261 0 None 10 5 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 427 7 0 5 4.4 CC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)s2)CC1 10.1016/s0960-894x(02)00347-5
122179430 120914 0 None -3 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 599 8 1 13 2.7 CCN(CC)c1ccc2cc(-n3cc(C(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)nn3)c(=O)oc2c1 10.1021/ml5004298
CHEMBL3582270 120914 0 None -3 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 599 8 1 13 2.7 CCN(CC)c1ccc2cc(-n3cc(C(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)nn3)c(=O)oc2c1 10.1021/ml5004298
44447061 153822 0 None -1 4 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 474 5 1 5 4.3 O=C(NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21)C(F)(F)F 10.1016/j.bmcl.2007.11.106
CHEMBL398711 153822 0 None -1 4 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 474 5 1 5 4.3 O=C(NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21)C(F)(F)F 10.1016/j.bmcl.2007.11.106
10626493 205645 0 None 239 3 Human 9.5 pKi = 9.5 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 550 7 1 5 4.0 CN1C=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)N(C)C1=O 10.1021/jm990612y
CHEMBL93843 205645 0 None 239 3 Human 9.5 pKi = 9.5 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 550 7 1 5 4.0 CN1C=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)N(C)C1=O 10.1021/jm990612y
10770007 34356 0 None 50 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 607 10 2 9 3.8 CCOC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
CHEMBL142957 34356 0 None 50 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 607 10 2 9 3.8 CCOC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
10768829 118866 0 None 32 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 541 7 2 6 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL344525 118866 0 None 32 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 541 7 2 6 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
10722099 120568 0 None 190 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 588 8 3 7 2.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1cc(F)c(F)c(F)c1 10.1021/jm990202+
CHEMBL357172 120568 0 None 190 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 588 8 3 7 2.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1cc(F)c(F)c(F)c1 10.1021/jm990202+
10721476 36753 0 None 691 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 554 6 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CC2)OCc2ccccc23)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL145170 36753 0 None 691 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 554 6 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CC2)OCc2ccccc23)C1c1ccc(F)c(F)c1 10.1021/jm990201h
10769621 118475 0 None 2290 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 584 8 2 7 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(OC(C)=O)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL342543 118475 0 None 2290 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 584 8 2 7 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(OC(C)=O)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
11712470 71646 0 None -5 4 Human 9.5 pKi = 9.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 468 14 1 8 4.2 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc([N+](=O)[O-])c1 10.1007/s00044-010-9379-1
CHEMBL197442 71646 0 None -5 4 Human 9.5 pKi = 9.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 468 14 1 8 4.2 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc([N+](=O)[O-])c1 10.1007/s00044-010-9379-1
11712470 71646 0 None -5 4 Human 9.5 pKi = 9.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 468 14 1 8 4.2 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc([N+](=O)[O-])c1 10.1007/s00044-010-9379-1
CHEMBL197442 71646 0 None -5 4 Human 9.5 pKi = 9.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 468 14 1 8 4.2 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc([N+](=O)[O-])c1 10.1007/s00044-010-9379-1
11712470 71646 0 None -5 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 468 14 1 8 4.2 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc([N+](=O)[O-])c1 10.1021/jm0580398
CHEMBL197442 71646 0 None -5 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 468 14 1 8 4.2 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc([N+](=O)[O-])c1 10.1021/jm0580398
44298626 193796 0 None 25 3 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 427 7 1 7 1.4 Cc1n[nH]c(=O)n(CCCN2CCN(c3ccccc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
CHEMBL55290 193796 0 None 25 3 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 427 7 1 7 1.4 Cc1n[nH]c(=O)n(CCCN2CCN(c3ccccc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
9960497 99997 0 None 154 6 Human 9.5 pKi = 9.5 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.9 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)OCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
CHEMBL290860 99997 0 None 154 6 Human 9.5 pKi = 9.5 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.9 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)OCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
3416533 193309 6 None 4 2 Rat 9.5 pKi = 9.5 Binding
Binding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranesBinding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranes
ChEMBL 447 5 0 8 2.0 COc1ccccc1N1CCN(CCn2c(=O)c3c(c4ccccc4n3C)n(C)c2=O)CC1 10.1021/jm00110a014
CHEMBL54716 193309 6 None 4 2 Rat 9.5 pKi = 9.5 Binding
Binding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranesBinding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranes
ChEMBL 447 5 0 8 2.0 COc1ccccc1N1CCN(CCn2c(=O)c3c(c4ccccc4n3C)n(C)c2=O)CC1 10.1021/jm00110a014
10961351 162937 0 None 1 4 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 449 7 1 7 3.0 CC(=O)c1c(-c2ccccc2)nn(C)c(=O)c1NCCN1CCN(c2ccccc2F)CC1 10.1021/jm0009336
CHEMBL420205 162937 0 None 1 4 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 449 7 1 7 3.0 CC(=O)c1c(-c2ccccc2)nn(C)c(=O)c1NCCN1CCN(c2ccccc2F)CC1 10.1021/jm0009336
71508640 86605 0 None 46 2 Bovine 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 388 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ccnn4C)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2325926 86605 0 None 46 2 Bovine 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 388 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ccnn4C)cc23)CC1 10.1016/j.bmc.2012.10.049
10097792 118071 0 None -1 8 Human 9.5 pKi = 9.5 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 508 13 1 8 4.1 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CN(C)C)c3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL341665 118071 0 None -1 8 Human 9.5 pKi = 9.5 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 508 13 1 8 4.1 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CN(C)C)c3)nc(N)c2cc1OC 10.1021/jm9810654
90645597 111984 0 None -2 3 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 654 12 3 9 4.2 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCC(=O)NCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298750 111984 0 None -2 3 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 654 12 3 9 4.2 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCC(=O)NCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
10841070 37431 0 None 2 4 Human 9.5 pKi = 9.5 Binding
Binding affinity against isolated human prostate using [3H]- prazosin.Binding affinity against isolated human prostate using [3H]- prazosin.
ChEMBL 585 10 0 5 7.4 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL145746 37431 0 None 2 4 Human 9.5 pKi = 9.5 Binding
Binding affinity against isolated human prostate using [3H]- prazosin.Binding affinity against isolated human prostate using [3H]- prazosin.
ChEMBL 585 10 0 5 7.4 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10504673 200977 0 None -1 3 Rat 9.5 pKi = 9.5 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 473 5 1 6 4.1 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(-c5ccccc5)csc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL61483 200977 0 None -1 3 Rat 9.5 pKi = 9.5 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 473 5 1 6 4.1 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(-c5ccccc5)csc4c3=O)C[C@@H]21 10.1021/jm000541z
9894665 103323 1 None 30 8 Human 9.5 pKi = 9.5 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 585 10 2 8 3.3 CC(C)Oc1ccccc1N1CCN(C[C@@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(N(C)C)cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL309106 103323 1 None 30 8 Human 9.5 pKi = 9.5 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 585 10 2 8 3.3 CC(C)Oc1ccccc1N1CCN(C[C@@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(N(C)C)cc2)C3=O)CC1 10.1021/jm9905918
10474042 169675 0 None -1 6 Human 9.5 pKi = 9.5 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 365 6 0 4 4.1 COc1cccc2c1CCCC2CCCN1CCN(c2ccccn2)CC1 10.1021/jm010866v
CHEMBL444590 169675 0 None -1 6 Human 9.5 pKi = 9.5 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 365 6 0 4 4.1 COc1cccc2c1CCCC2CCCN1CCN(c2ccccn2)CC1 10.1021/jm010866v
9955302 99691 0 None -1 3 Rat 9.5 pKi = 9.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccncc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL287965 99691 0 None -1 3 Rat 9.5 pKi = 9.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccncc54)c3=O)C[C@@H]21 10.1021/jm990567u
50905381 56041 0 None -1 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 422 11 2 6 2.7 COc1ccc(C[C@@H](C)NCCOc2ccccc2OC(C)C)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
CHEMBL1630938 56041 0 None -1 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 422 11 2 6 2.7 COc1ccc(C[C@@H](C)NCCOc2ccccc2OC(C)C)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
49782792 17714 0 None 1 6 Bovine 9.5 pKi = 9.5 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 381 3 1 4 3.3 CC(=O)NCc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259174 17714 0 None 1 6 Bovine 9.5 pKi = 9.5 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 381 3 1 4 3.3 CC(=O)NCc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
148842 3871 21 None 8 5 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm030825u
496 3871 21 None 8 5 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm030825u
CHEMBL278865 3871 21 None 8 5 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm030825u
13911290 27945 0 None -1 6 Human 9.5 pKi = 9.5 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 386 5 1 7 1.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sccc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL13735 27945 0 None -1 6 Human 9.5 pKi = 9.5 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 386 5 1 7 1.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sccc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
9809007 171986 6 None 134 6 Human 9.5 pKi = 9.5 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL448620 171986 6 None 134 6 Human 9.5 pKi = 9.5 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
9809007 171986 6 None 134 6 Human 9.5 pKi = 9.5 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL448620 171986 6 None 134 6 Human 9.5 pKi = 9.5 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
50905585 56042 0 None -1 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 470 12 2 6 3.5 COc1ccc(C[C@@H](C)NCCOc2ccccc2OCc2ccccc2)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
CHEMBL1630939 56042 0 None -1 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 470 12 2 6 3.5 COc1ccc(C[C@@H](C)NCCOc2ccccc2OCc2ccccc2)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
491 191 4 None -4 12 Bovine 9.5 pKi = 9.5 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
9891167 191 4 None -4 12 Bovine 9.5 pKi = 9.5 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
CHEMBL13856 191 4 None -4 12 Bovine 9.5 pKi = 9.5 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
9809007 171986 6 None 134 6 Human 9.5 pKi = 9.5 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
CHEMBL448620 171986 6 None 134 6 Human 9.5 pKi = 9.5 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
499 4002 15 None -1 15 Bovine 9.5 pKi = 9.5 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
5685 4002 15 None -1 15 Bovine 9.5 pKi = 9.5 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
CHEMBL25554 4002 15 None -1 15 Bovine 9.5 pKi = 9.5 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
9809007 171986 6 None 134 6 Human 9.5 pKi = 9.5 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
CHEMBL448620 171986 6 None 134 6 Human 9.5 pKi = 9.5 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
10599007 202800 0 None -1 8 Bovine 9.5 pKi = 9.5 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNC[C@@H]1Oc2ccccc2O[C@H]1c1ccc(C)cc1 10.1021/jm960069a
CHEMBL72657 202800 0 None -1 8 Bovine 9.5 pKi = 9.5 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNC[C@@H]1Oc2ccccc2O[C@H]1c1ccc(C)cc1 10.1021/jm960069a
10599007 202800 0 None 1 8 Human 9.5 pKi = 9.5 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNC[C@@H]1Oc2ccccc2O[C@H]1c1ccc(C)cc1 10.1016/j.bmcl.2004.11.032
CHEMBL72657 202800 0 None 1 8 Human 9.5 pKi = 9.5 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNC[C@@H]1Oc2ccccc2O[C@H]1c1ccc(C)cc1 10.1016/j.bmcl.2004.11.032
10917953 206239 0 None 1 11 Bovine 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL97242 206239 0 None 1 11 Bovine 9.5 pKi = 9.5 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
10743310 168655 0 None 3 3 Rat 9.5 pKi = 9.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 479 5 1 9 2.4 COc1cnc2sc3c(=O)n(CCN4C[C@@H]5CCc6c(OC)cccc6[C@@H]5C4)c(=O)[nH]c3c2n1 10.1021/jm990567u
CHEMBL441032 168655 0 None 3 3 Rat 9.5 pKi = 9.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 479 5 1 9 2.4 COc1cnc2sc3c(=O)n(CCN4C[C@@H]5CCc6c(OC)cccc6[C@@H]5C4)c(=O)[nH]c3c2n1 10.1021/jm990567u
9830741 206110 1 None -1 7 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards Alpha1A rat adrenergic receptors, using [125I]HEAT as radioligand.Binding affinity towards Alpha1A rat adrenergic receptors, using [125I]HEAT as radioligand.
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm000085e
CHEMBL96467 206110 1 None -1 7 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards Alpha1A rat adrenergic receptors, using [125I]HEAT as radioligand.Binding affinity towards Alpha1A rat adrenergic receptors, using [125I]HEAT as radioligand.
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm000085e
44275505 96340 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards recombinant human alpha-1A adrenergic receptorBinding affinity towards recombinant human alpha-1A adrenergic receptor
ChEMBL 556 10 2 7 2.6 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)C(C(=O)NCCCN2CCC(c3ccccn3)CC2)C(=O)N1 10.1021/jm030480f
CHEMBL265001 96340 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards recombinant human alpha-1A adrenergic receptorBinding affinity towards recombinant human alpha-1A adrenergic receptor
ChEMBL 556 10 2 7 2.6 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)C(C(=O)NCCCN2CCC(c3ccccn3)CC2)C(=O)N1 10.1021/jm030480f
9874983 65121 12 None - 1 Human 9.4 pKi = 9.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 557 9 2 7 3.5 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(c3ccccn3)CC2)C(=O)N1 10.1016/j.bmcl.2004.11.032
CHEMBL182998 65121 12 None - 1 Human 9.4 pKi = 9.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 557 9 2 7 3.5 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(c3ccccn3)CC2)C(=O)N1 10.1016/j.bmcl.2004.11.032
499 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
5685 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
CHEMBL25554 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
9830292 167615 0 None 562 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.3 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@@H](N3CCC(C#N)(c4ccccc4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL433284 167615 0 None 562 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.3 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@@H](N3CCC(C#N)(c4ccccc4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
2435 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
60149 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
98 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
CHEMBL12713 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
DB06144 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
2435 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmc.2012.10.049
60149 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmc.2012.10.049
98 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmc.2012.10.049
CHEMBL12713 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmc.2012.10.049
DB06144 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmc.2012.10.049
2435 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm100652h
60149 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm100652h
98 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm100652h
CHEMBL12713 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm100652h
DB06144 3520 78 None -3 49 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm100652h
9847845 28226 0 None -1 6 Bovine 9.4 pKi = 9.4 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(C)c(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL13754 28226 0 None -1 6 Bovine 9.4 pKi = 9.4 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(C)c(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
487 3564 17 None 1 12 Bovine 9.4 pKi = 9.4 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960069a
60602 3564 17 None 1 12 Bovine 9.4 pKi = 9.4 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960069a
CHEMBL405355 3564 17 None 1 12 Bovine 9.4 pKi = 9.4 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960069a
DB09239 3564 17 None 1 12 Bovine 9.4 pKi = 9.4 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960069a
44300129 166863 0 None 912 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 583 7 2 7 4.0 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@@H](N3CCC(c4ccccn4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL429697 166863 0 None 912 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 583 7 2 7 4.0 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@@H](N3CCC(c4ccccn4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
10838523 100717 0 None 1 3 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 482 4 1 7 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(Cl)nc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL295741 100717 0 None 1 3 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 482 4 1 7 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(Cl)nc54)c3=O)C[C@@H]21 10.1021/jm990567u
134149596 147921 0 None 4 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 368 6 0 5 3.6 CC(C)Oc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2016.06.052
CHEMBL3938038 147921 0 None 4 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 368 6 0 5 3.6 CC(C)Oc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2016.06.052
10767264 205256 0 None 102 3 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 486 7 3 3 4.1 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
CHEMBL91405 205256 0 None 102 3 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 486 7 3 3 4.1 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
4209 3102 71 None -2 34 Human 9.4 pKi = 9.4 Binding
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
4893 3102 71 None -2 34 Human 9.4 pKi = 9.4 Binding
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
503 3102 71 None -2 34 Human 9.4 pKi = 9.4 Binding
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
5385 3102 71 None -2 34 Human 9.4 pKi = 9.4 Binding
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
CHEMBL2 3102 71 None -2 34 Human 9.4 pKi = 9.4 Binding
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
DB00457 3102 71 None -2 34 Human 9.4 pKi = 9.4 Binding
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980053f
10839825 205004 0 None 2818 3 Human 9.4 pKi = 9.4 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 525 7 2 4 4.1 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1021/jm990612y
CHEMBL89965 205004 0 None 2818 3 Human 9.4 pKi = 9.4 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 525 7 2 4 4.1 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1021/jm990612y
10552608 99939 0 None 8 3 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 477 4 1 8 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5nc(C)c(C)nc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL290243 99939 0 None 8 3 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 477 4 1 8 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5nc(C)c(C)nc54)c3=O)C[C@@H]21 10.1021/jm990567u
11133288 165469 0 None 7 7 Human 9.4 pKi = 9.4 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 407 12 1 5 4.3 COc1cccc(OC)c1OCCNCCOc1ccccc1Cc1ccccc1 10.1021/jm011066n
CHEMBL42558 165469 0 None 7 7 Human 9.4 pKi = 9.4 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 407 12 1 5 4.3 COc1cccc(OC)c1OCCNCCOc1ccccc1Cc1ccccc1 10.1021/jm011066n
9865801 94273 6 None 3 3 Human 9.4 pKi = 9.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 401 8 2 5 5.0 COc1c(C)c(C)c(O)c(C)c1CN(C)CCOc1cc(C)c(O)cc1C(C)C 10.1021/jm960697s
CHEMBL25300 94273 6 None 3 3 Human 9.4 pKi = 9.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 401 8 2 5 5.0 COc1c(C)c(C)c(O)c(C)c1CN(C)CCOc1cc(C)c(O)cc1C(C)C 10.1021/jm960697s
11633517 72165 0 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 437 13 1 6 4.6 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc(C)c1 10.1021/jm0580398
CHEMBL199080 72165 0 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 437 13 1 6 4.6 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1cccc(C)c1 10.1021/jm0580398
10572854 112061 0 None 2 3 Bovine 9.4 pKi = 9.4 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 396 8 1 5 3.0 COc1ccccc1N1CCN(CCCNc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL330060 112061 0 None 2 3 Bovine 9.4 pKi = 9.4 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 396 8 1 5 3.0 COc1ccccc1N1CCN(CCCNc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10525639 205406 0 None 15 2 Bovine 9.4 pKi = 9.4 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 410 8 1 6 3.9 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)C(C)(C)C)CC1 10.1021/jm970166j
CHEMBL92261 205406 0 None 15 2 Bovine 9.4 pKi = 9.4 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 410 8 1 6 3.9 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)C(C)(C)C)CC1 10.1021/jm970166j
10554957 32759 0 None 1000 3 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 564 11 0 7 5.5 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(CCCCCN2CCC(C#N)(c3ccccc3)CC2)C(C)=N1 10.1021/jm9902032
CHEMBL141604 32759 0 None 1000 3 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 564 11 0 7 5.5 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(CCCCCN2CCC(C#N)(c3ccccc3)CC2)C(C)=N1 10.1021/jm9902032
10626772 35992 0 None 776 3 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 564 11 0 7 5.5 COCC1=NC(C)=C(C(=O)OC)C(c2ccc(F)c(F)c2)N1CCCCCN1CCC(C#N)(c2ccccc2)CC1 10.1021/jm9902032
CHEMBL144534 35992 0 None 776 3 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 564 11 0 7 5.5 COCC1=NC(C)=C(C(=O)OC)C(c2ccc(F)c(F)c2)N1CCCCCN1CCC(C#N)(c2ccccc2)CC1 10.1021/jm9902032
10650129 37260 0 None 162 3 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 540 10 0 7 5.2 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCN(c3ccccc3OC)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL145587 37260 0 None 162 3 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 540 10 0 7 5.2 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCN(c3ccccc3OC)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10841070 37431 0 None 2 4 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 585 10 0 5 7.4 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL145746 37431 0 None 2 4 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 585 10 0 5 7.4 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10815549 121487 0 None 234 3 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 509 9 0 5 6.2 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL359421 121487 0 None 234 3 Human 9.4 pKi = 9.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 509 9 0 5 6.2 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10032383 109608 0 None 194 6 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
136680387 109608 0 None 194 6 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
CHEMBL323579 109608 0 None 194 6 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
44390708 63925 0 None 630 3 Human 9.4 pKi = 9.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)[C@H](c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/j.bmcl.2004.11.032
CHEMBL180932 63925 0 None 630 3 Human 9.4 pKi = 9.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)[C@H](c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/j.bmcl.2004.11.032
9865801 94273 6 None 3 3 Human 9.4 pKi = 9.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 401 8 2 5 5.0 COc1c(C)c(C)c(O)c(C)c1CN(C)CCOc1cc(C)c(O)cc1C(C)C 10.1016/j.bmcl.2004.11.032
CHEMBL25300 94273 6 None 3 3 Human 9.4 pKi = 9.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 401 8 2 5 5.0 COc1c(C)c(C)c(O)c(C)c1CN(C)CCOc1cc(C)c(O)cc1C(C)C 10.1016/j.bmcl.2004.11.032
2389 3267 114 None -7 68 Rat 9.4 pKi = 9.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3267 114 None -7 68 Rat 9.4 pKi = 9.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3267 114 None -7 68 Rat 9.4 pKi = 9.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3267 114 None -7 68 Rat 9.4 pKi = 9.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3267 114 None -7 68 Rat 9.4 pKi = 9.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
44300111 100380 0 None 794 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 583 7 2 7 4.0 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@H](N3CCC(c4ccccn4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL293515 100380 0 None 794 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 583 7 2 7 4.0 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@H](N3CCC(c4ccccn4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
44431194 92114 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 448 5 0 6 3.6 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4ccncc4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
CHEMBL243229 92114 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 448 5 0 6 3.6 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4ccncc4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
9959689 101330 0 None 281 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 568 7 2 7 3.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
CHEMBL300222 101330 0 None 281 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 568 7 2 7 3.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
10393665 33685 0 None 47 3 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 593 9 2 9 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
CHEMBL142383 33685 0 None 47 3 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 593 9 2 9 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
10556164 121169 0 None 549 3 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 572 8 3 6 3.1 CC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1cc(F)c(F)c(F)c1 10.1021/jm990202+
CHEMBL358795 121169 0 None 549 3 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 572 8 3 6 3.1 CC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1cc(F)c(F)c(F)c1 10.1021/jm990202+
9809007 171986 6 None 134 6 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
CHEMBL448620 171986 6 None 134 6 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
10816815 118837 0 None 776 3 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 566 6 2 5 4.9 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CCCc4ccccc43)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL344339 118837 0 None 776 3 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 566 6 2 5 4.9 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CCCc4ccccc43)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
10839391 156816 0 None 1 3 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 472 4 1 7 3.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cc(C#N)ccc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL40780 156816 0 None 1 3 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 472 4 1 7 3.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cc(C#N)ccc54)c3=O)C[C@@H]21 10.1021/jm990567u
101333429 116562 0 None 588 6 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1cccc([N+](=O)[O-])c1 10.1021/jm00019a001
CHEMBL3392247 116562 0 None 588 6 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1cccc([N+](=O)[O-])c1 10.1021/jm00019a001
13305910 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182155 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL215421 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL3741808 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
13305910 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL1182155 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL215421 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL3741808 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
13305910 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL1182155 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL215421 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL3741808 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
13305910 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm301525w
CHEMBL1182155 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm301525w
CHEMBL215421 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm301525w
CHEMBL3741808 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm301525w
13305910 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1039/C4MD00484A
CHEMBL1182155 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1039/C4MD00484A
CHEMBL215421 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1039/C4MD00484A
CHEMBL3741808 11716 1 None -2 9 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1039/C4MD00484A
10624165 100083 0 None 3 3 Rat 9.4 pKi = 9.4 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 469 6 1 7 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(C(C)C)c(OC)sc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL291528 100083 0 None 3 3 Rat 9.4 pKi = 9.4 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 469 6 1 7 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(C(C)C)c(OC)sc4c3=O)C[C@@H]21 10.1021/jm000541z
10506729 201995 0 None 53 3 Human 9.4 pKi = 9.4 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 544 9 1 6 4.4 CC(C)Oc1ccccc1N1CCN(CCCNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
CHEMBL67552 201995 0 None 53 3 Human 9.4 pKi = 9.4 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 544 9 1 6 4.4 CC(C)Oc1ccccc1N1CCN(CCCNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
49781234 17732 0 None -1 4 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 390 2 0 5 4.1 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ccnn4C)cc32)CC1 10.1021/jm100652h
CHEMBL1259231 17732 0 None -1 4 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 390 2 0 5 4.1 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ccnn4C)cc32)CC1 10.1021/jm100652h
10344976 100732 1 None 1 6 Human 9.4 pKi = 9.4 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 477 11 1 10 3.4 COc1cc2nc(N(C)CCSSCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL29591 100732 1 None 1 6 Human 9.4 pKi = 9.4 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 477 11 1 10 3.4 COc1cc2nc(N(C)CCSSCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1021/jm9810654
49782791 17713 0 None 2 6 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 381 3 1 4 3.3 CC(=O)NCc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259173 17713 0 None 2 6 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 381 3 1 4 3.3 CC(=O)NCc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
10506222 110985 0 None 691 3 Human 9.4 pKi = 9.4 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 523 9 3 5 3.5 COCC1=C(C(=O)NCCCN2CCC(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
CHEMBL327716 110985 0 None 691 3 Human 9.4 pKi = 9.4 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 523 9 3 5 3.5 COCC1=C(C(=O)NCCCN2CCC(c3ccccc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
499 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1007/s00044-010-9379-1
5685 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1007/s00044-010-9379-1
CHEMBL25554 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1007/s00044-010-9379-1
499 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm021078o
5685 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm021078o
CHEMBL25554 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm021078o
499 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm030952q
5685 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm030952q
CHEMBL25554 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm030952q
499 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1007/s00044-010-9379-1
5685 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1007/s00044-010-9379-1
CHEMBL25554 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1007/s00044-010-9379-1
499 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.bmc.2010.08.002
5685 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.bmc.2010.08.002
CHEMBL25554 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.bmc.2010.08.002
499 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm991065j
5685 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm991065j
CHEMBL25554 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm991065j
499 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm800461k
5685 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm800461k
CHEMBL25554 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm800461k
499 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm301525w
5685 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm301525w
CHEMBL25554 4002 15 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm301525w
10527466 200990 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 448 5 2 6 2.3 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(NC(C)=O)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL61598 200990 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 448 5 2 6 2.3 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(NC(C)=O)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
49782794 17719 0 None -1 6 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 409 4 1 4 4.0 CC(C)C(=O)NCc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259189 17719 0 None -1 6 Bovine 9.4 pKi = 9.4 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 409 4 1 4 4.0 CC(C)C(=O)NCc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
9891166 33377 0 None 1 5 Bovine 9.4 pKi = 9.4 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 476 6 0 8 3.3 COc1ccccc1N1CCN(CCn2c(=O)c3c(-c4ccccc4)csc3n(C)c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL14213 33377 0 None 1 5 Bovine 9.4 pKi = 9.4 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 476 6 0 8 3.3 COc1ccccc1N1CCN(CCn2c(=O)c3c(-c4ccccc4)csc3n(C)c2=O)CC1 10.1016/s0960-894x(01)00159-7
10994812 203377 0 None 3 4 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 509 9 1 8 3.9 COc1ccc(Cl)cc1N1CCN(CCCNc2c(C(C)=O)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL77618 203377 0 None 3 4 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 509 9 1 8 3.9 COc1ccc(Cl)cc1N1CCN(CCCNc2c(C(C)=O)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
44299974 101411 0 None 89 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 608 7 2 8 3.4 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL300821 101411 0 None 89 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 608 7 2 8 3.4 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
10553935 161259 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 481 4 1 6 4.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(Cl)cc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL41444 161259 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 481 4 1 6 4.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(Cl)cc54)c3=O)C[C@@H]21 10.1021/jm990567u
10529370 205201 0 None 524 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 499 9 3 5 3.0 COCC1=C(C(=O)NCCCN2CCC(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1016/j.ejmech.2017.03.025
CHEMBL91125 205201 0 None 524 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 499 9 3 5 3.0 COCC1=C(C(=O)NCCCN2CCC(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1016/j.ejmech.2017.03.025
44447063 94134 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 434 6 1 5 4.2 CCC(=O)NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21 10.1016/j.bmcl.2007.11.106
CHEMBL252031 94134 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 434 6 1 5 4.2 CCC(=O)NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21 10.1016/j.bmcl.2007.11.106
10529370 205201 0 None 524 3 Human 9.4 pKi = 9.4 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 499 9 3 5 3.0 COCC1=C(C(=O)NCCCN2CCC(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
CHEMBL91125 205201 0 None 524 3 Human 9.4 pKi = 9.4 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 499 9 3 5 3.0 COCC1=C(C(=O)NCCCN2CCC(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
10602912 102252 0 None 301 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 558 9 3 8 2.9 CC(C)Oc1ccccc1N1CCN(C[C@@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(O)cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL304977 102252 0 None 301 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 558 9 3 8 2.9 CC(C)Oc1ccccc1N1CCN(C[C@@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(O)cc2)C3=O)CC1 10.1021/jm9905918
44300087 95961 0 None 67 3 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.5 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@@H](N3CCC(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL262002 95961 0 None 67 3 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.5 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@@H](N3CCC(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
10364994 167311 0 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 423 13 1 6 4.3 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1021/jm0580398
CHEMBL43116 167311 0 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 423 13 1 6 4.3 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1021/jm0580398
10364994 167311 0 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 423 13 1 6 4.3 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL43116 167311 0 None -6 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 423 13 1 6 4.3 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
10095156 78119 0 None 1 3 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL2112073 78119 0 None 1 3 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)C[C@@H]21 10.1021/jm990567u
10678154 170024 0 None 1 3 Rat 9.3 pKi = 9.3 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 397 4 1 6 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cscc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL445071 170024 0 None 1 3 Rat 9.3 pKi = 9.3 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 397 4 1 6 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cscc4c3=O)C[C@@H]21 10.1021/jm000541z
10414908 201067 0 None 204 3 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 539 7 0 4 5.9 Cc1ccc(C2(c3ccc(C)cc3)CC(=O)N(CCCN3CCC(C#N)(c4ccccc4Cl)CC3)C2=O)cc1 10.1016/s0960-894x(01)00320-1
CHEMBL62045 201067 0 None 204 3 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 539 7 0 4 5.9 Cc1ccc(C2(c3ccc(C)cc3)CC(=O)N(CCCN3CCC(C#N)(c4ccccc4Cl)CC3)C2=O)cc1 10.1016/s0960-894x(01)00320-1
71817386 102100 0 None 1 7 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL2419769 102100 0 None 1 7 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL3040851 102100 0 None 1 7 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
11049209 205662 0 None 8 10 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 486 6 1 5 4.4 Cn1ccc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL93923 205662 0 None 8 10 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 486 6 1 5 4.4 Cn1ccc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
44447068 153577 0 None 1 3 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 448 6 1 5 4.4 CC(C)C(=O)NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21 10.1016/j.bmcl.2007.11.106
CHEMBL398525 153577 0 None 1 3 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 448 6 1 5 4.4 CC(C)C(=O)NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21 10.1016/j.bmcl.2007.11.106
10647790 100908 0 None 4 3 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 463 4 1 8 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5nc(C)cnc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL297218 100908 0 None 4 3 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 463 4 1 8 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5nc(C)cnc54)c3=O)C[C@@H]21 10.1021/jm990567u
10507220 120750 0 None 316 3 Human 9.3 pKi = 9.3 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 0 7 5.6 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)cc1F 10.1021/jm9902032
CHEMBL357842 120750 0 None 316 3 Human 9.3 pKi = 9.3 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 0 7 5.6 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)cc1F 10.1021/jm9902032
10626843 168089 0 None 67 3 Human 9.3 pKi = 9.3 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 568 10 0 8 5.0 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCN(c3ccccc3C(=O)OC)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL436407 168089 0 None 67 3 Human 9.3 pKi = 9.3 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 568 10 0 8 5.0 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCN(c3ccccc3C(=O)OC)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10032383 109608 0 None 194 6 Human 9.3 pKi = 9.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
136680387 109608 0 None 194 6 Human 9.3 pKi = 9.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
CHEMBL323579 109608 0 None 194 6 Human 9.3 pKi = 9.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
18738385 202020 0 None 181 3 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 427 7 0 5 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)cs2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL67713 202020 0 None 181 3 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 427 7 0 5 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)cs2)CC1 10.1016/s0960-894x(02)00347-5
122065 188948 3 None 2 8 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 380 5 1 6 1.5 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3ccccc3c2=O)CC1 10.1021/jm970159v
CHEMBL51433 188948 3 None 2 8 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 380 5 1 6 1.5 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3ccccc3c2=O)CC1 10.1021/jm970159v
2865 4064 67 None -4 54 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2007.11.106
59 4064 67 None -4 54 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2007.11.106
60854 4064 67 None -4 54 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2007.11.106
CHEMBL708 4064 67 None -4 54 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2007.11.106
DB00246 4064 67 None -4 54 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2007.11.106
49781453 17670 0 None -1 4 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 386 2 0 3 5.3 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ccccc4)cc32)CC1 10.1021/jm100652h
CHEMBL1259043 17670 0 None -1 4 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 386 2 0 3 5.3 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ccccc4)cc32)CC1 10.1021/jm100652h
10393665 33685 0 None 47 3 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 593 9 2 9 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
CHEMBL142383 33685 0 None 47 3 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 593 9 2 9 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
9916549 121037 0 None 1 4 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL358595 121037 0 None 1 4 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
11757736 33510 0 None 870 4 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 570 9 2 6 4.3 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL142243 33510 0 None 870 4 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 570 9 2 6 4.3 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
10840177 37867 0 None 537 3 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 540 7 2 5 4.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL146109 37867 0 None 537 3 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 540 7 2 5 4.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
9891213 160943 0 None -12 6 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 477 5 1 8 4.0 COc1cc2nc(N3CCN(C(=O)OCc4ccccc4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4128084 160943 0 None -12 6 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 477 5 1 8 4.0 COc1cc2nc(N3CCN(C(=O)OCc4ccccc4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
489 145 22 None -4 13 Bovine 9.3 pKi = 9.3 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm970166j
5640 145 22 None -4 13 Bovine 9.3 pKi = 9.3 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm970166j
CHEMBL420060 145 22 None -4 13 Bovine 9.3 pKi = 9.3 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm970166j
44298447 100319 0 None 5 3 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 430 6 1 6 1.7 Cc1c[nH]c(=O)n(CCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
CHEMBL293149 100319 0 None 5 3 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 430 6 1 6 1.7 Cc1c[nH]c(=O)n(CCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
4209 3102 71 None -2 34 Human 9.3 pKi = 9.3 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
4893 3102 71 None -2 34 Human 9.3 pKi = 9.3 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
503 3102 71 None -2 34 Human 9.3 pKi = 9.3 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
5385 3102 71 None -2 34 Human 9.3 pKi = 9.3 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
CHEMBL2 3102 71 None -2 34 Human 9.3 pKi = 9.3 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
DB00457 3102 71 None -2 34 Human 9.3 pKi = 9.3 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
10029146 203968 0 None 331 3 Human 9.3 pKi = 9.3 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 504 8 0 6 3.9 CCOC(=O)[C@@H]1CN(CCCCN2C(=O)c3cc(Cl)ccc3S2(=O)=O)CC[C@@H]1c1ccccc1 10.1016/s0960-894x(98)00451-x
CHEMBL82267 203968 0 None 331 3 Human 9.3 pKi = 9.3 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 504 8 0 6 3.9 CCOC(=O)[C@@H]1CN(CCCCN2C(=O)c3cc(Cl)ccc3S2(=O)=O)CC[C@@H]1c1ccccc1 10.1016/s0960-894x(98)00451-x
11800077 100033 0 None 2 3 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 481 4 1 6 4.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccc(Cl)c54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL291154 100033 0 None 2 3 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 481 4 1 6 4.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccc(Cl)c54)c3=O)C[C@@H]21 10.1021/jm990567u
44289261 164349 0 None 12 7 Human 9.3 pKi = 9.3 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 417 9 1 4 5.1 COc1cccc(OC)c1OCCNCC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm011066n
CHEMBL42231 164349 0 None 12 7 Human 9.3 pKi = 9.3 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 417 9 1 4 5.1 COc1cccc(OC)c1OCCNCC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm011066n
52942395 17724 0 None 3 6 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 386 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL1259203 17724 0 None 3 6 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 386 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
49781448 17653 0 None 1 4 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 406 2 0 4 5.7 Cc1ccc(-c2ccc3c(c2)C(N2CCN(C)CC2)Cc2ccccc2S3)s1 10.1021/jm100652h
CHEMBL1259005 17653 0 None 1 4 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 406 2 0 4 5.7 Cc1ccc(-c2ccc3c(c2)C(N2CCN(C)CC2)Cc2ccccc2S3)s1 10.1021/jm100652h
52942395 17724 0 None 3 6 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 386 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1021/jm100652h
CHEMBL1259203 17724 0 None 3 6 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 386 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1021/jm100652h
10744687 99947 0 None -1 3 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 490 5 2 7 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(C(N)=O)cc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL290388 99947 0 None -1 3 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 490 5 2 7 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(C(N)=O)cc54)c3=O)C[C@@H]21 10.1021/jm990567u
13911290 27945 0 None -2 6 Rat 9.3 pKi = 9.3 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 386 5 1 7 1.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sccc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL13735 27945 0 None -2 6 Rat 9.3 pKi = 9.3 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 386 5 1 7 1.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sccc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
10769331 111032 0 None 79 6 Human 9.3 pKi = 9.3 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 566 9 2 7 5.9 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc(Cl)c([N+](=O)[O-])c1 10.1021/jm980077m
CHEMBL327931 111032 0 None 79 6 Human 9.3 pKi = 9.3 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 566 9 2 7 5.9 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc(Cl)c([N+](=O)[O-])c1 10.1021/jm980077m
10769331 84854 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 566 9 2 7 5.0 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc(Cl)c([N+](=O)[O-])c1 10.1007/s00044-004-0120-9
CHEMBL2260370 84854 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 566 9 2 7 5.0 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc(Cl)c([N+](=O)[O-])c1 10.1007/s00044-004-0120-9
15054191 196064 0 None 4 2 Rat 9.3 pKi = 9.3 Binding
Binding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranesBinding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranes
ChEMBL 423 4 2 5 2.6 O=c1[nH]c2c([nH]c3ccccc32)c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1021/jm00110a014
CHEMBL57163 196064 0 None 4 2 Rat 9.3 pKi = 9.3 Binding
Binding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranesBinding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranes
ChEMBL 423 4 2 5 2.6 O=c1[nH]c2c([nH]c3ccccc32)c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1021/jm00110a014
10917316 203766 0 None 10 4 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 447 8 1 8 2.6 COc1ccc(Cl)cc1N1CCN(CCCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL80599 203766 0 None 10 4 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 447 8 1 8 2.6 COc1ccc(Cl)cc1N1CCN(CCCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
10411384 156610 0 None -1 3 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cnccc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL40754 156610 0 None -1 3 Rat 9.3 pKi = 9.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cnccc54)c3=O)C[C@@H]21 10.1021/jm990567u
3157 1437 69 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm0580398
7170 1437 69 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm0580398
954 1437 69 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm0580398
CHEMBL707 1437 69 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm0580398
DB00590 1437 69 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm0580398
3157 1437 69 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm8016046
7170 1437 69 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm8016046
954 1437 69 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm8016046
CHEMBL707 1437 69 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm8016046
DB00590 1437 69 None -2 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm8016046
71508713 86627 0 None 295 2 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 388 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ccn(C)n4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2326176 86627 0 None 295 2 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 388 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ccn(C)n4)cc23)CC1 10.1016/j.bmc.2012.10.049
44358574 118851 0 None -2 5 Human 9.3 pKi = 9.3 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 340 9 1 4 4.0 COc1cccc2c1CCCC2CCCNCCOc1ccccn1 10.1021/jm010866v
CHEMBL344432 118851 0 None -2 5 Human 9.3 pKi = 9.3 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 340 9 1 4 4.0 COc1cccc2c1CCCC2CCCNCCOc1ccccn1 10.1021/jm010866v
44431607 147050 0 None 42 4 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 509 7 1 5 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3cccc(Cl)c3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL393105 147050 0 None 42 4 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 509 7 1 5 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3cccc(Cl)c3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
12765746 101797 3 None -3 11 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL303313 101797 3 None -3 11 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
11092112 205884 0 None 3 10 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL95175 205884 0 None 3 10 Bovine 9.3 pKi = 9.3 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
10844296 199720 0 None -1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 425 4 1 5 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(Cl)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL60471 199720 0 None -1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 425 4 1 5 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(Cl)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
9847196 29952 0 None -2 5 Rat 9.2 pKi = 9.2 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(-c4ccccc4)cc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL13903 29952 0 None -2 5 Rat 9.2 pKi = 9.2 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(-c4ccccc4)cc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity against human Alpha-1A adrenergic receptorBinding affinity against human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(99)00484-9
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity against human Alpha-1A adrenergic receptorBinding affinity against human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(99)00484-9
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity against human Alpha-1A adrenergic receptorBinding affinity against human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(99)00484-9
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity against human Alpha-1A adrenergic receptorBinding affinity against human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(99)00484-9
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity against human Alpha-1A adrenergic receptorBinding affinity against human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(99)00484-9
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity against human Alpha-1A adrenergic receptorBinding affinity against human Alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/s0960-894x(99)00484-9
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980506g
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980506g
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980506g
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980506g
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980506g
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm980506g
9916549 121037 0 None -1 4 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of ratIn vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of rat
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL358595 121037 0 None -1 4 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of ratIn vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of rat
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm981006q
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm981006q
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm981006q
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm981006q
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm981006q
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm981006q
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm9810654
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm030952q
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm030952q
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm030952q
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm030952q
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm030952q
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm030952q
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1007/s00044-010-9379-1
9824384 118269 1 None -14 8 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL342062 118269 1 None -14 8 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.05.003
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.05.003
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.05.003
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.05.003
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.05.003
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.ejmech.2017.05.003
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
10718317 100047 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ncccc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL291262 100047 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ncccc54)c3=O)C[C@@H]21 10.1021/jm990567u
10437624 120745 0 None 398 3 Human 9.2 pKi = 9.2 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 553 10 1 7 4.3 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL357828 120745 0 None 398 3 Human 9.2 pKi = 9.2 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 553 10 1 7 4.3 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
499 4002 15 None -1 15 Bovine 9.2 pKi = 9.2 Binding
Binding affinity of compound towards Alpha-1 adrenergic receptor using [3H]prazosin 0.5 nM ligand in frontal cortex calf was determinedBinding affinity of compound towards Alpha-1 adrenergic receptor using [3H]prazosin 0.5 nM ligand in frontal cortex calf was determined
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm950759z
5685 4002 15 None -1 15 Bovine 9.2 pKi = 9.2 Binding
Binding affinity of compound towards Alpha-1 adrenergic receptor using [3H]prazosin 0.5 nM ligand in frontal cortex calf was determinedBinding affinity of compound towards Alpha-1 adrenergic receptor using [3H]prazosin 0.5 nM ligand in frontal cortex calf was determined
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm950759z
CHEMBL25554 4002 15 None -1 15 Bovine 9.2 pKi = 9.2 Binding
Binding affinity of compound towards Alpha-1 adrenergic receptor using [3H]prazosin 0.5 nM ligand in frontal cortex calf was determinedBinding affinity of compound towards Alpha-1 adrenergic receptor using [3H]prazosin 0.5 nM ligand in frontal cortex calf was determined
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm950759z
3894573 3329 4 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1016/j.bmcl.2004.11.032
495 3329 4 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1016/j.bmcl.2004.11.032
CHEMBL88272 3329 4 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1016/j.bmcl.2004.11.032
44300107 100207 0 None 114 3 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.5 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL292365 100207 0 None 114 3 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.5 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
44294957 190440 0 None 295 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 556 7 2 8 2.7 O=C1OCC2=C1C(c1ccc(F)c(F)c1)N(C(=O)NCCCN1CCN(c3ccccc3[N+](=O)[O-])CC1)C(=O)N2 10.1016/s0960-894x(99)00653-8
CHEMBL51871 190440 0 None 295 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 556 7 2 8 2.7 O=C1OCC2=C1C(c1ccc(F)c(F)c1)N(C(=O)NCCCN1CCN(c3ccccc3[N+](=O)[O-])CC1)C(=O)N2 10.1016/s0960-894x(99)00653-8
2142 3035 54 None -2 37 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
4920903 3035 54 None -2 37 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
502 3035 54 None -2 37 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
5775 3035 54 None -2 37 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
CHEMBL597 3035 54 None -2 37 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
DB00692 3035 54 None -2 37 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/ml5004298
10697912 205254 0 None - 1 Human 9.2 pKi = 9.2 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 550 7 2 5 4.0 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1021/jm990612y
CHEMBL91403 205254 0 None - 1 Human 9.2 pKi = 9.2 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 550 7 2 5 4.0 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1021/jm990612y
10530552 33011 0 None 26 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 543 7 3 7 3.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL141821 33011 0 None 26 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 543 7 3 7 3.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990201h
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990201h
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990201h
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990201h
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990201h
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm990201h
24897950 56043 0 None -2 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 462 11 2 6 2.9 COc1ccc(C[C@@H](C)NCCOc2ccccc2OCC(F)(F)F)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
CHEMBL1630940 56043 0 None -2 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 462 11 2 6 2.9 COc1ccc(C[C@@H](C)NCCOc2ccccc2OCC(F)(F)F)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
4209 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm0009336
4893 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm0009336
503 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm0009336
5385 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm0009336
CHEMBL2 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm0009336
DB00457 3102 71 None -2 34 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm0009336
499 4002 15 None -1 15 Bovine 9.2 pKi = 9.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm960069a
5685 4002 15 None -1 15 Bovine 9.2 pKi = 9.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm960069a
CHEMBL25554 4002 15 None -1 15 Bovine 9.2 pKi = 9.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm960069a
11016418 105629 0 None 5 10 Bovine 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL313424 105629 0 None 5 10 Bovine 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
3157 1437 69 None -1 12 Rat 9.2 pKi = 9.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
7170 1437 69 None -1 12 Rat 9.2 pKi = 9.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
954 1437 69 None -1 12 Rat 9.2 pKi = 9.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
CHEMBL707 1437 69 None -1 12 Rat 9.2 pKi = 9.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
DB00590 1437 69 None -1 12 Rat 9.2 pKi = 9.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
10434440 203773 0 None -4 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 461 8 1 8 2.9 COc1ccccc1N1CCN(CCNc2c(C(C)=O)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL80641 203773 0 None -4 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 461 8 1 8 2.9 COc1ccccc1N1CCN(CCNc2c(C(C)=O)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
489 145 22 None -3 13 Human 9.2 pKi = 9.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm960697s
5640 145 22 None -3 13 Human 9.2 pKi = 9.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm960697s
CHEMBL420060 145 22 None -3 13 Human 9.2 pKi = 9.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm960697s
3894573 3329 4 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1021/jm960697s
495 3329 4 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1021/jm960697s
CHEMBL88272 3329 4 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1021/jm960697s
46934643 16483 0 None 6 4 Human 9.2 pKi = 9.2 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 479 7 0 6 3.5 COc1ccccc1N1CCN(C[C@H]2CO[C@@](CN3CCCCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242632 16483 0 None 6 4 Human 9.2 pKi = 9.2 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 479 7 0 6 3.5 COc1ccccc1N1CCN(C[C@H]2CO[C@@](CN3CCCCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
145956955 161540 0 None -2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 397 5 2 8 2.2 COc1cc2nc(N3CCC[C@H](NC(=O)c4ccco4)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
CHEMBL4161165 161540 0 None -2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 397 5 2 8 2.2 COc1cc2nc(N3CCC[C@H](NC(=O)c4ccco4)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
10742076 99841 0 None -1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1cccc2c1CCC1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC21 10.1021/jm990567u
CHEMBL289361 99841 0 None -1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1cccc2c1CCC1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC21 10.1021/jm990567u
44390708 63925 0 None 630 3 Human 9.2 pKi = 9.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)[C@H](c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1021/jm960697s
CHEMBL180932 63925 0 None 630 3 Human 9.2 pKi = 9.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)[C@H](c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1021/jm960697s
10834793 84142 0 None -1 7 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153557 84142 0 None -1 7 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220925 84142 0 None -1 7 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
56946573 71167 0 None 6 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 428 6 0 4 4.9 COc1ccccc1N1CCN(CC2CCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1021/jm200421e
CHEMBL1946780 71167 0 None 6 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 428 6 0 4 4.9 COc1ccccc1N1CCN(CC2CCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1021/jm200421e
CHEMBL1962870 71167 0 None 6 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 428 6 0 4 4.9 COc1ccccc1N1CCN(CC2CCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1021/jm200421e
9866614 14531 1 None 120 3 Human 9.2 pKi = 9.2 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 416 9 1 5 2.1 CC(C)Oc1ccccc1N1CCN(CCCNC(=O)CN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.11.032
CHEMBL12062 14531 1 None 120 3 Human 9.2 pKi = 9.2 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
ChEMBL 416 9 1 5 2.1 CC(C)Oc1ccccc1N1CCN(CCCNC(=O)CN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.11.032
135559170 101577 0 None 8 7 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(CC2CN3C(=O)Nc4ccccc4C3=N2)CC1 10.1021/jm970159v
CHEMBL302021 101577 0 None 8 7 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(CC2CN3C(=O)Nc4ccccc4C3=N2)CC1 10.1021/jm970159v
107715 199250 18 None -1 20 Rat 9.2 pKi = 9.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 199250 18 None -1 20 Rat 9.2 pKi = 9.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 199250 18 None -1 20 Rat 9.2 pKi = 9.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
9866614 14531 1 None 120 3 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 416 9 1 5 2.1 CC(C)Oc1ccccc1N1CCN(CCCNC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL12062 14531 1 None 120 3 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 416 9 1 5 2.1 CC(C)Oc1ccccc1N1CCN(CCCNC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
10792898 202238 0 None 93 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 556 9 2 7 3.5 Cc1ccc(N2C(=O)c3ccc(C(=O)NCC(O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
CHEMBL69295 202238 0 None 93 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 556 9 2 7 3.5 Cc1ccc(N2C(=O)c3ccc(C(=O)NCC(O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
9913988 17718 0 None -1 4 Bovine 9.2 pKi = 9.2 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 502 7 1 7 3.1 Cn1nnc(Cc2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm100652h
CHEMBL1259188 17718 0 None -1 4 Bovine 9.2 pKi = 9.2 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 502 7 1 7 3.1 Cn1nnc(Cc2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm100652h
1238 201475 21 None -3 17 Bovine 9.2 pKi = 9.2 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
CHEMBL64249 201475 21 None -3 17 Bovine 9.2 pKi = 9.2 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
10552656 160753 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 478 5 1 8 3.0 COc1ccc2sc3c(=O)n(CCN4C[C@@H]5CCc6c(OC)cccc6[C@@H]5C4)c(=O)[nH]c3c2n1 10.1021/jm990567u
CHEMBL41234 160753 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 478 5 1 8 3.0 COc1ccc2sc3c(=O)n(CCN4C[C@@H]5CCc6c(OC)cccc6[C@@H]5C4)c(=O)[nH]c3c2n1 10.1021/jm990567u
9895338 93996 0 None 223 3 Human 9.2 pKi = 9.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 622 11 2 7 6.8 CCC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)/C(=C(\O)OC)C(C)=N1 10.1021/jm960697s
CHEMBL25121 93996 0 None 223 3 Human 9.2 pKi = 9.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 622 11 2 7 6.8 CCC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)/C(=C(\O)OC)C(C)=N1 10.1021/jm960697s
3168 9157 84 None 1 22 Rat 9.2 pKi = 9.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9157 84 None 1 22 Rat 9.2 pKi = 9.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
10763038 200979 0 None -1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 391 4 1 5 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4ccccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL61491 200979 0 None -1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 391 4 1 5 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4ccccc4c3=O)C[C@@H]21 10.1021/jm000541z
52946023 17717 0 None 2 6 Bovine 9.2 pKi = 9.2 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 477 7 2 4 3.6 CC(=O)NCc1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm100652h
CHEMBL1259187 17717 0 None 2 6 Bovine 9.2 pKi = 9.2 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 477 7 2 4 3.6 CC(=O)NCc1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm100652h
10718348 99768 0 None 3 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 449 4 1 8 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ncncc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL288678 99768 0 None 3 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 449 4 1 8 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ncncc54)c3=O)C[C@@H]21 10.1021/jm990567u
10415038 4358 0 None 3 4 Human 9.2 pKi = 9.2 Binding
Ability to displace [125I]HEAT from cloned human Alpha-1A adrenergic receptor stably expressed in CHO cellsAbility to displace [125I]HEAT from cloned human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 545 6 1 7 5.3 Cc1noc(C)c1S(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3cccc4ccccc34)CC1)O2 10.1016/s0960-894x(98)00732-x
CHEMBL101610 4358 0 None 3 4 Human 9.2 pKi = 9.2 Binding
Ability to displace [125I]HEAT from cloned human Alpha-1A adrenergic receptor stably expressed in CHO cellsAbility to displace [125I]HEAT from cloned human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 545 6 1 7 5.3 Cc1noc(C)c1S(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3cccc4ccccc34)CC1)O2 10.1016/s0960-894x(98)00732-x
10368033 99946 0 None 5 4 Rat 9.2 pKi = 9.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 483 4 1 8 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ncc(Cl)nc54)c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL290387 99946 0 None 5 4 Rat 9.2 pKi = 9.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 483 4 1 8 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ncc(Cl)nc54)c3=O)C[C@@H]21 10.1021/jm000541z
10368033 99946 0 None 5 4 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 483 4 1 8 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ncc(Cl)nc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL290387 99946 0 None 5 4 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 483 4 1 8 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ncc(Cl)nc54)c3=O)C[C@@H]21 10.1021/jm990567u
6603950 201624 9 None -3 10 Bovine 9.2 pKi = 9.2 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
CHEMBL64875 201624 9 None -3 10 Bovine 9.2 pKi = 9.2 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
10554913 37099 0 None 11 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 561 7 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3cccc(Cl)c3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145443 37099 0 None 11 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 561 7 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3cccc(Cl)c3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
10745766 37236 0 None 141 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 578 9 3 8 2.7 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm990200p
CHEMBL145562 37236 0 None 141 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 578 9 3 8 2.7 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm990200p
10674333 37246 0 None 239 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 554 8 3 6 2.9 CC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145574 37246 0 None 239 3 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 554 8 3 6 2.9 CC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
10415156 120612 0 None 870 4 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 550 8 3 5 3.8 CCC1=C(C(N)=O)C(c2ccc(F)cc2F)N(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL357628 120612 0 None 870 4 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 550 8 3 5 3.8 CCC1=C(C(N)=O)C(c2ccc(F)cc2F)N(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
489 145 22 None -2 13 Rat 9.2 pKi = 9.2 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
5640 145 22 None -2 13 Rat 9.2 pKi = 9.2 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
CHEMBL420060 145 22 None -2 13 Rat 9.2 pKi = 9.2 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
10741071 168640 0 None -1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 425 4 1 5 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cccc(Cl)c4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL440865 168640 0 None -1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 425 4 1 5 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cccc(Cl)c4c3=O)C[C@@H]21 10.1021/jm000541z
10478895 99750 0 None 2 3 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 449 4 1 8 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5nccnc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL288530 99750 0 None 2 3 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 449 4 1 8 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5nccnc54)c3=O)C[C@@H]21 10.1021/jm990567u
20215436 28288 3 None -1 3 Rat 9.1 pKi = 9.1 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 355 4 1 8 2.1 COc1cc2nc(N3CCN(c4ccco4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL137598 28288 3 None -1 3 Rat 9.1 pKi = 9.1 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 355 4 1 8 2.1 COc1cc2nc(N3CCN(c4ccco4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
4209 3102 71 None -4 34 Bovine 9.1 pKi = 9.1 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
4893 3102 71 None -4 34 Bovine 9.1 pKi = 9.1 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
503 3102 71 None -4 34 Bovine 9.1 pKi = 9.1 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
5385 3102 71 None -4 34 Bovine 9.1 pKi = 9.1 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
CHEMBL2 3102 71 None -4 34 Bovine 9.1 pKi = 9.1 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
DB00457 3102 71 None -4 34 Bovine 9.1 pKi = 9.1 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
44431551 86769 0 None 33 4 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3cccc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL232780 86769 0 None 33 4 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3cccc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
44447067 94165 0 None -1 3 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 446 6 1 5 4.2 O=C(NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21)C1CC1 10.1016/j.bmcl.2007.11.106
CHEMBL252230 94165 0 None -1 3 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 446 6 1 5 4.2 O=C(NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21)C1CC1 10.1016/j.bmcl.2007.11.106
10348924 17748 0 None 3 5 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)
ChEMBL 620 10 1 10 3.8 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C#N)CC3)cccc2c1=O 10.1021/jm030825u
CHEMBL125989 17748 0 None 3 5 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)
ChEMBL 620 10 1 10 3.8 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C#N)CC3)cccc2c1=O 10.1021/jm030825u
10721564 205609 0 None 33 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 558 7 1 5 4.9 COC(=O)N1C(=O)N(C)C(C)=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1016/j.ejmech.2017.03.025
CHEMBL93623 205609 0 None 33 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 558 7 1 5 4.9 COC(=O)N1C(=O)N(C)C(C)=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1016/j.ejmech.2017.03.025
10721564 205609 0 None 33 3 Human 9.1 pKi = 9.1 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 558 7 1 5 4.9 COC(=O)N1C(=O)N(C)C(C)=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm990612y
CHEMBL93623 205609 0 None 33 3 Human 9.1 pKi = 9.1 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 558 7 1 5 4.9 COC(=O)N1C(=O)N(C)C(C)=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm990612y
10627003 202627 0 None 53 3 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 576 9 2 7 3.8 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(Cl)c2)C3=O)CC1 10.1021/jm9905918
CHEMBL71580 202627 0 None 53 3 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 576 9 2 7 3.8 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(Cl)c2)C3=O)CC1 10.1021/jm9905918
44431546 87700 0 None 3 4 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 482 7 1 6 3.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccccc3C#N)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234680 87700 0 None 3 4 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 482 7 1 6 3.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccccc3C#N)CC2)CC1 10.1016/j.bmcl.2007.04.008
10626911 101737 0 None 66 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 572 10 2 8 3.2 COc1ccc(N2C(=O)c3ccc(C(=O)NCC(O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
CHEMBL302940 101737 0 None 66 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 572 10 2 8 3.2 COc1ccc(N2C(=O)c3ccc(C(=O)NCC(O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
10625617 161135 0 None 1 3 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 477 5 1 7 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccc(OC)c54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL41344 161135 0 None 1 3 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 477 5 1 7 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccc(OC)c54)c3=O)C[C@@H]21 10.1021/jm990567u
3157 1437 69 None -2 12 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1016/j.ejmech.2017.05.003
7170 1437 69 None -2 12 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1016/j.ejmech.2017.05.003
954 1437 69 None -2 12 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1016/j.ejmech.2017.05.003
CHEMBL707 1437 69 None -2 12 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1016/j.ejmech.2017.05.003
DB00590 1437 69 None -2 12 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1016/j.ejmech.2017.05.003
10648335 99686 0 None 1 3 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 478 5 1 8 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5c(OC)ccnc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL287928 99686 0 None 1 3 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 478 5 1 8 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5c(OC)ccnc54)c3=O)C[C@@H]21 10.1021/jm990567u
10765077 99785 0 None -1 3 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 430 4 2 5 2.8 COc1cccc2c1CCC1CN(CCn3c(=O)[nH]c4c([nH]c5ccccc54)c3=O)CC21 10.1021/jm990567u
CHEMBL288809 99785 0 None -1 3 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 430 4 2 5 2.8 COc1cccc2c1CCC1CN(CCn3c(=O)[nH]c4c([nH]c5ccccc54)c3=O)CC21 10.1021/jm990567u
2142 3035 54 None -1 37 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
4920903 3035 54 None -1 37 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
502 3035 54 None -1 37 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
5775 3035 54 None -1 37 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
CHEMBL597 3035 54 None -1 37 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
DB00692 3035 54 None -1 37 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm970166j
3894573 3329 4 None 1 5 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1021/jm970166j
495 3329 4 None 1 5 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1021/jm970166j
CHEMBL88272 3329 4 None 1 5 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10.1021/jm970166j
10833725 204775 0 None 2 3 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 381 7 1 5 2.7 Cc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL88435 204775 0 None 2 3 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 381 7 1 5 2.7 Cc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10647341 205197 0 None 63 2 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 453 9 1 6 3.8 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC(C)(C)C)CC1 10.1021/jm970166j
CHEMBL91093 205197 0 None 63 2 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 453 9 1 6 3.8 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC(C)(C)C)CC1 10.1021/jm970166j
10550225 205343 0 None 25 2 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 423 8 1 6 3.0 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N2CCCC2)CC1 10.1021/jm970166j
CHEMBL91876 205343 0 None 25 2 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 423 8 1 6 3.0 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N2CCCC2)CC1 10.1021/jm970166j
10524875 205630 0 None 15 3 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ccncc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL93736 205630 0 None 15 3 Bovine 9.1 pKi = 9.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ccncc2C(=O)N(C)C)CC1 10.1021/jm970166j
9891937 193070 0 None 31 3 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 458 8 1 6 2.4 CCc1c[nH]c(=O)n(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
CHEMBL53675 193070 0 None 31 3 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 458 8 1 6 2.4 CCc1c[nH]c(=O)n(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
44298746 193949 0 None 19 3 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 452 7 1 6 2.4 Cc1c[nH]c(=O)n(CC2(CN3CCN(c4ccccc4OCC(F)(F)F)CC3)CC2)c1=O 10.1016/s0960-894x(03)00305-6
CHEMBL55629 193949 0 None 19 3 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 452 7 1 6 2.4 Cc1c[nH]c(=O)n(CC2(CN3CCN(c4ccccc4OCC(F)(F)F)CC3)CC2)c1=O 10.1016/s0960-894x(03)00305-6
9865577 111804 1 None 1 3 Bovine 9.1 pKi = 9.1 Binding
The compound was screened in vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorThe compound was screened in vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL329160 111804 1 None 1 3 Bovine 9.1 pKi = 9.1 Binding
The compound was screened in vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorThe compound was screened in vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10674840 202012 0 None 50 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 585 10 2 8 3.3 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(N(C)C)cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL67648 202012 0 None 50 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 585 10 2 8 3.3 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(N(C)C)cc2)C3=O)CC1 10.1021/jm9905918
44431192 92113 0 None 1 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 448 5 0 6 3.6 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4cccnc4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
CHEMBL243228 92113 0 None 1 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 448 5 0 6 3.6 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4cccnc4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
10917920 110945 0 None 7 11 Bovine 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL327527 110945 0 None 7 11 Bovine 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
56944383 111614 0 None -1 12 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 111614 0 None -1 12 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
10603739 16197 0 None 46 3 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 607 10 2 9 3.8 CCC1=C(C(=O)OC)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL123012 16197 0 None 46 3 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 607 10 2 9 3.8 CCC1=C(C(=O)OC)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
10698141 33588 0 None 21 3 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 561 7 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL142307 33588 0 None 21 3 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 561 7 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
11430126 60224 0 None -1 6 Human 9.1 pKi = 9.1 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 421 4 1 9 2.0 COc1cc2nc(N3CCN(C(=O)C4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
CHEMBL175934 60224 0 None -1 6 Human 9.1 pKi = 9.1 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 421 4 1 9 2.0 COc1cc2nc(N3CCN(C(=O)C4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
3584 3706 60 None -2 14 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990567u
5401 3706 60 None -2 14 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990567u
7302 3706 60 None -2 14 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990567u
CHEMBL611 3706 60 None -2 14 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990567u
DB01162 3706 60 None -2 14 Rat 9.1 pKi = 9.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990567u
10793261 120527 0 None 2290 4 Human 9.1 pKi = 9.1 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 575 10 3 8 3.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
CHEMBL356829 120527 0 None 2290 4 Human 9.1 pKi = 9.1 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 575 10 3 8 3.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
57402366 68958 0 None -1 5 Pig 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928139 68958 0 None -1 5 Pig 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
10740866 101612 0 None 1 3 Rat 9.1 pKi = 9.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 421 5 1 6 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)cccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL302203 101612 0 None 1 3 Rat 9.1 pKi = 9.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 421 5 1 6 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)cccc4c3=O)C[C@@H]21 10.1021/jm000541z
10740369 200168 0 None -1 3 Rat 9.1 pKi = 9.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 411 4 1 6 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(C)csc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL60721 200168 0 None -1 3 Rat 9.1 pKi = 9.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 411 4 1 6 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(C)csc4c3=O)C[C@@H]21 10.1021/jm000541z
9847196 29952 0 None -3 5 Human 9.1 pKi = 9.1 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(-c4ccccc4)cc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL13903 29952 0 None -3 5 Human 9.1 pKi = 9.1 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(-c4ccccc4)cc3c2=O)CC1 10.1016/s0960-894x(01)00159-7
49781676 17675 0 None 1 4 Bovine 9.1 pKi = 9.1 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 400 2 0 3 5.7 Cc1ccccc1-c1ccc2c(c1)C(N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259062 17675 0 None 1 4 Bovine 9.1 pKi = 9.1 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 400 2 0 3 5.7 Cc1ccccc1-c1ccc2c(c1)C(N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
46934639 16476 0 None 6 4 Human 9.1 pKi = 9.1 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 465 7 0 6 3.1 COc1ccccc1N1CCN(C[C@H]2CO[C@@](CN3CCCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242541 16476 0 None 6 4 Human 9.1 pKi = 9.1 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 465 7 0 6 3.1 COc1ccccc1N1CCN(C[C@H]2CO[C@@](CN3CCCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
69782867 161023 0 None -5 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 549 8 1 9 4.4 COc1cc2nc(N3CCN(C(=O)COc4c(OC)cccc4C(C)C)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4129291 161023 0 None -5 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 549 8 1 9 4.4 COc1cc2nc(N3CCN(C(=O)COc4c(OC)cccc4C(C)C)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
44431547 87701 0 None 34 4 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccccc3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234681 87701 0 None 34 4 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccccc3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
10721568 202143 0 None 32 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 558 9 3 8 2.9 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(O)cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL68604 202143 0 None 32 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 558 9 3 8 2.9 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(O)cc2)C3=O)CC1 10.1021/jm9905918
2389 3267 114 None -7 68 Rat 9.1 pKi = 9.1 Binding
Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3267 114 None -7 68 Rat 9.1 pKi = 9.1 Binding
Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3267 114 None -7 68 Rat 9.1 pKi = 9.1 Binding
Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3267 114 None -7 68 Rat 9.1 pKi = 9.1 Binding
Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3267 114 None -7 68 Rat 9.1 pKi = 9.1 Binding
Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
10949698 203566 0 None 1 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 413 8 1 8 1.9 COc1ccccc1N1CCN(CCCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL79161 203566 0 None 1 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 413 8 1 8 1.9 COc1ccccc1N1CCN(CCCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
71462043 84131 0 None -1 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153555 84131 0 None -1 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220895 84131 0 None -1 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
44431564 87200 0 None 34 4 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 501 8 1 6 4.2 COc1ccc(C)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL233623 87200 0 None 34 4 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 501 8 1 6 4.2 COc1ccc(C)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
9872440 101783 0 None 81 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 556 9 2 7 3.5 Cc1cccc(N2C(=O)c3ccc(C(=O)NCC(O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)c1 10.1021/jm9905918
CHEMBL303248 101783 0 None 81 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 556 9 2 7 3.5 Cc1cccc(N2C(=O)c3ccc(C(=O)NCC(O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)c1 10.1021/jm9905918
10506673 202218 0 None 72 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 542 9 2 7 3.2 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccccc2)C3=O)CC1 10.1021/jm9905918
CHEMBL69143 202218 0 None 72 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 542 9 2 7 3.2 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccccc2)C3=O)CC1 10.1021/jm9905918
10047430 104269 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 414 7 0 6 3.4 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3CCCC3=O)cs2)CC1 10.1016/s0960-894x(02)00436-5
CHEMBL310768 104269 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 414 7 0 6 3.4 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3CCCC3=O)cs2)CC1 10.1016/s0960-894x(02)00436-5
44299973 195766 0 None 6 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 608 7 2 8 3.4 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@@H](N3CCN(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL56974 195766 0 None 6 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 608 7 2 8 3.4 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@@H](N3CCN(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
44295192 101239 0 None 338 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 574 7 2 10 2.4 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc3nonc3c2)CC1 10.1016/s0960-894x(99)00653-8
CHEMBL299539 101239 0 None 338 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 574 7 2 10 2.4 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc3nonc3c2)CC1 10.1016/s0960-894x(99)00653-8
9959689 101330 0 None 281 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 568 7 2 7 3.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
CHEMBL300222 101330 0 None 281 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 568 7 2 7 3.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
44447065 94162 0 None -1 3 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 448 7 1 5 4.6 CCCC(=O)NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21 10.1016/j.bmcl.2007.11.106
CHEMBL252228 94162 0 None -1 3 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 448 7 1 5 4.6 CCCC(=O)NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21 10.1016/j.bmcl.2007.11.106
71452768 79146 0 None 53 3 Human 9.1 pKi = 9.1 Binding
Tested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assayTested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assay
ChEMBL 475 6 1 4 5.0 C[C@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1016/s0960-894x(00)00524-2
CHEMBL2114249 79146 0 None 53 3 Human 9.1 pKi = 9.1 Binding
Tested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assayTested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assay
ChEMBL 475 6 1 4 5.0 C[C@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1016/s0960-894x(00)00524-2
10503057 102135 0 None 1 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 436 5 1 7 2.3 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc([N+](=O)[O-])ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL304215 102135 0 None 1 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 436 5 1 7 2.3 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc([N+](=O)[O-])ccc4c3=O)C[C@@H]21 10.1021/jm000541z
11519153 85308 0 None 2 4 Human 9.0 pKi = 9.0 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 514 9 1 6 4.7 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OC4CC4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL229085 85308 0 None 2 4 Human 9.0 pKi = 9.0 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 514 9 1 6 4.7 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OC4CC4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
11519153 85308 0 None 2 4 Human 9.0 pKi = 9.0 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 514 9 1 6 4.7 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OC4CC4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL229085 85308 0 None 2 4 Human 9.0 pKi = 9.0 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 514 9 1 6 4.7 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OC4CC4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
44289525 165431 0 None 4 9 Bovine 9.0 pKi = 9.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]-prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]-prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNCC1Oc2ccccc2OC1c1ccc(C)cc1 10.1021/jm960069a
CHEMBL42539 165431 0 None 4 9 Bovine 9.0 pKi = 9.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]-prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]-prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNCC1Oc2ccccc2OC1c1ccc(C)cc1 10.1021/jm960069a
10601065 111803 0 None 173 3 Human 9.0 pKi = 9.0 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 488 7 4 4 2.8 O=C1NC=C(C(=O)NCCCN2CCC(O)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1021/jm990612y
CHEMBL329143 111803 0 None 173 3 Human 9.0 pKi = 9.0 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 488 7 4 4 2.8 O=C1NC=C(C(=O)NCCCN2CCC(O)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1021/jm990612y
90645605 111933 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 666 13 2 9 5.2 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccc(NC(=O)CCCC(=O)NCCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298023 111933 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 666 13 2 9 5.2 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccc(NC(=O)CCCC(=O)NCCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
10549596 84168 0 None -3 7 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153553 84168 0 None -3 7 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2221147 84168 0 None -3 7 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
4209 3102 71 None -4 34 Bovine 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
4893 3102 71 None -4 34 Bovine 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
503 3102 71 None -4 34 Bovine 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
5385 3102 71 None -4 34 Bovine 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
CHEMBL2 3102 71 None -4 34 Bovine 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
DB00457 3102 71 None -4 34 Bovine 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
9931976 59984 1 None 4 4 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 421 4 0 7 3.3 COc1ccccc1N1CCN(CC2CN=C3c4ccccc4N=C(SC)N32)CC1 10.1021/jm970159v
CHEMBL1744044 59984 1 None 4 4 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 421 4 0 7 3.3 COc1ccccc1N1CCN(CC2CN=C3c4ccccc4N=C(SC)N32)CC1 10.1021/jm970159v
4209 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
4893 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
503 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
5385 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
CHEMBL2 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
DB00457 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm960510x
90645598 111914 0 None -16 3 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 668 12 2 9 4.5 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCC(=O)N(C)Cc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3297829 111914 0 None -16 3 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 668 12 2 9 4.5 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCC(=O)N(C)Cc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
10650843 202142 0 None 57 3 Human 9.0 pKi = 9.0 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 576 9 2 7 3.8 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(Cl)cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL68601 202142 0 None 57 3 Human 9.0 pKi = 9.0 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 576 9 2 7 3.8 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(Cl)cc2)C3=O)CC1 10.1021/jm9905918
49781677 17676 0 None -1 4 Bovine 9.0 pKi = 9.0 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 400 2 0 3 5.7 Cc1cccc(-c2ccc3c(c2)C(N2CCN(C)CC2)Cc2ccccc2S3)c1 10.1021/jm100652h
CHEMBL1259063 17676 0 None -1 4 Bovine 9.0 pKi = 9.0 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 400 2 0 3 5.7 Cc1cccc(-c2ccc3c(c2)C(N2CCN(C)CC2)Cc2ccccc2S3)c1 10.1021/jm100652h
10841070 37431 0 None -2 4 Rat 9.0 pKi = 9.0 Binding
Binding affinity against isolated rat prostate using [3H]- prazosin.Binding affinity against isolated rat prostate using [3H]- prazosin.
ChEMBL 585 10 0 5 7.4 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL145746 37431 0 None -2 4 Rat 9.0 pKi = 9.0 Binding
Binding affinity against isolated rat prostate using [3H]- prazosin.Binding affinity against isolated rat prostate using [3H]- prazosin.
ChEMBL 585 10 0 5 7.4 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
57390116 68941 0 None -1 5 Pig 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928122 68941 0 None -1 5 Pig 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
10793720 202364 0 None 57 2 Human 9.0 pKi = 9.0 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 602 11 2 9 3.2 COc1ccc(N2C(=O)c3ccc(C(=O)NCC(O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1OC 10.1021/jm9905918
CHEMBL70095 202364 0 None 57 2 Human 9.0 pKi = 9.0 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 602 11 2 9 3.2 COc1ccc(N2C(=O)c3ccc(C(=O)NCC(O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1OC 10.1021/jm9905918
9910451 163567 0 None 3 8 Bovine 9.0 pKi = 9 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL420997 163567 0 None 3 8 Bovine 9.0 pKi = 9 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
10481087 168888 0 None 281 3 Human 9.0 pKi = 9 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 499 8 1 3 6.2 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3Cl)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
CHEMBL44294 168888 0 None 281 3 Human 9.0 pKi = 9 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 499 8 1 3 6.2 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3Cl)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
9959671 32437 0 None 363 3 Human 9.0 pKi = 9 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 0 7 5.6 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL141322 32437 0 None 363 3 Human 9.0 pKi = 9 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 0 7 5.6 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10506484 36552 0 None 489 3 Human 9.0 pKi = 9 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 534 9 0 6 5.9 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C#N)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL145001 36552 0 None 489 3 Human 9.0 pKi = 9 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 534 9 0 6 5.9 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C#N)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
9894818 98455 0 None 83 7 Human 9.0 pKi = 9 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL279436 98455 0 None 83 7 Human 9.0 pKi = 9 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
9894818 98455 0 None 83 7 Human 9.0 pKi = 9 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
CHEMBL279436 98455 0 None 83 7 Human 9.0 pKi = 9 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
44431548 86609 0 None 26 4 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 502 8 1 7 3.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL232593 86609 0 None 26 4 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 502 8 1 7 3.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2007.04.008
17753379 87361 0 None -1 4 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 521 8 1 6 4.5 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL233816 87361 0 None -1 4 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 521 8 1 6 4.5 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
44431594 87577 0 None 17 4 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 532 9 1 8 3.8 COc1ccc([N+](=O)[O-])cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234422 87577 0 None 17 4 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 532 9 1 8 3.8 COc1ccc([N+](=O)[O-])cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
10928520 203872 0 None 1 4 Human 9.0 pKi = 9 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 453 7 1 7 3.3 COc1ccc(Cl)cc1N1CCN(CCNc2cc(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL81486 203872 0 None 1 4 Human 9.0 pKi = 9 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 453 7 1 7 3.3 COc1ccc(Cl)cc1N1CCN(CCNc2cc(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
497 3301 6 None 61 3 Human 9.0 pKi = 9 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10.1021/jm960697s
9872515 3301 6 None 61 3 Human 9.0 pKi = 9 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10.1021/jm960697s
CHEMBL24777 3301 6 None 61 3 Human 9.0 pKi = 9 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10.1021/jm960697s
148842 3871 21 None 8 5 Human 9.0 pKi = 9 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm960697s
496 3871 21 None 8 5 Human 9.0 pKi = 9 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm960697s
CHEMBL278865 3871 21 None 8 5 Human 9.0 pKi = 9 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1021/jm960697s
148842 3871 21 None 8 5 Human 9.0 pKi = 9 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1016/j.bmcl.2004.11.032
496 3871 21 None 8 5 Human 9.0 pKi = 9 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1016/j.bmcl.2004.11.032
CHEMBL278865 3871 21 None 8 5 Human 9.0 pKi = 9 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 10.1016/j.bmcl.2004.11.032
609483 123132 10 None - 1 Human 9.0 pKi = 9 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 407 5 0 5 2.8 COc1ccccc1N1CCN(CCN2C(=O)c3ccccc3C(C)(C)C2=O)CC1 10.1016/j.bmcl.2004.11.032
CHEMBL362051 123132 10 None - 1 Human 9.0 pKi = 9 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 407 5 0 5 2.8 COc1ccccc1N1CCN(CCN2C(=O)c3ccccc3C(C)(C)C2=O)CC1 10.1016/j.bmcl.2004.11.032
90645606 111934 0 None 2 3 Human 9.0 pKi = 9 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 652 12 2 9 4.8 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccc(NC(=O)CCCNC(=O)Cc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298024 111934 0 None 2 3 Human 9.0 pKi = 9 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 652 12 2 9 4.8 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccc(NC(=O)CCCNC(=O)Cc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
56668277 62835 0 None 616 3 Human 9.0 pKi = 9 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.3 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@H](N3CCC(C#N)(c4ccccc4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL1789975 62835 0 None 616 3 Human 9.0 pKi = 9 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.3 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@H](N3CCC(C#N)(c4ccccc4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
11984570 92358 0 None 2 3 Human 9.0 pKi = 9 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 465 5 0 5 4.3 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4cccc(F)c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
CHEMBL243694 92358 0 None 2 3 Human 9.0 pKi = 9 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 465 5 0 5 4.3 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4cccc(F)c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
49781680 17688 0 None 4 4 Bovine 9.0 pKi = 9 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 414 2 0 3 6.0 Cc1cccc(C)c1-c1ccc2c(c1)C(N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259097 17688 0 None 4 4 Bovine 9.0 pKi = 9 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 414 2 0 3 6.0 Cc1cccc(C)c1-c1ccc2c(c1)C(N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
10626610 36507 0 None 251 3 Human 9.0 pKi = 9 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 556 8 2 6 4.2 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL144965 36507 0 None 251 3 Human 9.0 pKi = 9 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 556 8 2 6 4.2 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
44298770 101127 0 None 10 3 Human 9.0 pKi = 9 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 464 7 1 6 2.5 O=c1[nH]cc(Cl)c(=O)n1CCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
CHEMBL298838 101127 0 None 10 3 Human 9.0 pKi = 9 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 464 7 1 6 2.5 O=c1[nH]cc(Cl)c(=O)n1CCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
15840661 197771 0 None 31 3 Human 9.0 pKi = 9 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 432 7 1 5 2.2 O=C1CCNC(=O)N1CCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
CHEMBL59153 197771 0 None 31 3 Human 9.0 pKi = 9 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 432 7 1 5 2.2 O=C1CCNC(=O)N1CCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
10717073 200929 0 None 1 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 421 5 1 6 2.4 COc1ccc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2c1 10.1021/jm000541z
CHEMBL61225 200929 0 None 1 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 421 5 1 6 2.4 COc1ccc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2c1 10.1021/jm000541z
10507089 101845 0 None 186 2 Human 9.0 pKi = 9.0 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 560 9 2 7 3.3 CC(C)Oc1ccccc1N1CCN(C[C@@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
CHEMBL303627 101845 0 None 186 2 Human 9.0 pKi = 9.0 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 560 9 2 7 3.3 CC(C)Oc1ccccc1N1CCN(C[C@@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
10644505 100284 0 None -1 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 397 4 1 6 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4sccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL292881 100284 0 None -1 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 397 4 1 6 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4sccc4c3=O)C[C@@H]21 10.1021/jm000541z
4209 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Compound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary glandCompound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970740r
4893 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Compound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary glandCompound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970740r
503 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Compound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary glandCompound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970740r
5385 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Compound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary glandCompound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970740r
CHEMBL2 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Compound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary glandCompound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970740r
DB00457 3102 71 None -3 34 Rat 9.0 pKi = 9.0 Binding
Compound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary glandCompound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary gland
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm970740r
9895326 205289 0 None 177 6 Human 9.0 pKi = 9.0 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 621 12 3 6 5.7 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CC)N1 10.1021/jm980077m
CHEMBL91550 205289 0 None 177 6 Human 9.0 pKi = 9.0 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 621 12 3 6 5.7 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CC)N1 10.1021/jm980077m
9895326 205289 0 None 177 6 Human 9.0 pKi = 9.0 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 621 12 3 6 5.7 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CC)N1 10.1007/s00044-004-0120-9
CHEMBL91550 205289 0 None 177 6 Human 9.0 pKi = 9.0 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 621 12 3 6 5.7 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CC)N1 10.1007/s00044-004-0120-9
10742076 99841 0 None -1 3 Rat 9.0 pKi = 9.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1cccc2c1CCC1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC21 10.1021/jm990567u
CHEMBL289361 99841 0 None -1 3 Rat 9.0 pKi = 9.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1cccc2c1CCC1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC21 10.1021/jm990567u
10606661 100459 0 None 1 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 441 5 1 7 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(C)c(OC)sc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL294027 100459 0 None 1 3 Rat 9.0 pKi = 9.0 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 441 5 1 7 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(C)c(OC)sc4c3=O)C[C@@H]21 10.1021/jm000541z
90645592 111979 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 555 7 2 8 4.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)c5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298745 111979 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 555 7 2 8 4.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)c5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
90645596 111983 0 None -2 3 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 640 11 3 9 3.8 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCC(=O)NCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298749 111983 0 None -2 3 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 640 11 3 9 3.8 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCC(=O)NCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
10507411 33945 0 None 457 3 Human 9.0 pKi = 9.0 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 577 9 0 5 7.3 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3C(F)(F)F)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL142606 33945 0 None 457 3 Human 9.0 pKi = 9.0 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 577 9 0 5 7.3 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(c3ccccc3C(F)(F)F)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10318686 103793 0 None 60 3 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 398 7 0 6 2.9 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCC3=O)no2)CC1 10.1016/s0960-894x(02)00436-5
CHEMBL309969 103793 0 None 60 3 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 398 7 0 6 2.9 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCC3=O)no2)CC1 10.1016/s0960-894x(02)00436-5
44295046 101450 0 None 117 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 577 8 2 9 2.8 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(99)00653-8
CHEMBL301077 101450 0 None 117 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 577 8 2 9 2.8 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(99)00653-8
57390118 68945 0 None -1 5 Pig 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928126 68945 0 None -1 5 Pig 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
57393628 68956 0 None -3 5 Pig 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928137 68956 0 None -3 5 Pig 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
49781678 17681 0 None -1 4 Bovine 9.0 pKi = 9.0 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 400 2 0 3 5.7 Cc1ccc(-c2ccc3c(c2)C(N2CCN(C)CC2)Cc2ccccc2S3)cc1 10.1021/jm100652h
CHEMBL1259079 17681 0 None -1 4 Bovine 9.0 pKi = 9.0 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 400 2 0 3 5.7 Cc1ccc(-c2ccc3c(c2)C(N2CCN(C)CC2)Cc2ccccc2S3)cc1 10.1021/jm100652h
10555288 34502 0 None 45 3 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 582 8 2 7 4.2 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1cccc(Cl)c1 10.1021/jm990200p
CHEMBL143066 34502 0 None 45 3 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 582 8 2 7 4.2 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1cccc(Cl)c1 10.1021/jm990200p
10769058 165115 0 None 208 3 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 552 6 2 5 4.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL424494 165115 0 None 208 3 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 552 6 2 5 4.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
44289321 161407 0 None 6 3 Human 9.0 pKi = 9.0 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 455 8 1 3 5.1 Cc1ccc(C(C(=O)NCCCN2CCN(c3ccccc3C)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
CHEMBL415887 161407 0 None 6 3 Human 9.0 pKi = 9.0 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 455 8 1 3 5.1 Cc1ccc(C(C(=O)NCCCN2CCN(c3ccccc3C)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
9982050 101451 0 None 2 4 Human 9.0 pKi = 9.0 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 467 6 1 9 2.5 COc1ccccc1N1CCN(CCNc2ccc3c4c(=O)n(C)nc(Cl)c4cn3n2)CC1 10.1021/jm981006q
CHEMBL301078 101451 0 None 2 4 Human 9.0 pKi = 9.0 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 467 6 1 9 2.5 COc1ccccc1N1CCN(CCNc2ccc3c4c(=O)n(C)nc(Cl)c4cn3n2)CC1 10.1021/jm981006q
10531766 205259 0 None 199 6 Human 9.0 pKi = 9.0 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 607 9 2 7 6.3 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
CHEMBL91415 205259 0 None 199 6 Human 9.0 pKi = 9.0 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 607 9 2 7 6.3 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
10531766 84850 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 607 9 2 7 5.4 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1007/s00044-004-0120-9
CHEMBL2260366 84850 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 607 9 2 7 5.4 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1007/s00044-004-0120-9
52942152 16871 0 None -2 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 438 13 1 7 4.2 COc1cccc([N+](=O)[O-])c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1254743 16871 0 None -2 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 438 13 1 7 4.2 COc1cccc([N+](=O)[O-])c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
71659980 145348 0 None 1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 354 6 0 5 3.2 CCOc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2016.06.052
CHEMBL3917716 145348 0 None 1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 354 6 0 5 3.2 CCOc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2016.06.052
78815633 146971 2 None 1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 340 7 0 4 3.5 CCOc1ccccc1N1CCN(CCc2ccc(OC)cc2)CC1 10.1016/j.ejmech.2016.06.052
CHEMBL3930616 146971 2 None 1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 340 7 0 4 3.5 CCOc1ccccc1N1CCN(CCc2ccc(OC)cc2)CC1 10.1016/j.ejmech.2016.06.052
10621309 201078 0 None -1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 405 4 1 5 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cccc(C)c4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL62110 201078 0 None -1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 405 4 1 5 2.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cccc(C)c4c3=O)C[C@@H]21 10.1021/jm000541z
9851486 204962 0 None 223 6 Human 8.9 pKi = 8.9 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 592 10 2 6 6.0 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL89685 204962 0 None 223 6 Human 8.9 pKi = 8.9 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 592 10 2 6 6.0 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
9851486 204962 0 None 223 6 Human 8.9 pKi = 8.9 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 592 10 2 6 6.0 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL89685 204962 0 None 223 6 Human 8.9 pKi = 8.9 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 592 10 2 6 6.0 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
10409038 84804 0 None 41 4 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membraneDisplacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membrane
ChEMBL 405 2 2 5 3.6 COc1cc2c(cc1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL225853 84804 0 None 41 4 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membraneDisplacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membrane
ChEMBL 405 2 2 5 3.6 COc1cc2c(cc1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
10620533 200169 0 None 1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 392 4 1 6 1.8 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4ncccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL60722 200169 0 None 1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 392 4 1 6 1.8 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4ncccc4c3=O)C[C@@H]21 10.1021/jm000541z
10770057 101589 0 None 42 3 Human 8.9 pKi = 8.9 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 610 9 2 7 4.5 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(Cl)c(Cl)c2)C3=O)CC1 10.1021/jm9905918
CHEMBL302092 101589 0 None 42 3 Human 8.9 pKi = 8.9 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 610 9 2 7 4.5 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(Cl)c(Cl)c2)C3=O)CC1 10.1021/jm9905918
19085869 167551 0 None 30 3 Human 8.9 pKi = 8.9 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 469 6 0 7 3.2 Cc1ccc2oc(=O)n(C3CCN(CCCCN4C(=O)c5ccccc5S4(=O)=O)CC3)c2c1 10.1016/s0960-894x(98)00446-6
CHEMBL432947 167551 0 None 30 3 Human 8.9 pKi = 8.9 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 469 6 0 7 3.2 Cc1ccc2oc(=O)n(C3CCN(CCCCN4C(=O)c5ccccc5S4(=O)=O)CC3)c2c1 10.1016/s0960-894x(98)00446-6
10578548 36766 0 None 398 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 548 9 0 6 6.2 COC(=O)C1=C(C)N=C(C)N(CCC[C@H](C)CN2CCC(C#N)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL145178 36766 0 None 398 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 548 9 0 6 6.2 COC(=O)C1=C(C)N=C(C)N(CCC[C@H](C)CN2CCC(C#N)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10643502 100469 0 None 1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 380 4 2 5 1.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4[nH]ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL294098 100469 0 None 1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 380 4 2 5 1.7 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4[nH]ccc4c3=O)C[C@@H]21 10.1021/jm000541z
11505007 168346 0 None -3 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 557 9 1 7 4.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL438673 168346 0 None -3 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 557 9 1 7 4.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
44431616 87634 0 None 3 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 471 8 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234649 87634 0 None 3 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 471 8 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
10342554 104290 0 None 33 3 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 428 7 0 6 3.8 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3CCCCC3=O)cs2)CC1 10.1016/s0960-894x(02)00436-5
CHEMBL310890 104290 0 None 33 3 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 428 7 0 6 3.8 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3CCCCC3=O)cs2)CC1 10.1016/s0960-894x(02)00436-5
57400556 68953 0 None -1 5 Pig 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928134 68953 0 None -1 5 Pig 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
57400557 68955 0 None -1 5 Pig 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928136 68955 0 None -1 5 Pig 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
10650633 37289 0 None 64 3 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 566 8 2 7 3.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)cc1 10.1021/jm990200p
CHEMBL145610 37289 0 None 64 3 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 566 8 2 7 3.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)cc1 10.1021/jm990200p
10603727 37442 0 None 114 3 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 606 10 3 8 3.4 CCC1=C(C(=O)NC)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL145752 37442 0 None 114 3 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 606 10 3 8 3.4 CCC1=C(C(=O)NC)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
11994665 11714 0 None -1 7 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cccc(-c2ccccc2)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182151 11714 0 None -1 7 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cccc(-c2ccccc2)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL215151 11714 0 None -1 7 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cccc(-c2ccccc2)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
10770317 202184 0 None 123 2 Human 8.9 pKi = 8.9 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 632 12 2 10 3.2 COc1cc(N2C(=O)c3ccc(C(=O)NCC(O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc(OC)c1OC 10.1021/jm9905918
CHEMBL68913 202184 0 None 123 2 Human 8.9 pKi = 8.9 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 632 12 2 10 3.2 COc1cc(N2C(=O)c3ccc(C(=O)NCC(O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc(OC)c1OC 10.1021/jm9905918
44268966 33203 0 None 5 6 Bovine 8.9 pKi = 8.9 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 476 7 1 7 3.6 COc1ccccc1N1CCN(CCCn2c(=O)[nH]c3scc(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL14199 33203 0 None 5 6 Bovine 8.9 pKi = 8.9 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 476 7 1 7 3.6 COc1ccccc1N1CCN(CCCn2c(=O)[nH]c3scc(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
44275255 98139 0 None 223 3 Human 8.9 pKi = 8.9 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 636 12 2 7 7.2 CCC1=NC(CC)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)/C1=C(\O)OC 10.1021/jm960697s
CHEMBL276932 98139 0 None 223 3 Human 8.9 pKi = 8.9 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 636 12 2 7 7.2 CCC1=NC(CC)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)/C1=C(\O)OC 10.1021/jm960697s
11554541 71449 0 None -25 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 468 14 1 8 4.2 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccc([N+](=O)[O-])cc1 10.1021/jm0580398
CHEMBL196817 71449 0 None -25 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 468 14 1 8 4.2 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccc([N+](=O)[O-])cc1 10.1021/jm0580398
11751173 63081 0 None -1 6 Human 8.9 pKi = 8.9 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 445 4 1 9 2.3 COc1cc2nc(N3CCN(C4=CC(=O)c5ccccc5C4=O)CC3)nc(N)c2cc1OC 10.1021/jm049153d
CHEMBL179743 63081 0 None -1 6 Human 8.9 pKi = 8.9 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 445 4 1 9 2.3 COc1cc2nc(N3CCN(C4=CC(=O)c5ccccc5C4=O)CC3)nc(N)c2cc1OC 10.1021/jm049153d
497 3301 6 None 61 3 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10.1016/s0960-894x(03)00305-6
9872515 3301 6 None 61 3 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10.1016/s0960-894x(03)00305-6
CHEMBL24777 3301 6 None 61 3 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10.1016/s0960-894x(03)00305-6
9804599 101217 0 None 25 3 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 430 7 1 6 1.8 O=c1cc[nH]c(=O)n1CCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
CHEMBL299452 101217 0 None 25 3 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 430 7 1 6 1.8 O=c1cc[nH]c(=O)n1CCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
10506361 157151 0 None 1 3 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 492 5 1 8 3.5 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc([N+](=O)[O-])cc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL40819 157151 0 None 1 3 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 492 5 1 8 3.5 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc([N+](=O)[O-])cc54)c3=O)C[C@@H]21 10.1021/jm990567u
499 4002 15 None -1 15 Rat 8.9 pKi = 8.9 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm960069a
5685 4002 15 None -1 15 Rat 8.9 pKi = 8.9 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm960069a
CHEMBL25554 4002 15 None -1 15 Rat 8.9 pKi = 8.9 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm960069a
10696645 143578 0 None -1 3 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 461 4 1 6 3.9 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccc(C)c54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL39037 143578 0 None -1 3 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 461 4 1 6 3.9 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccc(C)c54)c3=O)C[C@@H]21 10.1021/jm990567u
44431554 166114 0 None 20 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL428197 166114 0 None 20 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
11857710 141819 0 None 1 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 518 8 1 5 5.4 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1 10.1016/j.bmcl.2007.04.098
CHEMBL388897 141819 0 None 1 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 518 8 1 5 5.4 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1 10.1016/j.bmcl.2007.04.098
497 3301 6 None 61 3 Human 8.9 pKi = 8.9 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10.1016/j.bmcl.2004.11.032
9872515 3301 6 None 61 3 Human 8.9 pKi = 8.9 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10.1016/j.bmcl.2004.11.032
CHEMBL24777 3301 6 None 61 3 Human 8.9 pKi = 8.9 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10.1016/j.bmcl.2004.11.032
56961506 120912 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 544 5 2 13 1.6 COc1cc2nc(N3CCN(C(=O)c4cn(-c5cc6ccc(O)cc6oc5=O)nn4)CC3)nc(N)c2cc1OC 10.1021/ml5004298
CHEMBL3582269 120912 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 544 5 2 13 1.6 COc1cc2nc(N3CCN(C(=O)c4cn(-c5cc6ccc(O)cc6oc5=O)nn4)CC3)nc(N)c2cc1OC 10.1021/ml5004298
10973768 107061 0 None -3 11 Bovine 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL318901 107061 0 None -3 11 Bovine 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
49781894 17709 0 None -3 4 Bovine 8.9 pKi = 8.9 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 423 3 1 4 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(CNC(=O)C(C)(C)C)cc32)CC1 10.1021/jm100652h
CHEMBL1259158 17709 0 None -3 4 Bovine 8.9 pKi = 8.9 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 423 3 1 4 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(CNC(=O)C(C)(C)C)cc32)CC1 10.1021/jm100652h
10099811 120497 1 None 676 4 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of dogIn vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of dog
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL356584 120497 1 None 676 4 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of dogIn vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of dog
ChEMBL 583 9 3 6 3.5 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
10841851 34077 0 None 562 3 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 569 9 4 6 2.2 CCC1=C(C(N)=O)C(c2ccc(F)cc2F)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C(=O)N1 10.1021/jm990202+
CHEMBL142718 34077 0 None 562 3 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 569 9 4 6 2.2 CCC1=C(C(N)=O)C(c2ccc(F)cc2F)N(C(=O)NCCCN2CCN(c3ccccc3C(N)=O)CC2)C(=O)N1 10.1021/jm990202+
9894818 98455 0 None 83 7 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm00019a001
CHEMBL279436 98455 0 None 83 7 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm00019a001
9809007 171986 6 None 134 6 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
CHEMBL448620 171986 6 None 134 6 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
9982585 101033 0 None 281 3 Human 8.9 pKi = 8.9 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 479 8 1 3 5.8 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3C)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
CHEMBL298058 101033 0 None 281 3 Human 8.9 pKi = 8.9 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 479 8 1 3 5.8 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3C)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
16721110 83261 0 None -7 3 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 451 5 1 6 3.7 COc1ccc(Cl)cc1N1CCN(CCn2c(C)nc3c([nH]c4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
CHEMBL220515 83261 0 None -7 3 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 451 5 1 6 3.7 COc1ccc(Cl)cc1N1CCN(CCn2c(C)nc3c([nH]c4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
11384634 94247 0 None -134 4 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 420 5 1 5 3.8 CC(=O)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
CHEMBL252818 94247 0 None -134 4 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 420 5 1 5 3.8 CC(=O)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
10480509 141787 0 None 89 2 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membraneDisplacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membrane
ChEMBL 483 2 2 5 4.4 COc1cc2c(c(Br)c1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL388564 141787 0 None 89 2 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membraneDisplacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membrane
ChEMBL 483 2 2 5 4.4 COc1cc2c(c(Br)c1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
136806217 205955 0 None 12 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 576 13 4 8 2.7 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
44328806 205955 0 None 12 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 576 13 4 8 2.7 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
CHEMBL95548 205955 0 None 12 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 576 13 4 8 2.7 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
10627021 106598 0 None 194 6 Human 8.9 pKi = 8.9 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 577 9 2 5 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C)cc1 10.1021/jm980077m
CHEMBL315914 106598 0 None 194 6 Human 8.9 pKi = 8.9 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 577 9 2 5 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C)cc1 10.1021/jm980077m
10627021 84849 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 577 9 2 5 6.0 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C)cc1 10.1007/s00044-004-0120-9
CHEMBL2260365 84849 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 577 9 2 5 6.0 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C)cc1 10.1007/s00044-004-0120-9
10606657 199793 0 None -1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 419 4 1 5 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C)c(C)cc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL60510 199793 0 None -1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 419 4 1 5 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C)c(C)cc4c3=O)C[C@@H]21 10.1021/jm000541z
52942047 16471 0 None 5 4 Human 8.9 pKi = 8.9 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 451 7 0 6 2.7 COc1ccccc1N1CCN(C[C@H]2CO[C@](CN3CCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242444 16471 0 None 5 4 Human 8.9 pKi = 8.9 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 451 7 0 6 2.7 COc1ccccc1N1CCN(C[C@H]2CO[C@](CN3CCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
44447039 153840 0 None -2 4 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 472 6 1 6 4.7 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1ccco1 10.1016/j.bmcl.2007.11.106
CHEMBL398744 153840 0 None -2 4 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 472 6 1 6 4.7 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1ccco1 10.1016/j.bmcl.2007.11.106
71454559 79219 0 None -1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 397 4 1 6 2.4 COc1cccc2c1CCC1CN(CCn3c(=O)[nH]c4ccsc4c3=O)CC21 10.1021/jm000541z
CHEMBL2115086 79219 0 None -1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 397 4 1 6 2.4 COc1cccc2c1CCC1CN(CCn3c(=O)[nH]c4ccsc4c3=O)CC21 10.1021/jm000541z
10692195 100127 0 None -1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 397 4 1 6 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4ccsc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL291839 100127 0 None -1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 397 4 1 6 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4ccsc4c3=O)C[C@@H]21 10.1021/jm000541z
20215436 28288 3 None -3 3 Human 8.9 pKi = 8.9 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 355 4 1 8 2.1 COc1cc2nc(N3CCN(c4ccco4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL137598 28288 3 None -3 3 Human 8.9 pKi = 8.9 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 355 4 1 8 2.1 COc1cc2nc(N3CCN(c4ccco4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
11857639 85307 0 None 56 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 492 7 1 4 5.2 CC(C)Oc1ccccc1C1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.098
CHEMBL229084 85307 0 None 56 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 492 7 1 4 5.2 CC(C)Oc1ccccc1C1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.098
6603950 201624 9 None -3 10 Bovine 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL64875 201624 9 None -3 10 Bovine 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
56837636 68940 0 None 7 5 Pig 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928121 68940 0 None 7 5 Pig 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
10095044 101821 0 None 1 3 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at human Alpha-1A adrenergic receptor.In vitro binding affinity at human Alpha-1A adrenergic receptor.
ChEMBL 445 6 0 8 3.2 COc1ccccc1N1CCN(CCn2nc(-c3ccccc3)c3c(C)onc3c2=O)CC1 10.1021/jm0307741
CHEMBL303464 101821 0 None 1 3 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at human Alpha-1A adrenergic receptor.In vitro binding affinity at human Alpha-1A adrenergic receptor.
ChEMBL 445 6 0 8 3.2 COc1ccccc1N1CCN(CCn2nc(-c3ccccc3)c3c(C)onc3c2=O)CC1 10.1021/jm0307741
11189150 131398 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranesInhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranes
ChEMBL 413 7 1 6 3.2 O=C(NCCCCN1CCN(c2csc3cc(F)ccc23)CC1)c1cnccn1 10.1021/jm0491804
CHEMBL369520 131398 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranesInhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranes
ChEMBL 413 7 1 6 3.2 O=C(NCCCCN1CCN(c2csc3cc(F)ccc23)CC1)c1cnccn1 10.1021/jm0491804
10691912 167446 0 None 1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 392 4 1 6 1.8 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cnccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL432147 167446 0 None 1 3 Rat 8.9 pKi = 8.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 392 4 1 6 1.8 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cnccc4c3=O)C[C@@H]21 10.1021/jm000541z
46224879 199852 3 None -6 7 Human 8.9 pKi = 8.9 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL605405 199852 3 None -6 7 Human 8.9 pKi = 8.9 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
11712250 72639 0 None -5 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 457 13 1 6 5.0 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccccc1Cl 10.1021/jm0580398
CHEMBL200839 72639 0 None -5 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 457 13 1 6 5.0 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccccc1Cl 10.1021/jm0580398
11454386 62762 0 None -1 6 Human 8.9 pKi = 8.9 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 477 8 1 9 3.6 COc1cc2nc(N3CCN(C(=O)CCCCC4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
CHEMBL178923 62762 0 None -1 6 Human 8.9 pKi = 8.9 Binding
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cellsEquilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
ChEMBL 477 8 1 9 3.6 COc1cc2nc(N3CCN(C(=O)CCCCC4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
11270912 197901 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 451 6 0 4 4.6 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL59262 197901 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 451 6 0 4 4.6 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
11270912 197901 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 451 6 0 4 4.6 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL59262 197901 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 451 6 0 4 4.6 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
10578990 202135 0 None 48 3 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 572 10 2 8 3.2 COc1ccccc1N1C(=O)c2ccc(C(=O)NCC(O)CN3CCN(c4ccccc4OC(C)C)CC3)cc2C1=O 10.1021/jm9905918
CHEMBL68565 202135 0 None 48 3 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 572 10 2 8 3.2 COc1ccccc1N1C(=O)c2ccc(C(=O)NCC(O)CN3CCN(c4ccccc4OC(C)C)CC3)cc2C1=O 10.1021/jm9905918
10508332 105498 0 None 109 6 Human 8.8 pKi = 8.8 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 638 11 2 8 6.4 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])c(OC)c1 10.1021/jm980077m
CHEMBL313160 105498 0 None 109 6 Human 8.8 pKi = 8.8 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 638 11 2 8 6.4 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])c(OC)c1 10.1021/jm980077m
10508332 84852 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 638 11 2 8 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])c(OC)c1 10.1007/s00044-004-0120-9
CHEMBL2260368 84852 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 638 11 2 8 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])c(OC)c1 10.1007/s00044-004-0120-9
44420428 83067 0 None -3 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 434 5 0 7 3.8 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccccc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL220221 83067 0 None -3 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 434 5 0 7 3.8 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccccc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
90645593 111980 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 569 8 2 8 3.9 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)Cc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298746 111980 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 569 8 2 8 3.9 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)Cc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
44420428 83067 0 None -3 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 434 5 0 7 3.8 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
CHEMBL220221 83067 0 None -3 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 434 5 0 7 3.8 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
10678161 100335 0 None -1 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 455 5 1 8 2.2 COC(=O)c1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2s1 10.1021/jm000541z
CHEMBL293236 100335 0 None -1 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 455 5 1 8 2.2 COC(=O)c1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2s1 10.1021/jm000541z
10256583 28604 0 None 1 3 Rat 8.8 pKi = 8.8 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 497 7 1 7 4.1 COc1cc2nc(N3CCN(C(=O)CC(c4ccccc4)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL137903 28604 0 None 1 3 Rat 8.8 pKi = 8.8 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 497 7 1 7 4.1 COc1cc2nc(N3CCN(C(=O)CC(c4ccccc4)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
44431599 87622 0 None 10 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 505 7 1 5 4.8 Cc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1Cl 10.1016/j.bmcl.2007.04.008
CHEMBL234609 87622 0 None 10 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 505 7 1 5 4.8 Cc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1Cl 10.1016/j.bmcl.2007.04.008
9915831 101621 0 None 50 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 560 9 2 7 3.3 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
CHEMBL302246 101621 0 None 50 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 560 9 2 7 3.3 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
9850782 103111 0 None 72 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 560 9 2 7 3.3 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(F)cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL308671 103111 0 None 72 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 560 9 2 7 3.3 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(F)cc2)C3=O)CC1 10.1021/jm9905918
9931977 62696 0 None -1 4 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 421 4 0 7 3.3 COc1ccccc1N1CCN(C[C@H]2CN=C3c4ccccc4N=C(SC)N32)CC1 10.1021/jm970159v
CHEMBL1788223 62696 0 None -1 4 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 421 4 0 7 3.3 COc1ccccc1N1CCN(C[C@H]2CN=C3c4ccccc4N=C(SC)N32)CC1 10.1021/jm970159v
49781451 17661 0 None -2 4 Bovine 8.8 pKi = 8.8 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 387 2 0 4 4.7 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ccncc4)cc32)CC1 10.1021/jm100652h
CHEMBL1259024 17661 0 None -2 4 Bovine 8.8 pKi = 8.8 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 387 2 0 4 4.7 CN1CCN(C2Cc3ccccc3Sc3ccc(-c4ccncc4)cc32)CC1 10.1021/jm100652h
49781679 17682 0 None -1 4 Bovine 8.8 pKi = 8.8 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 414 2 0 3 6.0 Cc1cccc(-c2ccc3c(c2)C(N2CCN(C)CC2)Cc2ccccc2S3)c1C 10.1021/jm100652h
CHEMBL1259080 17682 0 None -1 4 Bovine 8.8 pKi = 8.8 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 414 2 0 3 6.0 Cc1cccc(-c2ccc3c(c2)C(N2CCN(C)CC2)Cc2ccccc2S3)c1C 10.1021/jm100652h
10531022 120543 0 None 44 3 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 566 8 2 7 3.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1cccc(F)c1 10.1021/jm990200p
CHEMBL356978 120543 0 None 44 3 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 566 8 2 7 3.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1cccc(F)c1 10.1021/jm990200p
11123606 203714 0 None 2 4 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 475 9 1 8 3.3 COc1ccccc1N1CCN(CCCNc2c(C(C)=O)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL80260 203714 0 None 2 4 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 475 9 1 8 3.3 COc1ccccc1N1CCN(CCCNc2c(C(C)=O)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
11539392 140698 0 None -12 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 437 13 1 6 4.6 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccccc1C 10.1021/jm0580398
CHEMBL382972 140698 0 None -12 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 437 13 1 6 4.6 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccccc1C 10.1021/jm0580398
16121006 11721 0 None -75 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182182 11721 0 None -75 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL217469 11721 0 None -75 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
16121006 11721 0 None -75 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL1182182 11721 0 None -75 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL217469 11721 0 None -75 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
10716502 204839 0 None 39 2 Bovine 8.8 pKi = 8.8 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 410 7 1 5 2.5 COc1ccccc1N1CCN(CCC(=O)Nc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL88820 204839 0 None 39 2 Bovine 8.8 pKi = 8.8 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 410 7 1 5 2.5 COc1ccccc1N1CCN(CCC(=O)Nc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10789868 204993 0 None 158 2 Bovine 8.8 pKi = 8.8 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 453 10 1 6 4.0 COc1ccccc1N1CCN(CCCNc2ccncc2C(=O)N(C(C)C)C(C)C)CC1 10.1021/jm970166j
CHEMBL89916 204993 0 None 158 2 Bovine 8.8 pKi = 8.8 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 453 10 1 6 4.0 COc1ccccc1N1CCN(CCCNc2ccncc2C(=O)N(C(C)C)C(C)C)CC1 10.1021/jm970166j
10552164 205163 0 None -1 3 Bovine 8.8 pKi = 8.8 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 466 9 1 6 3.4 CN(C)C(=O)c1cccnc1N1CCC(NCCOc2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL90869 205163 0 None -1 3 Bovine 8.8 pKi = 8.8 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 466 9 1 6 3.4 CN(C)C(=O)c1cccnc1N1CCC(NCCOc2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
10646065 205165 0 None -1 3 Bovine 8.8 pKi = 8.8 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 425 8 2 6 3.2 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)NC(C)(C)C)CC1 10.1021/jm970166j
CHEMBL90874 205165 0 None -1 3 Bovine 8.8 pKi = 8.8 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 425 8 2 6 3.2 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)NC(C)(C)C)CC1 10.1021/jm970166j
44324012 205508 0 None 6 3 Bovine 8.8 pKi = 8.8 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 397 8 2 6 2.4 COc1ccccc1N1CCN(CCCNc2nc(C)cc(C)c2C(N)=O)CC1 10.1021/jm970166j
CHEMBL92901 205508 0 None 6 3 Bovine 8.8 pKi = 8.8 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 397 8 2 6 2.4 COc1ccccc1N1CCN(CCCNc2nc(C)cc(C)c2C(N)=O)CC1 10.1021/jm970166j
44298671 162614 0 None 19 3 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 460 8 1 7 1.8 COc1c[nH]c(=O)n(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
CHEMBL418112 162614 0 None 19 3 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 460 8 1 7 1.8 COc1c[nH]c(=O)n(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
44298734 195023 0 None 31 3 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 444 7 1 6 2.1 Cc1cc(=O)n(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c(=O)[nH]1 10.1016/s0960-894x(03)00305-6
CHEMBL56489 195023 0 None 31 3 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 444 7 1 6 2.1 Cc1cc(=O)n(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c(=O)[nH]1 10.1016/s0960-894x(03)00305-6
10256583 28604 0 None -1 3 Human 8.8 pKi = 8.8 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 497 7 1 7 4.1 COc1cc2nc(N3CCN(C(=O)CC(c4ccccc4)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL137903 28604 0 None -1 3 Human 8.8 pKi = 8.8 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 497 7 1 7 4.1 COc1cc2nc(N3CCN(C(=O)CC(c4ccccc4)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
10627094 120565 0 None 269 3 Human 8.8 pKi = 8.8 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 581 10 0 7 5.8 COC(=O)C1=C(C)N=C(C)N(CCC[C@H](C)CN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL357131 120565 0 None 269 3 Human 8.8 pKi = 8.8 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 581 10 0 7 5.8 COC(=O)C1=C(C)N=C(C)N(CCC[C@H](C)CN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
44431587 87392 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 565 8 1 6 4.7 COc1ccc(Br)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL233849 87392 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 565 8 1 6 4.7 COc1ccc(Br)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
44431560 145033 0 None -2 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.008
CHEMBL391530 145033 0 None -2 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.008
44431602 147049 0 None 5 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 525 7 1 5 5.2 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL393104 147049 0 None 5 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 525 7 1 5 5.2 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2007.04.008
44299975 101405 0 None 4 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 608 7 2 8 3.4 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@H](N3CCN(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL300766 101405 0 None 4 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 608 7 2 8 3.4 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@@H]2CC[C@H](N3CCN(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
155552185 173479 0 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] prazosin from alpha1A adrenergic receptor (unknown origin)Displacement of [3H] prazosin from alpha1A adrenergic receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 173479 0 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] prazosin from alpha1A adrenergic receptor (unknown origin)Displacement of [3H] prazosin from alpha1A adrenergic receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
9959689 101330 0 None 281 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 568 7 2 7 3.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
CHEMBL300222 101330 0 None 281 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 568 7 2 7 3.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
11046644 30473 0 None -4 6 Human 8.8 pKi = 8.8 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 361 6 0 4 4.0 COc1cccc2c(CCCN3CCN(c4ccccn4)CC3)cccc12 10.1021/jm010866v
CHEMBL139505 30473 0 None -4 6 Human 8.8 pKi = 8.8 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 361 6 0 4 4.0 COc1cccc2c(CCCN3CCN(c4ccccn4)CC3)cccc12 10.1021/jm010866v
10813408 157796 0 None 2 3 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 449 4 1 8 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cncnc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL40896 157796 0 None 2 3 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 449 4 1 8 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cncnc54)c3=O)C[C@@H]21 10.1021/jm990567u
90645599 111927 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 668 13 3 9 4.2 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCC(=O)NCCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298017 111927 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 668 13 3 9 4.2 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCC(=O)NCCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
10767959 160387 0 None -2 3 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 472 4 1 7 3.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(C#N)cc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL41155 160387 0 None -2 3 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 472 4 1 7 3.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(C#N)cc54)c3=O)C[C@@H]21 10.1021/jm990567u
132266 1247 9 None -23 9 Rat 8.8 pKi = 8.8 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm960510x
486 1247 9 None -23 9 Rat 8.8 pKi = 8.8 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm960510x
CHEMBL423294 1247 9 None -23 9 Rat 8.8 pKi = 8.8 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm960510x
90645601 111929 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 564 10 2 9 3.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCN(C)C)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298019 111929 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 564 10 2 9 3.0 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCN(C)C)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
136680383 167428 0 None 21 3 Human 8.8 pKi = 8.8 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(N)=O)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
44328800 167428 0 None 21 3 Human 8.8 pKi = 8.8 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(N)=O)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
CHEMBL432026 167428 0 None 21 3 Human 8.8 pKi = 8.8 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(N)=O)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
16041629 94989 0 None 1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3cc(F)ccc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL257097 94989 0 None 1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3cc(F)ccc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
155515982 169432 0 None -6 17 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] prazosin from alpha1A adrenergic receptor (unknown origin)Displacement of [3H] prazosin from alpha1A adrenergic receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 169432 0 None -6 17 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] prazosin from alpha1A adrenergic receptor (unknown origin)Displacement of [3H] prazosin from alpha1A adrenergic receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
10580182 37225 0 None 1862 3 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 658 7 1 8 4.0 COCC1=C(C(=O)OC)C(c2cc(F)c(F)c(F)c2)N(C(=O)N2CCC(N3CCC(C(=O)OC)(c4ccccc4)CC3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL145553 37225 0 None 1862 3 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 658 7 1 8 4.0 COCC1=C(C(=O)OC)C(c2cc(F)c(F)c(F)c2)N(C(=O)N2CCC(N3CCC(C(=O)OC)(c4ccccc4)CC3)CC2)C(=O)N1 10.1021/jm990201h
9984150 101286 0 None 891 3 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 519 7 0 4 5.6 Cc1ccc(C2(c3ccc(C)cc3)CC(=O)N(CCCN3CCC(C#N)(c4ccccc4C)CC3)C2=O)cc1 10.1016/s0960-894x(01)00320-1
CHEMBL299914 101286 0 None 891 3 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 519 7 0 4 5.6 Cc1ccc(C2(c3ccc(C)cc3)CC(=O)N(CCCN3CCC(C#N)(c4ccccc4C)CC3)C2=O)cc1 10.1016/s0960-894x(01)00320-1
10599007 202800 0 None -5 8 Rat 8.8 pKi = 8.8 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNC[C@@H]1Oc2ccccc2O[C@H]1c1ccc(C)cc1 10.1021/jm960069a
CHEMBL72657 202800 0 None -5 8 Rat 8.8 pKi = 8.8 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNC[C@@H]1Oc2ccccc2O[C@H]1c1ccc(C)cc1 10.1021/jm960069a
10793665 106456 0 None 69 6 Human 8.8 pKi = 8.8 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 597 9 2 5 7.2 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)cc1 10.1021/jm980077m
CHEMBL314960 106456 0 None 69 6 Human 8.8 pKi = 8.8 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 597 9 2 5 7.2 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)cc1 10.1021/jm980077m
10793665 84843 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 597 9 2 5 6.3 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)cc1 10.1007/s00044-004-0120-9
CHEMBL2260359 84843 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 597 9 2 5 6.3 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)cc1 10.1007/s00044-004-0120-9
15054187 191060 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranesBinding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranes
ChEMBL 389 4 2 5 2.0 O=c1[nH]c2c([nH]c3ccccc32)c(=O)n1CCN1CCN(c2ccccc2)CC1 10.1021/jm00110a014
CHEMBL51963 191060 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranesBinding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranes
ChEMBL 389 4 2 5 2.0 O=c1[nH]c2c([nH]c3ccccc32)c(=O)n1CCN1CCN(c2ccccc2)CC1 10.1021/jm00110a014
11857709 85187 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 556 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL228334 85187 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 556 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
11857638 143266 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 516 9 1 6 5.0 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL390129 143266 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 516 9 1 6 5.0 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
11857711 85180 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 506 7 1 4 5.5 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1)c1cc(Cl)ccc1F 10.1016/j.bmcl.2007.04.098
CHEMBL228280 85180 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 506 7 1 4 5.5 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1)c1cc(Cl)ccc1F 10.1016/j.bmcl.2007.04.098
11857709 85187 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 556 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL228334 85187 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 556 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
9808529 202165 0 None 20 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 587 10 2 9 3.1 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc([N+](=O)[O-])cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL68746 202165 0 None 20 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 587 10 2 9 3.1 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc([N+](=O)[O-])cc2)C3=O)CC1 10.1021/jm9905918
18738384 163814 0 None 25 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 441 7 0 5 4.8 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCCC3=O)cs2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL421297 163814 0 None 25 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 441 7 0 5 4.8 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCCC3=O)cs2)CC1 10.1016/s0960-894x(02)00347-5
44431180 92403 0 None -9 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 497 5 0 5 5.4 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4ccc5ccccc5c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
CHEMBL243864 92403 0 None -9 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 497 5 0 5 5.4 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4ccc5ccccc5c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
10793023 120995 0 None 60 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 562 8 2 7 3.8 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1cccc(C)c1 10.1021/jm990200p
CHEMBL358489 120995 0 None 60 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 562 8 2 7 3.8 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1cccc(C)c1 10.1021/jm990200p
10394346 16767 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)
ChEMBL 638 11 2 10 3.0 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C(N)=O)CC3)cccc2c1=O 10.1021/jm030825u
CHEMBL125365 16767 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)Inhibition of [3H]prazosin binding to cloned human Alpha-1A adrenergic receptor in CHO cells (chinese hamster ovary cells)
ChEMBL 638 11 2 10 3.0 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C(N)=O)CC3)cccc2c1=O 10.1021/jm030825u
487 3564 17 None -1 12 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00019a001
60602 3564 17 None -1 12 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00019a001
CHEMBL405355 3564 17 None -1 12 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00019a001
DB09239 3564 17 None -1 12 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00019a001
11270912 197901 0 None -2 5 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 451 6 0 4 4.6 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL59262 197901 0 None -2 5 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 451 6 0 4 4.6 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
10674896 204908 0 None 83 6 Human 8.7 pKi = 8.7 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 588 9 2 6 6.4 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C#N)cc1 10.1021/jm980077m
CHEMBL89243 204908 0 None 83 6 Human 8.7 pKi = 8.7 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 588 9 2 6 6.4 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C#N)cc1 10.1021/jm980077m
10674896 84834 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 588 9 2 6 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C#N)cc1 10.1007/s00044-004-0120-9
CHEMBL2260149 84834 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 588 9 2 6 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C#N)cc1 10.1007/s00044-004-0120-9
53327748 63043 0 None 2 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 435 8 0 5 3.5 COc1ccccc1N1CCN(CCCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796033 63043 0 None 2 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 435 8 0 5 3.5 COc1ccccc1N1CCN(CCCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
9894818 98455 0 None 83 7 Human 8.7 pKi = 8.7 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL279436 98455 0 None 83 7 Human 8.7 pKi = 8.7 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
10651654 110982 0 None 61 6 Human 8.7 pKi = 8.7 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 631 9 2 5 7.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)c(Cl)c1 10.1021/jm980077m
CHEMBL327712 110982 0 None 61 6 Human 8.7 pKi = 8.7 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 631 9 2 5 7.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)c(Cl)c1 10.1021/jm980077m
10651654 84851 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 631 9 2 5 7.0 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)c(Cl)c1 10.1007/s00044-004-0120-9
CHEMBL2260367 84851 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 631 9 2 5 7.0 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)c(Cl)c1 10.1007/s00044-004-0120-9
9894818 98455 0 None 83 7 Human 8.7 pKi = 8.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
CHEMBL279436 98455 0 None 83 7 Human 8.7 pKi = 8.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
44390749 63564 0 None 173 6 Human 8.7 pKi = 8.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 607 11 3 6 5.3 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm960697s
CHEMBL180561 63564 0 None 173 6 Human 8.7 pKi = 8.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 607 11 3 6 5.3 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm960697s
4209 3102 71 None -2 34 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
4893 3102 71 None -2 34 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
503 3102 71 None -2 34 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
5385 3102 71 None -2 34 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
CHEMBL2 3102 71 None -2 34 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
DB00457 3102 71 None -2 34 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1016/j.bmcl.2013.12.024
145962342 160864 0 None -29 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 521 9 0 8 5.1 CCCN(CCC)c1nc(N2CCN(C(=O)c3ccco3)[C@@H]3CCCC[C@@H]32)nc2cc(OC)c(OC)cc12 10.1016/j.bmc.2018.05.023
CHEMBL4126860 160864 0 None -29 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 521 9 0 8 5.1 CCCN(CCC)c1nc(N2CCN(C(=O)c3ccco3)[C@@H]3CCCC[C@@H]32)nc2cc(OC)c(OC)cc12 10.1016/j.bmc.2018.05.023
10767981 194578 0 None -1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 509 11 1 9 3.5 COc1cc2nc(N(C)CCCCCCN(C)C(=O)C3COc4ccccc4O3)nc(N)c2cc1OC 10.1021/jm8016046
CHEMBL561851 194578 0 None -1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 509 11 1 9 3.5 COc1cc2nc(N(C)CCCCCCN(C)C(=O)C3COc4ccccc4O3)nc(N)c2cc1OC 10.1021/jm8016046
44390749 63564 0 None 173 6 Human 8.7 pKi = 8.7 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 607 11 3 6 5.3 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1016/s0960-894x(99)00484-9
CHEMBL180561 63564 0 None 173 6 Human 8.7 pKi = 8.7 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 607 11 3 6 5.3 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1016/s0960-894x(99)00484-9
9894818 98455 0 None 83 7 Human 8.7 pKi = 8.7 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
CHEMBL279436 98455 0 None 83 7 Human 8.7 pKi = 8.7 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
44447059 94100 0 None -23 4 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 473 6 1 7 4.1 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1ccno1 10.1016/j.bmcl.2007.11.106
CHEMBL251834 94100 0 None -23 4 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 473 6 1 7 4.1 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1ccno1 10.1016/j.bmcl.2007.11.106
10742417 201076 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 455 5 1 6 3.0 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1Cl 10.1021/jm000541z
CHEMBL62109 201076 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 455 5 1 6 3.0 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1Cl 10.1021/jm000541z
10793503 119197 0 None 616 3 Human 8.7 pKi = 8.7 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 588 11 2 8 4.5 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
CHEMBL347499 119197 0 None 616 3 Human 8.7 pKi = 8.7 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 588 11 2 8 4.5 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
44390749 63564 0 None 173 6 Human 8.7 pKi = 8.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 607 11 3 6 5.3 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1016/j.bmcl.2004.11.032
CHEMBL180561 63564 0 None 173 6 Human 8.7 pKi = 8.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 607 11 3 6 5.3 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1016/j.bmcl.2004.11.032
57391895 68944 0 None 14 5 Pig 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928125 68944 0 None 14 5 Pig 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
9916549 121037 0 None 1 4 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of dogIn vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of dog
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL358595 121037 0 None 1 4 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of dogIn vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of dog
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
9916549 121037 0 None 1 4 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
CHEMBL358595 121037 0 None 1 4 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 592 10 3 8 3.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990200p
10531675 36535 0 None 19 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 602 8 2 5 5.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL144989 36535 0 None 19 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 602 8 2 5 5.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
10793503 119197 0 None 616 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 588 11 2 8 4.5 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
CHEMBL347499 119197 0 None 616 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 588 11 2 8 4.5 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
44446999 94246 0 None 2 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 474 5 1 5 4.3 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)C(F)(F)F 10.1016/j.bmcl.2007.11.106
CHEMBL252816 94246 0 None 2 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 474 5 1 5 4.3 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)C(F)(F)F 10.1016/j.bmcl.2007.11.106
10048729 188544 0 None 3 4 Human 8.7 pKi = 8.7 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 437 5 1 8 2.5 Cn1nc(Cl)c2cn3nc(NCCN4CCN(c5ccccc5)CC4)ccc3c2c1=O 10.1021/jm981006q
CHEMBL51074 188544 0 None 3 4 Human 8.7 pKi = 8.7 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 437 5 1 8 2.5 Cn1nc(Cl)c2cn3nc(NCCN4CCN(c5ccccc5)CC4)ccc3c2c1=O 10.1021/jm981006q
9847845 28226 0 None -7 6 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(C)c(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL13754 28226 0 None -7 6 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(C)c(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
11604548 72528 0 None -31 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 437 13 1 6 4.6 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccc(C)cc1 10.1007/s00044-010-9379-1
CHEMBL200366 72528 0 None -31 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 437 13 1 6 4.6 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccc(C)cc1 10.1007/s00044-010-9379-1
11532563 165815 0 None -6 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 453 14 1 7 4.3 COc1cccc(COc2ccccc2OCCNCCOc2c(OC)cccc2OC)c1 10.1007/s00044-010-9379-1
CHEMBL427552 165815 0 None -6 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 453 14 1 7 4.3 COc1cccc(COc2ccccc2OCCNCCOc2c(OC)cccc2OC)c1 10.1007/s00044-010-9379-1
11604548 72528 0 None -31 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 437 13 1 6 4.6 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccc(C)cc1 10.1007/s00044-010-9379-1
CHEMBL200366 72528 0 None -31 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 437 13 1 6 4.6 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccc(C)cc1 10.1007/s00044-010-9379-1
11532563 165815 0 None -6 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 453 14 1 7 4.3 COc1cccc(COc2ccccc2OCCNCCOc2c(OC)cccc2OC)c1 10.1007/s00044-010-9379-1
CHEMBL427552 165815 0 None -6 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 453 14 1 7 4.3 COc1cccc(COc2ccccc2OCCNCCOc2c(OC)cccc2OC)c1 10.1007/s00044-010-9379-1
9809007 171986 6 None 134 6 Human 8.7 pKi = 8.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm960697s
CHEMBL448620 171986 6 None 134 6 Human 8.7 pKi = 8.7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm960697s
11705133 71971 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 453 14 1 7 4.3 COc1ccccc1COc1ccccc1OCCNCCOc1c(OC)cccc1OC 10.1021/jm0580398
CHEMBL198431 71971 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 453 14 1 7 4.3 COc1ccccc1COc1ccccc1OCCNCCOc1c(OC)cccc1OC 10.1021/jm0580398
11604548 72528 0 None -31 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 437 13 1 6 4.6 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccc(C)cc1 10.1021/jm0580398
CHEMBL200366 72528 0 None -31 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 437 13 1 6 4.6 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccc(C)cc1 10.1021/jm0580398
11669646 72587 0 None -19 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 453 14 1 7 4.3 COc1ccc(COc2ccccc2OCCNCCOc2c(OC)cccc2OC)cc1 10.1021/jm0580398
CHEMBL200580 72587 0 None -19 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 453 14 1 7 4.3 COc1ccc(COc2ccccc2OCCNCCOc2c(OC)cccc2OC)cc1 10.1021/jm0580398
11532563 165815 0 None -6 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 453 14 1 7 4.3 COc1cccc(COc2ccccc2OCCNCCOc2c(OC)cccc2OC)c1 10.1021/jm0580398
CHEMBL427552 165815 0 None -6 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 453 14 1 7 4.3 COc1cccc(COc2ccccc2OCCNCCOc2c(OC)cccc2OC)c1 10.1021/jm0580398
52941004 16895 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 407 13 1 5 4.7 CCOc1ccccc1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1254914 16895 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 407 13 1 5 4.7 CCOc1ccccc1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
71817547 102092 0 None -7 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
CHEMBL2419771 102092 0 None -7 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
CHEMBL3040800 102092 0 None -7 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
134139869 145655 0 None -1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 384 8 0 5 3.9 COc1ccc(CCN2CCN(c3ccccc3OC(C)C)CC2)cc1OC 10.1016/j.ejmech.2016.06.052
CHEMBL3920110 145655 0 None -1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 384 8 0 5 3.9 COc1ccc(CCN2CCN(c3ccccc3OC(C)C)CC2)cc1OC 10.1016/j.ejmech.2016.06.052
10642742 205058 0 None 3 3 Bovine 8.7 pKi = 8.7 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 367 7 1 5 2.4 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2)CC1 10.1021/jm970166j
CHEMBL90287 205058 0 None 3 3 Bovine 8.7 pKi = 8.7 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 367 7 1 5 2.4 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2)CC1 10.1021/jm970166j
44298694 100212 0 None 9 3 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 426 7 1 6 2.0 Cc1cn(CCCN2CCN(c3ccccc3OCC(F)(F)F)CC2)c(=O)[nH]c1=O 10.1016/s0960-894x(03)00305-6
CHEMBL292403 100212 0 None 9 3 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 426 7 1 6 2.0 Cc1cn(CCCN2CCN(c3ccccc3OCC(F)(F)F)CC2)c(=O)[nH]c1=O 10.1016/s0960-894x(03)00305-6
10415038 4358 0 None 3 4 Human 8.0 pKi = 8 Binding
Binding affinity against Alpha-1A adrenergic receptor in human prostatic tissueBinding affinity against Alpha-1A adrenergic receptor in human prostatic tissue
ChEMBL 545 6 1 7 5.3 Cc1noc(C)c1S(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3cccc4ccccc34)CC1)O2 10.1016/s0960-894x(98)00732-x
CHEMBL101610 4358 0 None 3 4 Human 8.0 pKi = 8 Binding
Binding affinity against Alpha-1A adrenergic receptor in human prostatic tissueBinding affinity against Alpha-1A adrenergic receptor in human prostatic tissue
ChEMBL 545 6 1 7 5.3 Cc1noc(C)c1S(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3cccc4ccccc34)CC1)O2 10.1016/s0960-894x(98)00732-x
10415038 4358 0 None -3 4 Rat 8.0 pKi = 8 Binding
Binding affinity against Alpha-1A adrenergic receptor in rat prostatic tissueBinding affinity against Alpha-1A adrenergic receptor in rat prostatic tissue
ChEMBL 545 6 1 7 5.3 Cc1noc(C)c1S(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3cccc4ccccc34)CC1)O2 10.1016/s0960-894x(98)00732-x
CHEMBL101610 4358 0 None -3 4 Rat 8.0 pKi = 8 Binding
Binding affinity against Alpha-1A adrenergic receptor in rat prostatic tissueBinding affinity against Alpha-1A adrenergic receptor in rat prostatic tissue
ChEMBL 545 6 1 7 5.3 Cc1noc(C)c1S(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3cccc4ccccc34)CC1)O2 10.1016/s0960-894x(98)00732-x
135398737 942 89 None -5 92 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 942 89 None -5 92 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 942 89 None -5 92 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 942 89 None -5 92 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 942 89 None -5 92 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
2389 3267 114 None -14 68 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 3267 114 None -14 68 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 3267 114 None -14 68 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 3267 114 None -14 68 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 3267 114 None -14 68 Human 8.0 pKi = 8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
52937631 60963 0 None -50 3 Human 8.0 pKi = 8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 347 4 0 4 3.4 Cc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
CHEMBL1767141 60963 0 None -50 3 Human 8.0 pKi = 8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 347 4 0 4 3.4 Cc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
44431587 166588 0 None 3 4 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 565 8 1 6 4.7 COc1ccc(Br)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL429076 166588 0 None 3 4 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 565 8 1 6 4.7 COc1ccc(Br)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
11857792 143359 0 None 3 4 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 560 8 1 5 5.8 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1 10.1016/j.bmcl.2007.04.098
CHEMBL390192 143359 0 None 3 4 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 560 8 1 5 5.8 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1 10.1016/j.bmcl.2007.04.098
1524 2141 89 None -7 52 Rat 8.0 pKi = 8 Binding
Binding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 minsBinding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
197 2141 89 None -7 52 Rat 8.0 pKi = 8 Binding
Binding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 minsBinding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
3822 2141 89 None -7 52 Rat 8.0 pKi = 8 Binding
Binding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 minsBinding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
88 2141 89 None -7 52 Rat 8.0 pKi = 8 Binding
Binding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 minsBinding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
CHEMBL51 2141 89 None -7 52 Rat 8.0 pKi = 8 Binding
Binding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 minsBinding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
DB12465 2141 89 None -7 52 Rat 8.0 pKi = 8 Binding
Binding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 minsBinding affinity to rat forebrain homogenate membrane alpha 1 adrenergic receptor incubated for 10 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
115 340 66 None -3 7 Human 8.0 pKi = 8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm960697s
2092 340 66 None -3 7 Human 8.0 pKi = 8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm960697s
7109 340 66 None -3 7 Human 8.0 pKi = 8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm960697s
CHEMBL709 340 66 None -3 7 Human 8.0 pKi = 8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm960697s
DB00346 340 66 None -3 7 Human 8.0 pKi = 8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm960697s
46934793 16436 0 None -7 4 Human 8.0 pKi = 8 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 533 7 0 7 3.8 COc1ccccc1N1CCN(C[C@@H]2CO[C@@](CN3C(=O)CC4(CCCC4)CC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1241557 16436 0 None -7 4 Human 8.0 pKi = 8 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 533 7 0 7 3.8 COc1ccccc1N1CCN(C[C@@H]2CO[C@@](CN3C(=O)CC4(CCCC4)CC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
52941056 16927 0 None -1 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 363 11 1 4 4.3 c1ccc(COc2ccccc2OCCNCCOc2ccccc2)cc1 10.1016/j.bmc.2010.08.002
CHEMBL1255086 16927 0 None -1 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 363 11 1 4 4.3 c1ccc(COc2ccccc2OCCNCCOc2ccccc2)cc1 10.1016/j.bmc.2010.08.002
11668565 15881 0 None -3 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 404 8 1 4 4.9 Fc1ccccc1N1CCN(CCCCNc2ccc(-c3ccccc3)cn2)CC1 10.1016/j.bmcl.2010.07.096
CHEMBL1223799 15881 0 None -3 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 404 8 1 4 4.9 Fc1ccccc1N1CCN(CCCCNc2ccc(-c3ccccc3)cn2)CC1 10.1016/j.bmcl.2010.07.096
71508685 86610 0 None 2 2 Bovine 8.0 pKi = 8 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 385 3 0 3 5.6 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ccncc4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2325930 86610 0 None 2 2 Bovine 8.0 pKi = 8 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 385 3 0 3 5.6 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ccncc4)cc23)CC1 10.1016/j.bmc.2012.10.049
10555223 36879 0 None 158 3 Human 8.0 pKi = 8 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 579 9 3 8 3.3 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC(C)=C(C(=O)O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm990200p
CHEMBL145267 36879 0 None 158 3 Human 8.0 pKi = 8 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 579 9 3 8 3.3 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC(C)=C(C(=O)O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm990200p
53328685 63054 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 435 7 0 5 3.3 COc1ccccc1N1CCN(CCCN2C(=O)CC(C)(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796044 63054 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 435 7 0 5 3.3 COc1ccccc1N1CCN(CCCN2C(=O)CC(C)(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
118716707 114490 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 519 5 0 6 3.9 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)c4ccc(C(F)(F)F)cc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342860 114490 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 519 5 0 6 3.9 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)c4ccc(C(F)(F)F)cc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
44447013 168826 0 None -4 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 500 6 1 5 5.2 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1ccc(F)cc1 10.1016/j.bmcl.2007.11.106
CHEMBL442290 168826 0 None -4 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 500 6 1 5 5.2 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1ccc(F)cc1 10.1016/j.bmcl.2007.11.106
127028034 137112 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 404 9 0 4 5.2 COc1ccccc1N1CCN(CCCCCOc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2015.12.068
CHEMBL3758368 137112 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 404 9 0 4 5.2 COc1ccccc1N1CCN(CCCCCOc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2015.12.068
44447028 94157 0 None -10 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 510 8 1 5 5.4 O=C(CCc1ccccc1)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
CHEMBL252201 94157 0 None -10 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 510 8 1 5 5.4 O=C(CCc1ccccc1)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
8459 3234 3 None -27 3 Human 8.0 pKi = 8.0 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 495 8 1 9 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)COc1c(OC)cccc1C(C)C 10.1021/jm9805337
9891980 3234 3 None -27 3 Human 8.0 pKi = 8.0 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 495 8 1 9 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)COc1c(OC)cccc1C(C)C 10.1021/jm9805337
CHEMBL430717 3234 3 None -27 3 Human 8.0 pKi = 8.0 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 495 8 1 9 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)COc1c(OC)cccc1C(C)C 10.1021/jm9805337
44428849 143085 0 None -6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 436 4 2 7 2.8 COc1cc2nc(N3CCN(C(=O)c4ccc[nH]4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
CHEMBL389978 143085 0 None -6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 436 4 2 7 2.8 COc1cc2nc(N3CCN(C(=O)c4ccc[nH]4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
118716706 114488 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 451 5 0 6 2.9 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)c4ccccc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342859 114488 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 451 5 0 6 2.9 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)c4ccccc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
11474937 195488 0 None -9 4 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 395 5 0 4 3.4 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2C2CC2)CC1 10.1021/jm030944+
CHEMBL56804 195488 0 None -9 4 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 395 5 0 4 3.4 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2C2CC2)CC1 10.1021/jm030944+
44447008 94316 0 None -2 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 482 6 1 5 5.1 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1ccccc1 10.1016/j.bmcl.2007.11.106
CHEMBL253233 94316 0 None -2 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 482 6 1 5 5.1 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1ccccc1 10.1016/j.bmcl.2007.11.106
9867616 167752 0 None -2 3 Rat 8.0 pKi = 8.0 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 435 6 1 8 2.2 COc1cc2nc(N3CCN(C(=O)CC(=O)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL434228 167752 0 None -2 3 Rat 8.0 pKi = 8.0 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 435 6 1 8 2.2 COc1cc2nc(N3CCN(C(=O)CC(=O)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
44318081 162750 0 None 3 3 Human 7.0 pKi = 7 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 504 8 0 6 3.9 CCOC(=O)[C@H]1CN(CCCCN2C(=O)c3cc(Cl)ccc3S2(=O)=O)CC[C@@H]1c1ccccc1 10.1016/s0960-894x(98)00451-x
CHEMBL418926 162750 0 None 3 3 Human 7.0 pKi = 7 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 504 8 0 6 3.9 CCOC(=O)[C@H]1CN(CCCCN2C(=O)c3cc(Cl)ccc3S2(=O)=O)CC[C@@H]1c1ccccc1 10.1016/s0960-894x(98)00451-x
9822477 197761 0 None -34 5 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 403 4 0 4 3.5 Cc1ccc(Cl)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1007/s00044-010-9379-1
CHEMBL59149 197761 0 None -34 5 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 403 4 0 4 3.5 Cc1ccc(Cl)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1007/s00044-010-9379-1
242 467 117 None -14 52 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 467 117 None -14 52 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 467 117 None -14 52 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 467 117 None -14 52 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 467 117 None -14 52 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
2337 3193 72 None -5 63 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
50 3193 72 None -5 63 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
5002 3193 72 None -5 63 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
CHEMBL716 3193 72 None -5 63 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
DB01224 3193 72 None -5 63 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
52937119 60976 0 None -15 3 Human 7.0 pKi = 7 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 367 4 0 4 3.6 CN1CCC(Cn2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1 10.1021/jm1013874
CHEMBL1767155 60976 0 None -15 3 Human 7.0 pKi = 7 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 367 4 0 4 3.6 CN1CCC(Cn2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1 10.1021/jm1013874
24803641 60980 0 None -199 4 Human 7.0 pKi = 7 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 612 10 0 6 7.5 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(Cc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
CHEMBL1767159 60980 0 None -199 4 Human 7.0 pKi = 7 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 612 10 0 6 7.5 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(Cc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
24803639 60987 0 None -251 4 Human 7.0 pKi = 7 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 622 14 1 7 6.8 O=c1c2ccccc2c(Cc2ccc(O)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767166 60987 0 None -251 4 Human 7.0 pKi = 7 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 622 14 1 7 6.8 O=c1c2ccccc2c(Cc2ccc(O)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
44431557 146127 0 None -1 4 Human 7.0 pKi = 7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 541 8 1 6 4.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL392377 146127 0 None -1 4 Human 7.0 pKi = 7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 541 8 1 6 4.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
10362296 94632 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 378 8 1 3 3.6 CC(=O)CC(=O)NCCCN1CCC(c2ccccc2)(c2ccccc2)CC1 10.1021/jm960697s
CHEMBL25537 94632 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 378 8 1 3 3.6 CC(=O)CC(=O)NCCCN1CCC(c2ccccc2)(c2ccccc2)CC1 10.1021/jm960697s
44417715 11718 0 None 2 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 399 8 1 6 3.4 COc1cccc(OC)c1OCCNC[C@@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL1182160 11718 0 None 2 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 399 8 1 6 3.4 COc1cccc(OC)c1OCCNC[C@@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL215857 11718 0 None 2 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 399 8 1 6 3.4 COc1cccc(OC)c1OCCNC[C@@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
11135150 7507 0 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 435 10 1 6 4.0 COc1cccc(OC)c1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
CHEMBL1087942 7507 0 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 435 10 1 6 4.0 COc1cccc(OC)c1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
CHEMBL287686 7507 0 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 435 10 1 6 4.0 COc1cccc(OC)c1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
9822477 197761 0 None -34 5 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 403 4 0 4 3.5 Cc1ccc(Cl)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1007/s00044-010-9379-1
CHEMBL59149 197761 0 None -34 5 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 403 4 0 4 3.5 Cc1ccc(Cl)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1007/s00044-010-9379-1
9908478 193953 0 None -7079 8 Human 6.0 pKi = 6 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 391 4 0 4 2.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)ccc2F)CC1 10.1021/jm0491391
CHEMBL556313 193953 0 None -7079 8 Human 6.0 pKi = 6 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 391 4 0 4 2.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)ccc2F)CC1 10.1021/jm0491391
135398745 2858 108 None -39 66 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 2858 108 None -39 66 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 2858 108 None -39 66 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 2858 108 None -39 66 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
9923249 5506 0 None - 1 Rat 6.0 pKi = 6 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 323 4 2 4 2.8 CCS(=O)(=O)Nc1cccc2c1SCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL107726 5506 0 None - 1 Rat 6.0 pKi = 6 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 323 4 2 4 2.8 CCS(=O)(=O)Nc1cccc2c1SCCC2c1c[nH]cn1 10.1021/jm030551a
16041451 97346 0 None -5 4 Human 7.0 pKi = 7 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 500 7 2 5 5.4 COc1ccc(Cl)cc1NC(=O)NC1CCC(N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL271913 97346 0 None -5 4 Human 7.0 pKi = 7 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 500 7 2 5 5.4 COc1ccc(Cl)cc1NC(=O)NC1CCC(N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.11.068
16756753 91682 0 None -37 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
CHEMBL242003 91682 0 None -37 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
44417709 12299 0 None 2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 395 8 1 6 3.7 COc1cccc(OC)c1OCCNC[C@@H]1COc2cc3ccccc3cc2O1 10.1021/jm060358r
CHEMBL1185857 12299 0 None 2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 395 8 1 6 3.7 COc1cccc(OC)c1OCCNC[C@@H]1COc2cc3ccccc3cc2O1 10.1021/jm060358r
CHEMBL436955 12299 0 None 2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 395 8 1 6 3.7 COc1cccc(OC)c1OCCNC[C@@H]1COc2cc3ccccc3cc2O1 10.1021/jm060358r
127025275 137144 0 None -263 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 474 9 2 5 4.7 CCOC(=O)Nc1cccc(N2CCN(CCCCNC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2015.12.068
CHEMBL3758665 137144 0 None -263 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 474 9 2 5 4.7 CCOC(=O)Nc1cccc(N2CCN(CCCCNC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2015.12.068
19085921 104417 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 513 7 0 9 2.6 COC(=O)c1ccc2c(c1)oc(=O)n2C1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL311290 104417 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 513 7 0 9 2.6 COC(=O)c1ccc2c(c1)oc(=O)n2C1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/s0960-894x(98)00446-6
10939408 47144 0 None -181 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
CHEMBL154508 47144 0 None -181 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
25022505 187697 0 None 2 3 Rat 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 586 10 1 8 2.9 COC(=O)C(C)N1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL500266 187697 0 None 2 3 Rat 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 586 10 1 8 2.9 COC(=O)C(C)N1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
3191 102372 93 None -204 25 Rat 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102372 93 None -204 25 Rat 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
102 4051 44 None -346 50 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00019a001
3659 4051 44 None -346 50 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00019a001
8969 4051 44 None -346 50 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00019a001
CHEMBL15245 4051 44 None -346 50 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00019a001
DB01392 4051 44 None -346 50 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00019a001
127046693 139124 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000341aCl ADRA1ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000341aCl ADRA1A
ChEMBL 300 3 2 4 2.2 C[C@@H](c1cccc(C#N)c1)n1cc(Cl)cc(C(N)=O)c1=N nan
CHEMBL3797887 139124 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000341aCl ADRA1ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000341aCl ADRA1A
ChEMBL 300 3 2 4 2.2 C[C@@H](c1cccc(C#N)c1)n1cc(Cl)cc(C(N)=O)c1=N nan
CHEMBL4762646 139124 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000341aCl ADRA1ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000341aCl ADRA1A
ChEMBL 300 3 2 4 2.2 C[C@@H](c1cccc(C#N)c1)n1cc(Cl)cc(C(N)=O)c1=N nan
2812 4696 96 None -2238 34 Rat 5.0 pKi = 5.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4696 96 None -2238 34 Rat 5.0 pKi = 5.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
9844321 100381 0 None -588 5 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 407 4 0 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL293539 100381 0 None -588 5 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 407 4 0 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)ccc2Cl)CC1 10.1021/jm030944+
10669270 165725 0 None -28 2 Rat 7.0 pKi = 7.0 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 410 5 0 4 2.6 O=C1C2CCCN2C(=O)N1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm970216k
CHEMBL42706 165725 0 None -28 2 Rat 7.0 pKi = 7.0 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 410 5 0 4 2.6 O=C1C2CCCN2C(=O)N1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm970216k
14004040 51344 0 None -6 2 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 227 0 0 2 3.5 c1ccc2c3c(oc2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL158371 51344 0 None -6 2 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 227 0 0 2 3.5 c1ccc2c3c(oc2c1)C1CCCCN1CC3 10.1021/jm00398a025
145951352 162198 0 None -2 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 397 5 2 8 2.2 COc1cc2nc(N3CCC[C@@H](NC(=O)c4ccco4)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
CHEMBL4171710 162198 0 None -2 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 397 5 2 8 2.2 COc1cc2nc(N3CCC[C@@H](NC(=O)c4ccco4)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
56945164 71155 0 None -338 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 417 9 2 4 4.4 COc1ccccc1OCCNC[C@H]1CCC(c2ccccc2)(c2ccccc2)[C@@H]1O 10.1021/jm200421e
CHEMBL1946786 71155 0 None -338 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 417 9 2 4 4.4 COc1ccccc1OCCNC[C@H]1CCC(c2ccccc2)(c2ccccc2)[C@@H]1O 10.1021/jm200421e
CHEMBL1962756 71155 0 None -338 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 417 9 2 4 4.4 COc1ccccc1OCCNC[C@H]1CCC(c2ccccc2)(c2ccccc2)[C@@H]1O 10.1021/jm200421e
14004039 119043 3 None -5 2 Bovine 6.0 pKi = 6.0 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 193 0 0 2 2.8 c1cc2c(s1)C1CCCCN1CC2 10.1021/jm00398a025
CHEMBL346016 119043 3 None -5 2 Bovine 6.0 pKi = 6.0 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 193 0 0 2 2.8 c1cc2c(s1)C1CCCCN1CC2 10.1021/jm00398a025
10744391 205621 0 None 7 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 514 7 1 3 4.8 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H](c2ccc(F)c(F)c2)N(C)C(=O)N1C 10.1021/jm990612y
CHEMBL93693 205621 0 None 7 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 514 7 1 3 4.8 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H](c2ccc(F)c(F)c2)N(C)C(=O)N1C 10.1021/jm990612y
1353 1872 85 None -6 86 Human 8.0 pKi = 8.0 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1872 85 None -6 86 Human 8.0 pKi = 8.0 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1872 85 None -6 86 Human 8.0 pKi = 8.0 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1872 85 None -6 86 Human 8.0 pKi = 8.0 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1872 85 None -6 86 Human 8.0 pKi = 8.0 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
10092649 192461 51 None 1 9 Human 8.0 pKi = 8.0 Binding
Binding affinity to human adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to human adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1021/jm100697g
CHEMBL522460 192461 51 None 1 9 Human 8.0 pKi = 8.0 Binding
Binding affinity to human adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to human adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1021/jm100697g
11519153 85178 0 None 3 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 514 9 1 6 4.7 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OC4CC4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL228278 85178 0 None 3 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 514 9 1 6 4.7 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OC4CC4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
11857861 193102 0 None -1 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 520 10 1 6 4.5 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCCF)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL538397 193102 0 None -1 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 520 10 1 6 4.5 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCCF)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
44431611 87043 0 None -7 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 509 7 1 5 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Cl)cc3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL233410 87043 0 None -7 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 509 7 1 5 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Cl)cc3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
17753379 87361 0 None -1 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 521 8 1 6 4.5 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL233816 87361 0 None -1 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 521 8 1 6 4.5 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
44431599 87578 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 505 7 1 5 4.8 Cc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1Cl 10.1016/j.bmcl.2007.04.008
CHEMBL234423 87578 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 505 7 1 5 4.8 Cc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1Cl 10.1016/j.bmcl.2007.04.008
44431574 145725 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 505 8 1 6 4.0 COc1ccc(F)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL392066 145725 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 505 8 1 6 4.0 COc1ccc(F)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
11519153 85178 0 None 3 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 514 9 1 6 4.7 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OC4CC4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL228278 85178 0 None 3 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 514 9 1 6 4.7 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OC4CC4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
16041091 94764 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 468 7 2 4 4.5 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)NCc3cccc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL256041 94764 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 468 7 2 4 4.5 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)NCc3cccc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
16041263 94990 0 None -1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 470 6 2 4 5.4 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL257098 94990 0 None -1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 470 6 2 4 5.4 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
145946966 167025 0 None -5 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 354 7 0 4 3.9 COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4209888 167025 0 None -5 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 354 7 0 4 3.9 COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4300899 167025 0 None -5 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 354 7 0 4 3.9 COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
6603808 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL214986 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL36622 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL3740374 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
6603808 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL214986 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL36622 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL3740374 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
6603808 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm301525w
CHEMBL214986 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm301525w
CHEMBL36622 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm301525w
CHEMBL3740374 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm301525w
6603808 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1039/C4MD00484A
CHEMBL214986 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1039/C4MD00484A
CHEMBL36622 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1039/C4MD00484A
CHEMBL3740374 126987 2 None -1 9 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1039/C4MD00484A
46934637 16477 0 None -7 4 Human 7.9 pKi = 7.9 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 465 7 0 6 3.1 COc1ccccc1N1CCN(C[C@@H]2CO[C@@](CN3CCCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242542 16477 0 None -7 4 Human 7.9 pKi = 7.9 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 465 7 0 6 3.1 COc1ccccc1N1CCN(C[C@@H]2CO[C@@](CN3CCCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
11994551 11720 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 369 7 1 5 3.4 COc1ccc2c(c1OCCNC[C@@H]1COc3ccccc3O1)CCCC2 10.1021/jm060358r
CHEMBL1182179 11720 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 369 7 1 5 3.4 COc1ccc2c(c1OCCNC[C@@H]1COc3ccccc3O1)CCCC2 10.1021/jm060358r
CHEMBL217143 11720 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 369 7 1 5 3.4 COc1ccc2c(c1OCCNC[C@@H]1COc3ccccc3O1)CCCC2 10.1021/jm060358r
50905589 56045 0 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 406 7 2 6 2.1 COc1ccc(C[C@@H](C)NC[C@@H]2Oc3ccccc3O[C@@H]2C)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
CHEMBL1630942 56045 0 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 406 7 2 6 2.1 COc1ccc(C[C@@H](C)NC[C@@H]2Oc3ccccc3O[C@@H]2C)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
44328920 108141 0 None 15 6 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 705 14 3 7 5.9 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCC(F)(F)F)N1 10.1016/s0960-894x(99)00484-9
CHEMBL320736 108141 0 None 15 6 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 705 14 3 7 5.9 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCC(F)(F)F)N1 10.1016/s0960-894x(99)00484-9
118716710 114493 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 444 5 1 7 1.3 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)C4CCCN4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342863 114493 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 444 5 1 7 1.3 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)C4CCCN4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
14004040 51344 0 None -6 2 Bovine 7.0 pKi = 7.0 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 227 0 0 2 3.5 c1ccc2c3c(oc2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL158371 51344 0 None -6 2 Bovine 7.0 pKi = 7.0 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 227 0 0 2 3.5 c1ccc2c3c(oc2c1)C1CCCCN1CC3 10.1021/jm00398a025
10254390 71329 0 None -851 8 Rat 7.0 pKi = 7.0 Binding
Binding affinity for rat Alpha-1A adrenergic receptor using [11C] radiotracerBinding affinity for rat Alpha-1A adrenergic receptor using [11C] radiotracer
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm050171k
CHEMBL196476 71329 0 None -851 8 Rat 7.0 pKi = 7.0 Binding
Binding affinity for rat Alpha-1A adrenergic receptor using [11C] radiotracerBinding affinity for rat Alpha-1A adrenergic receptor using [11C] radiotracer
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm050171k
16041090 94936 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 496 8 2 6 4.7 COc1ccc(NC(=O)NC2CCC(N3CCN(c4ccccc4OC(C)C)CC3)CC2)c(OC)c1 10.1016/j.bmcl.2007.11.068
CHEMBL256853 94936 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 496 8 2 6 4.7 COc1ccc(NC(=O)NC2CCC(N3CCN(c4ccccc4OC(C)C)CC3)CC2)c(OC)c1 10.1016/j.bmcl.2007.11.068
13938361 184771 0 None -141 2 Bovine 7.0 pKi = 7.0 Binding
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortexEvaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN([C@@H]1CCN2CCc3c(oc4ccccc34)[C@@H]2C1)S(=O)(=O)CCO 10.1021/jm00150a002
CHEMBL48603 184771 0 None -141 2 Bovine 7.0 pKi = 7.0 Binding
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortexEvaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN([C@@H]1CCN2CCc3c(oc4ccccc34)[C@@H]2C1)S(=O)(=O)CCO 10.1021/jm00150a002
14004039 119043 3 None -5 2 Bovine 6.0 pKi = 6.0 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 193 0 0 2 2.8 c1cc2c(s1)C1CCCCN1CC2 10.1021/jm00398a025
CHEMBL346016 119043 3 None -5 2 Bovine 6.0 pKi = 6.0 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 193 0 0 2 2.8 c1cc2c(s1)C1CCCCN1CC2 10.1021/jm00398a025
10242469 31211 0 None - 1 Bovine 6.0 pKi = 6.0 Binding
In Vitro Alpha-1 adrenergic receptor binding affinity on calf frontal cortex membrane preparationIn Vitro Alpha-1 adrenergic receptor binding affinity on calf frontal cortex membrane preparation
ChEMBL 217 1 1 4 0.9 CN1CC(C2=NCCN2)Oc2ccccc21 10.1021/jm021050c
CHEMBL14028 31211 0 None - 1 Bovine 6.0 pKi = 6.0 Binding
In Vitro Alpha-1 adrenergic receptor binding affinity on calf frontal cortex membrane preparationIn Vitro Alpha-1 adrenergic receptor binding affinity on calf frontal cortex membrane preparation
ChEMBL 217 1 1 4 0.9 CN1CC(C2=NCCN2)Oc2ccccc21 10.1021/jm021050c
9887884 118767 42 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of alpha1A adrenergic receptor (unknown origin)Inhibition of alpha1A adrenergic receptor (unknown origin)
ChEMBL 412 4 0 3 5.1 O=C1c2ccccc2C(Cc2ccnc(F)c2)(Cc2ccnc(F)c2)c2ccccc21 10.1016/j.bmcl.2019.126681
CHEMBL343822 118767 42 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of alpha1A adrenergic receptor (unknown origin)Inhibition of alpha1A adrenergic receptor (unknown origin)
ChEMBL 412 4 0 3 5.1 O=C1c2ccccc2C(Cc2ccnc(F)c2)(Cc2ccnc(F)c2)c2ccccc21 10.1016/j.bmcl.2019.126681
10577609 26765 0 None -75 3 Human 6.0 pKi = 6.0 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 509 8 1 9 3.5 COc1cc2nc(N3CCN(C(=O)C(C)Oc4c(OC)cccc4C(C)C)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL136458 26765 0 None -75 3 Human 6.0 pKi = 6.0 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 509 8 1 9 3.5 COc1cc2nc(N3CCN(C(=O)C(C)Oc4c(OC)cccc4C(C)C)CC3)nc(N)c2cc1OC 10.1021/jm9805337
1935 3664 92 None -190 6 Rat 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 nan
2551 3664 92 None -190 6 Rat 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 nan
6687 3664 92 None -190 6 Rat 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 nan
CHEMBL95 3664 92 None -190 6 Rat 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 nan
DB00382 3664 92 None -190 6 Rat 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 nan
118717460 114631 0 None -2 4 Human 7.0 pKi = 7.0 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 412 10 2 4 6.9 Cc1ccc2c(NCCCCCCCNc3ccnc4cc(C)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343982 114631 0 None -2 4 Human 7.0 pKi = 7.0 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 412 10 2 4 6.9 Cc1ccc2c(NCCCCCCCNc3ccnc4cc(C)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
2419 687 22 None -288 12 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
9 687 22 None -288 12 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
CHEMBL13647 687 22 None -288 12 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
118717460 114631 0 None -2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 412 10 2 4 6.9 Cc1ccc2c(NCCCCCCCNc3ccnc4cc(C)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343982 114631 0 None -2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 412 10 2 4 6.9 Cc1ccc2c(NCCCCCCCNc3ccnc4cc(C)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
481 2836 5 None 4 3 Human 6.0 pKi = 6.0 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
9838763 2836 5 None 4 3 Human 6.0 pKi = 6.0 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
CHEMBL72958 2836 5 None 4 3 Human 6.0 pKi = 6.0 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
131829 203010 11 None -173 6 Human 6.0 pKi = 6.0 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 295 1 4 5 1.7 Brc1c(NC2=NCCN2)ccc2c1NCCN2 10.1016/0960-894X(95)00391-6
CHEMBL74283 203010 11 None -173 6 Human 6.0 pKi = 6.0 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 295 1 4 5 1.7 Brc1c(NC2=NCCN2)ccc2c1NCCN2 10.1016/0960-894X(95)00391-6
34458 97878 65 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 minsDisplacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 mins
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3C1C2)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL275097 97878 65 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 minsDisplacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 mins
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3C1C2)OCO4 10.1021/acs.jmedchem.6b01217
9892644 195660 0 None -30 4 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 511 4 0 4 4.0 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(Br)ccc2Br)CC1 10.1021/jm030944+
CHEMBL56899 195660 0 None -30 4 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 511 4 0 4 4.0 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(Br)ccc2Br)CC1 10.1021/jm030944+
9906978 42451 1 None -2 12 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 42451 1 None -2 12 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
10775000 106897 2 None -30 5 Bovine 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 214 1 2 2 2.6 Oc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL317912 106897 2 None -30 5 Bovine 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 214 1 2 2 2.6 Oc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
11301627 9293 0 None 1 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 319 4 2 3 3.0 CC(C)S(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL111537 9293 0 None 1 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 319 4 2 3 3.0 CC(C)S(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
11301627 9293 0 None 1 2 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 319 4 2 3 3.0 CC(C)S(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL111537 9293 0 None 1 2 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 319 4 2 3 3.0 CC(C)S(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
9922027 114898 0 None 1 3 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 289 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCC=C2c1c[nH]cn1 10.1021/jm030551a
CHEMBL3350265 114898 0 None 1 3 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 289 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCC=C2c1c[nH]cn1 10.1021/jm030551a
10835395 205072 0 None -7 2 Rat 6.9 pKi = 6.9 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 410 6 0 4 3.7 FC(F)(F)c1cccc(N2CCN(CCCCN3CC4CCCCN4C3)CC2)c1 10.1021/jm970216k
CHEMBL90384 205072 0 None -7 2 Rat 6.9 pKi = 6.9 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 410 6 0 4 3.7 FC(F)(F)c1cccc(N2CCN(CCCCN3CC4CCCCN4C3)CC2)c1 10.1021/jm970216k
3151 1429 93 None -147 27 Rat 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 1429 93 None -147 27 Rat 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 1429 93 None -147 27 Rat 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 1429 93 None -147 27 Rat 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 1429 93 None -147 27 Rat 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
127027974 137223 0 None -9 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 396 8 1 4 3.4 COc1ccccc1N1CCN(CCCCNC(=O)N(C)c2ccccc2)CC1 10.1016/j.bmcl.2015.12.068
CHEMBL3759312 137223 0 None -9 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 396 8 1 4 3.4 COc1ccccc1N1CCN(CCCCNC(=O)N(C)c2ccccc2)CC1 10.1016/j.bmcl.2015.12.068
46881493 6895 0 None -14 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 389 8 1 4 4.3 Cc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
CHEMBL1084658 6895 0 None -14 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 389 8 1 4 4.3 Cc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
9845172 168532 0 None -79 4 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 422 4 0 3 4.9 O=C1CC2(CCCC2)CC(=O)N1CCN1CCC(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL440118 168532 0 None -79 4 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 422 4 0 3 4.9 O=C1CC2(CCCC2)CC(=O)N1CCN1CCC(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
11584530 15908 0 None -158 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 454 8 1 4 5.8 FC(F)(F)c1cccc(N2CCN(CCCCNc3cc(-c4ccccc4)ccn3)CC2)c1 10.1016/j.bmcl.2010.07.096
CHEMBL1223857 15908 0 None -158 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 454 8 1 4 5.8 FC(F)(F)c1cccc(N2CCN(CCCCNc3cc(-c4ccccc4)ccn3)CC2)c1 10.1016/j.bmcl.2010.07.096
9929936 167338 0 None -11 5 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 383 4 0 4 3.1 Cc1ccc(C)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1021/jm030944+
CHEMBL431354 167338 0 None -11 5 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 383 4 0 4 3.1 Cc1ccc(C)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1021/jm030944+
9822812 194189 0 None -45 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 409 4 0 4 3.4 O=C1CC2(CCC2)CC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL55882 194189 0 None -45 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 409 4 0 4 3.4 O=C1CC2(CCC2)CC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
11857862 141510 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 538 10 1 6 4.8 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCC(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL387833 141510 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 538 10 1 6 4.8 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCC(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
44431607 87042 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 509 7 1 5 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cccc(Cl)c3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL233407 87042 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 509 7 1 5 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cccc(Cl)c3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
11857794 85227 0 None 5 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 562 9 1 5 5.7 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1cccc(OC(F)F)c1 10.1016/j.bmcl.2007.04.098
CHEMBL228553 85227 0 None 5 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 562 9 1 5 5.7 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1cccc(OC(F)F)c1 10.1016/j.bmcl.2007.04.098
11857862 141510 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 538 10 1 6 4.8 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCC(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL387833 141510 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 538 10 1 6 4.8 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCC(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
4038180 202 11 None 2 6 Rat 7.9 pKi = 7.9 Binding
Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.009 - 0.015)Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.009 - 0.015)
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm025550h
480 202 11 None 2 6 Rat 7.9 pKi = 7.9 Binding
Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.009 - 0.015)Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.009 - 0.015)
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm025550h
CHEMBL109783 202 11 None 2 6 Rat 7.9 pKi = 7.9 Binding
Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.009 - 0.015)Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.009 - 0.015)
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm025550h
44308466 202083 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 429 7 0 7 3.2 COC(=O)[C@@H]1CCCN1Cc1ccc(CN2CCN(c3ccccc3OC)CC2)s1 10.1016/s0960-894x(02)00347-5
CHEMBL68241 202083 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 429 7 0 7 3.2 COC(=O)[C@@H]1CCCN1Cc1ccc(CN2CCN(c3ccccc3OC)CC2)s1 10.1016/s0960-894x(02)00347-5
68604 77818 25 None -12 6 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-WB4101 from rat forebrain homogenate alpha 1 adrenergic receptorDisplacement of [3H]-WB4101 from rat forebrain homogenate alpha 1 adrenergic receptor
ChEMBL 401 5 0 6 2.9 Cc1nc2n(c(=O)c1CCN1CCC(C(=O)c3ccc(F)cc3)CC1)CCS2 10.1021/acs.jmedchem.2c00633
CHEMBL2105437 77818 25 None -12 6 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-WB4101 from rat forebrain homogenate alpha 1 adrenergic receptorDisplacement of [3H]-WB4101 from rat forebrain homogenate alpha 1 adrenergic receptor
ChEMBL 401 5 0 6 2.9 Cc1nc2n(c(=O)c1CCN1CCC(C(=O)c3ccc(F)cc3)CC1)CCS2 10.1021/acs.jmedchem.2c00633
11590801 15859 0 None -7 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 428 7 1 4 5.3 FC(F)(F)c1cccc(N2CCN(CCCCNc3ccc4ccccc4n3)CC2)c1 10.1016/j.bmcl.2010.07.096
CHEMBL1223747 15859 0 None -7 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 428 7 1 4 5.3 FC(F)(F)c1cccc(N2CCN(CCCCNc3ccc4ccccc4n3)CC2)c1 10.1016/j.bmcl.2010.07.096
2142 3035 54 None -2 37 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2018.04.059
4920903 3035 54 None -2 37 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2018.04.059
502 3035 54 None -2 37 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2018.04.059
5775 3035 54 None -2 37 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2018.04.059
CHEMBL597 3035 54 None -2 37 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2018.04.059
DB00692 3035 54 None -2 37 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2018.04.059
10745664 121489 0 None 12 3 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 572 8 2 8 3.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3cccc([N+](=O)[O-])c3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL359433 121489 0 None 12 3 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 572 8 2 8 3.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3cccc([N+](=O)[O-])c3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
44289344 167970 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 441 8 1 3 4.8 Cc1ccc(C(C(=O)NCCCN2CCN(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
CHEMBL435576 167970 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 441 8 1 3 4.8 Cc1ccc(C(C(=O)NCCCN2CCN(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
3039881 173675 6 None -19 3 Human 7.9 pKi = 7.9 Binding
The compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligandThe compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligand
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL45491 173675 6 None -19 3 Human 7.9 pKi = 7.9 Binding
The compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligandThe compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligand
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
1443 1989 30 None -2 11 Bovine 7.9 pKi = 7.9 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
33625 1989 30 None -2 11 Bovine 7.9 pKi = 7.9 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
501 1989 30 None -2 11 Bovine 7.9 pKi = 7.9 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
CHEMBL279516 1989 30 None -2 11 Bovine 7.9 pKi = 7.9 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
DB08950 1989 30 None -2 11 Bovine 7.9 pKi = 7.9 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
4038180 202 11 None 2 6 Rat 7.9 pKi = 7.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
480 202 11 None 2 6 Rat 7.9 pKi = 7.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
CHEMBL109783 202 11 None 2 6 Rat 7.9 pKi = 7.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
118716721 114504 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 466 5 1 6 3.3 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)Nc4ccccc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342874 114504 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 466 5 1 6 3.3 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)Nc4ccccc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
4038180 202 11 None 2 6 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm030551a
480 202 11 None 2 6 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm030551a
CHEMBL109783 202 11 None 2 6 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm030551a
10644955 165623 7 None -1 3 Rat 7.9 pKi = 7.9 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 404 6 0 4 3.1 O=C1C2CCCCN2C(=O)N1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm970216k
CHEMBL42644 165623 7 None -1 3 Rat 7.9 pKi = 7.9 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 404 6 0 4 3.1 O=C1C2CCCCN2C(=O)N1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm970216k
9824384 118269 1 None -14 8 Human 7.9 pKi = 7.9 Binding
Compound was tested for binding affinity against human hippocampus Alpha-1A adrenergic receptor using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against human hippocampus Alpha-1A adrenergic receptor using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1021/jm960510x
CHEMBL342062 118269 1 None -14 8 Human 7.9 pKi = 7.9 Binding
Compound was tested for binding affinity against human hippocampus Alpha-1A adrenergic receptor using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against human hippocampus Alpha-1A adrenergic receptor using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1021/jm960510x
10252540 84919 1 None -58 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
CHEMBL2261604 84919 1 None -58 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
132266 1247 9 None -48 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2007.01.028
486 1247 9 None -48 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2007.01.028
CHEMBL423294 1247 9 None -48 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2007.01.028
132266 1247 9 None -48 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2018.05.023
486 1247 9 None -48 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2018.05.023
CHEMBL423294 1247 9 None -48 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1016/j.bmc.2018.05.023
52948119 16472 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 451 7 0 6 2.7 COc1ccccc1N1CCN(C[C@@H]2CO[C@](CN3CCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242445 16472 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 451 7 0 6 2.7 COc1ccccc1N1CCN(C[C@@H]2CO[C@](CN3CCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
118716723 114506 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 446 4 1 6 2.5 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)NC(C)(C)C)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342876 114506 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 446 4 1 6 2.5 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)NC(C)(C)C)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
44288162 168422 0 None -2 3 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1ccc2c(c1)C1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC1CC2 10.1021/jm990567u
CHEMBL43921 168422 0 None -2 3 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1ccc2c(c1)C1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC1CC2 10.1021/jm990567u
10622830 101940 0 None 5 3 Rat 7.9 pKi = 7.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 437 6 1 6 3.2 COc1cc2c(cc1OC)C(=O)N(CCN1C[C@@H]3CCc4c(OC)cccc4[C@@H]3C1)CN2 10.1021/jm000541z
CHEMBL303988 101940 0 None 5 3 Rat 7.9 pKi = 7.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 437 6 1 6 3.2 COc1cc2c(cc1OC)C(=O)N(CCN1C[C@@H]3CCc4c(OC)cccc4[C@@H]3C1)CN2 10.1021/jm000541z
118717456 114625 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 342 5 2 4 4.9 Cc1ccc2c(NCCNc3ccnc4cc(C)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343977 114625 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 342 5 2 4 4.9 Cc1ccc2c(NCCNc3ccnc4cc(C)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
9797396 12757 0 None -39 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 325 5 1 2 4.2 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
CHEMBL1188811 12757 0 None -39 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 325 5 1 2 4.2 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
CHEMBL537428 12757 0 None -39 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 325 5 1 2 4.2 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
9797396 12757 0 None -39 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 325 5 1 2 4.2 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
CHEMBL1188811 12757 0 None -39 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 325 5 1 2 4.2 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
CHEMBL537428 12757 0 None -39 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 325 5 1 2 4.2 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
44586430 186437 0 None 3 3 Rat 6.9 pKi = 6.9 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 528 9 1 6 3.4 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL490865 186437 0 None 3 3 Rat 6.9 pKi = 6.9 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 528 9 1 6 3.4 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
155525650 176054 0 None -22 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 9 1 4 4.2 c1ccc(OCCNC[C@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4457585 176054 0 None -22 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 9 1 4 4.2 c1ccc(OCCNC[C@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4597956 176054 0 None -22 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 9 1 4 4.2 c1ccc(OCCNC[C@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
118717456 114625 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 342 5 2 4 4.9 Cc1ccc2c(NCCNc3ccnc4cc(C)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343977 114625 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 342 5 2 4 4.9 Cc1ccc2c(NCCNc3ccnc4cc(C)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
145949210 162187 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 459 5 2 9 2.8 COc1cc2nc(N3CCC[C@@H](NC4=CC(=O)c5ccccc5C4=O)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
CHEMBL4171491 162187 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 459 5 2 9 2.8 COc1cc2nc(N3CCC[C@@H](NC4=CC(=O)c5ccccc5C4=O)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
145946292 166932 0 None -19 2 Human 5.9 pKi = 5.9 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 382 6 2 5 2.9 CNc1ccc2c(c1)[C@H](NCCOc1cc(F)ccc1F)CCS2(=O)=O 10.1016/j.ejmech.2017.07.071
CHEMBL4210954 166932 0 None -19 2 Human 5.9 pKi = 5.9 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 382 6 2 5 2.9 CNc1ccc2c(c1)[C@H](NCCOc1cc(F)ccc1F)CCS2(=O)=O 10.1016/j.ejmech.2017.07.071
CHEMBL4299802 166932 0 None -19 2 Human 5.9 pKi = 5.9 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 382 6 2 5 2.9 CNc1ccc2c(c1)[C@H](NCCOc1cc(F)ccc1F)CCS2(=O)=O 10.1016/j.ejmech.2017.07.071
12909389 60035 0 None 64 2 Bovine 5.9 pKi = 5.9 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 320 1 1 3 3.7 CN1CCC(=C2c3cc(C(=O)O)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL174649 60035 0 None 64 2 Bovine 5.9 pKi = 5.9 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 320 1 1 3 3.7 CN1CCC(=C2c3cc(C(=O)O)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
10221004 202521 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70973 202521 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
9953974 77465 0 None 5 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 421 4 0 7 3.3 COc1ccccc1N1CCN(C[C@@H]2CN=C3c4ccccc4N=C(SC)N32)CC1 10.1021/jm970159v
CHEMBL2092927 77465 0 None 5 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 421 4 0 7 3.3 COc1ccccc1N1CCN(C[C@@H]2CN=C3c4ccccc4N=C(SC)N32)CC1 10.1021/jm970159v
10694274 197334 0 None 1 3 Rat 6.9 pKi = 6.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 437 6 1 5 3.7 COc1cc2c(cc1OC)NC(=O)N(CCN1C[C@@H]3CCc4c(OC)cccc4[C@@H]3C1)C2 10.1021/jm000541z
CHEMBL58585 197334 0 None 1 3 Rat 6.9 pKi = 6.9 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 437 6 1 5 3.7 COc1cc2c(cc1OC)NC(=O)N(CCN1C[C@@H]3CCc4c(OC)cccc4[C@@H]3C1)C2 10.1021/jm000541z
4543 169972 36 None -24 30 Rat 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169972 36 None -24 30 Rat 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169972 36 None -24 30 Rat 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
9950711 108706 0 None 5 4 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 359 4 2 3 3.2 O=S(=O)(CC(F)(F)F)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL321644 108706 0 None 5 4 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 359 4 2 3 3.2 O=S(=O)(CC(F)(F)F)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
16655023 106942 1 None -102 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human cloned alpha-1A receptorDisplacement of [3H]prazosin from human cloned alpha-1A receptor
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmc.2007.03.053
CHEMBL318235 106942 1 None -102 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human cloned alpha-1A receptorDisplacement of [3H]prazosin from human cloned alpha-1A receptor
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmc.2007.03.053
9822477 197761 0 None -43 5 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 403 4 0 4 3.5 Cc1ccc(Cl)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1021/jm030944+
CHEMBL59149 197761 0 None -43 5 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 403 4 0 4 3.5 Cc1ccc(Cl)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1021/jm030944+
11183468 109371 2 None -2 6 Rat 6.9 pKi = 6.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 213 1 2 2 2.5 Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL323402 109371 2 None -2 6 Rat 6.9 pKi = 6.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 213 1 2 2 2.5 Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
52937526 60958 0 None -1258 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 363 5 0 5 3.1 COc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
CHEMBL1767137 60958 0 None -1258 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 363 5 0 5 3.1 COc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
24803798 60981 0 None -501 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 640 12 0 6 7.9 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
CHEMBL1767160 60981 0 None -501 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 640 12 0 6 7.9 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
218362 203082 5 None -75 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 216 1 1 3 2.0 c1ccc2c(c1)CCCC2NC1=NCCO1 10.1016/0960-894X(94)85032-1
CHEMBL75030 203082 5 None -75 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 216 1 1 3 2.0 c1ccc2c(c1)CCCC2NC1=NCCO1 10.1016/0960-894X(94)85032-1
151779 193027 1 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 384 10 2 4 6.3 c1ccc2c(NCCCCCCCNc3ccnc4ccccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL533979 193027 1 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 384 10 2 4 6.3 c1ccc2c(NCCCCCCCNc3ccnc4ccccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
127040061 136390 0 None -33 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNC[C@H]2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1039/C4MD00484A
CHEMBL3739932 136390 0 None -33 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNC[C@H]2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1039/C4MD00484A
CHEMBL3742489 136390 0 None -33 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNC[C@H]2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1039/C4MD00484A
127036186 136876 0 None -39 19 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3753318 136876 0 None -39 19 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
127026052 137015 0 None -75 19 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 137015 0 None -75 19 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
183528 168125 5 None -16 2 Human 4.9 pKi = 4.9 Binding
Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 420 3 4 3 4.7 O=C(c1nc(-c2c[nH]c3cc(Br)ccc23)c[nH]1)c1c[nH]c2cc(O)ccc12 10.1016/0960-894X(96)00376-9
CHEMBL436760 168125 5 None -16 2 Human 4.9 pKi = 4.9 Binding
Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 420 3 4 3 4.7 O=C(c1nc(-c2c[nH]c3cc(Br)ccc23)c[nH]1)c1c[nH]c2cc(O)ccc12 10.1016/0960-894X(96)00376-9
151779 193027 1 None 1 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 384 10 2 4 6.3 c1ccc2c(NCCCCCCCNc3ccnc4ccccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL533979 193027 1 None 1 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 384 10 2 4 6.3 c1ccc2c(NCCCCCCCNc3ccnc4ccccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
44328739 205907 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 691 16 3 6 7.5 CCCCCC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCC)=C(CC)N1 10.1016/s0960-894x(99)00484-9
CHEMBL95263 205907 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 691 16 3 6 7.5 CCCCCC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCC)=C(CC)N1 10.1016/s0960-894x(99)00484-9
1376848 202052 8 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 366 4 0 4 3.8 COc1ccccc1N1CCN(Cc2ccc(Br)s2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL67932 202052 8 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 366 4 0 4 3.8 COc1ccccc1N1CCN(Cc2ccc(Br)s2)CC1 10.1016/s0960-894x(02)00347-5
9954092 194961 0 None -1000 6 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 423 4 0 4 3.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL56438 194961 0 None -1000 6 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 423 4 0 4 3.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
9903797 9333 5 None 18 4 Rat 6.9 pKi = 6.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 279 5 2 3 2.1 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1C 10.1007/s00044-004-0020-z
CHEMBL111734 9333 5 None 18 4 Rat 6.9 pKi = 6.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 279 5 2 3 2.1 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1C 10.1007/s00044-004-0020-z
25181489 186764 0 None -158 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNC[C@@H]2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm301525w
CHEMBL493285 186764 0 None -158 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNC[C@@H]2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm301525w
9903797 9333 5 None 18 4 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 279 5 2 3 2.1 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1C 10.1021/jm030551a
CHEMBL111734 9333 5 None 18 4 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 279 5 2 3 2.1 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1C 10.1021/jm030551a
11747739 13109 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1191324 13109 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL542402 13109 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44267890 16315 0 None 41 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 460 8 1 5 2.0 O=C(CN1CCCCC1=O)NCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL12364 16315 0 None 41 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 460 8 1 5 2.0 O=C(CN1CCCCC1=O)NCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(00)00169-4
44460394 203657 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 398 7 0 6 2.9 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3CCCC3=O)co2)CC1 10.1016/s0960-894x(02)00436-5
CHEMBL79940 203657 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 398 7 0 6 2.9 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3CCCC3=O)co2)CC1 10.1016/s0960-894x(02)00436-5
9959671 32437 0 None 363 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 0 7 5.6 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL141322 32437 0 None 363 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 0 7 5.6 COC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
15054189 193901 0 None 23 3 Rat 7.9 pKi = 7.9 Binding
Binding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranesBinding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranes
ChEMBL 433 6 2 6 2.4 COc1ccccc1N1CCN(CCCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1021/jm00110a014
CHEMBL55528 193901 0 None 23 3 Rat 7.9 pKi = 7.9 Binding
Binding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranesBinding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranes
ChEMBL 433 6 2 6 2.4 COc1ccccc1N1CCN(CCCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1021/jm00110a014
2389 3267 114 None -7 68 Rat 7.9 pKi = 7.9 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
5073 3267 114 None -7 68 Rat 7.9 pKi = 7.9 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
96 3267 114 None -7 68 Rat 7.9 pKi = 7.9 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
CHEMBL85 3267 114 None -7 68 Rat 7.9 pKi = 7.9 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
DB00734 3267 114 None -7 68 Rat 7.9 pKi = 7.9 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
10623356 167555 0 None -8 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 448 7 0 5 4.0 COc1ccccc1N1CCN(CCN(C(=O)c2ccc(F)c(C)c2)c2ccccn2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL1910243 167555 0 None -8 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 448 7 0 5 4.0 COc1ccccc1N1CCN(CCN(C(=O)c2ccc(F)c(C)c2)c2ccccn2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL43297 167555 0 None -8 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 448 7 0 5 4.0 COc1ccccc1N1CCN(CCN(C(=O)c2ccc(F)c(C)c2)c2ccccn2)CC1 10.1021/acs.jmedchem.2c00633
2274 3112 53 None -6 32 Rat 7.9 pKi = 7.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3112 53 None -6 32 Rat 7.9 pKi = 7.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3112 53 None -6 32 Rat 7.9 pKi = 7.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3112 53 None -6 32 Rat 7.9 pKi = 7.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3112 53 None -6 32 Rat 7.9 pKi = 7.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
44331136 109180 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 540 7 1 5 5.8 O=C1CC2(CCN(CCc3cccc4ccccc34)CC2)Oc2ccc(NS(=O)(=O)Cc3ccccc3)cc21 10.1016/s0960-894x(98)00732-x
CHEMBL322688 109180 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 540 7 1 5 5.8 O=C1CC2(CCN(CCc3cccc4ccccc34)CC2)Oc2ccc(NS(=O)(=O)Cc3ccccc3)cc21 10.1016/s0960-894x(98)00732-x
13141184 165326 0 None 17 2 Bovine 7.9 pKi = 7.9 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 376 1 0 3 5.6 CN1CCC(=C2c3cc(SC(F)(F)F)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL424967 165326 0 None 17 2 Bovine 7.9 pKi = 7.9 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 376 1 0 3 5.6 CN1CCC(=C2c3cc(SC(F)(F)F)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
57402365 68938 0 None 10 5 Pig 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928119 68938 0 None 10 5 Pig 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
11393666 192374 0 None -33 19 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 192374 0 None -33 19 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 192374 0 None -33 19 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
53779053 78013 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Tested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assayTested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assay
ChEMBL 475 6 1 4 5.0 C[C@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H]1c1ccc(F)c(F)c1 10.1016/s0960-894x(00)00524-2
CHEMBL2111563 78013 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Tested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assayTested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assay
ChEMBL 475 6 1 4 5.0 C[C@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H]1c1ccc(F)c(F)c1 10.1016/s0960-894x(00)00524-2
124 2921 44 None -14 33 Bovine 7.9 pKi = 7.9 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
2032 2921 44 None -14 33 Bovine 7.9 pKi = 7.9 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
4636 2921 44 None -14 33 Bovine 7.9 pKi = 7.9 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
CHEMBL762 2921 44 None -14 33 Bovine 7.9 pKi = 7.9 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
DB00935 2921 44 None -14 33 Bovine 7.9 pKi = 7.9 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
10623356 167555 0 None -8 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to alpha1A receptorBinding affinity to alpha1A receptor
ChEMBL 448 7 0 5 4.0 COc1ccccc1N1CCN(CCN(C(=O)c2ccc(F)c(C)c2)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910243 167555 0 None -8 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to alpha1A receptorBinding affinity to alpha1A receptor
ChEMBL 448 7 0 5 4.0 COc1ccccc1N1CCN(CCN(C(=O)c2ccc(F)c(C)c2)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL43297 167555 0 None -8 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to alpha1A receptorBinding affinity to alpha1A receptor
ChEMBL 448 7 0 5 4.0 COc1ccccc1N1CCN(CCN(C(=O)c2ccc(F)c(C)c2)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
44431618 144359 0 None 3 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 488 8 1 7 3.3 COc1ccncc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL391017 144359 0 None 3 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 488 8 1 7 3.3 COc1ccncc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
2470 3583 46 None -316 60 Bovine 7.9 pKi = 7.9 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm960510x
3300 3583 46 None -316 60 Bovine 7.9 pKi = 7.9 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm960510x
5265 3583 46 None -316 60 Bovine 7.9 pKi = 7.9 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm960510x
99 3583 46 None -316 60 Bovine 7.9 pKi = 7.9 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm960510x
CHEMBL267930 3583 46 None -316 60 Bovine 7.9 pKi = 7.9 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm960510x
44447010 153694 0 None -4 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 496 6 1 5 5.4 Cc1ccc(C(=O)NC2CCc3ccc(CCN4CCN(c5nsc6ccccc56)CC4)cc32)cc1 10.1016/j.bmcl.2007.11.106
CHEMBL398618 153694 0 None -4 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 496 6 1 5 5.4 Cc1ccc(C(=O)NC2CCc3ccc(CCN4CCN(c5nsc6ccccc56)CC4)cc32)cc1 10.1016/j.bmcl.2007.11.106
44431545 144475 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 457 7 1 5 3.9 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL391107 144475 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 457 7 1 5 3.9 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
2419 687 22 None -275 12 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
9 687 22 None -275 12 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
CHEMBL13647 687 22 None -275 12 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
9954092 194961 0 None -1000 6 Human 6.9 pKi = 6.9 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 423 4 0 4 3.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1016/j.bmcl.2004.11.032
CHEMBL56438 194961 0 None -1000 6 Human 6.9 pKi = 6.9 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 423 4 0 4 3.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1016/j.bmcl.2004.11.032
145946376 166946 0 None -426 3 Human 6.9 pKi = 6.9 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 382 6 2 5 2.9 CNc1ccc2c(c1)[C@@H](NCCOc1cc(F)ccc1F)CCS2(=O)=O 10.1016/j.ejmech.2017.07.071
CHEMBL4207824 166946 0 None -426 3 Human 6.9 pKi = 6.9 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 382 6 2 5 2.9 CNc1ccc2c(c1)[C@@H](NCCOc1cc(F)ccc1F)CCS2(=O)=O 10.1016/j.ejmech.2017.07.071
CHEMBL4299993 166946 0 None -426 3 Human 6.9 pKi = 6.9 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 382 6 2 5 2.9 CNc1ccc2c(c1)[C@@H](NCCOc1cc(F)ccc1F)CCS2(=O)=O 10.1016/j.ejmech.2017.07.071
12909383 130168 1 None 5 2 Bovine 6.9 pKi = 6.9 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 278 0 0 2 3.6 CN1CCC(=C2c3ccccc3CCn3cccc32)CC1 10.1021/jm00361a008
CHEMBL368413 130168 1 None 5 2 Bovine 6.9 pKi = 6.9 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 278 0 0 2 3.6 CN1CCC(=C2c3ccccc3CCn3cccc32)CC1 10.1021/jm00361a008
9929458 122533 0 None -61 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 373 5 1 2 4.8 c1ccc2c(c1)CCN(CCCN1CCC(c3c[nH]c4ccccc34)CC1)C2 10.1016/j.bmcl.2015.07.046
CHEMBL3609359 122533 0 None -61 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 373 5 1 2 4.8 c1ccc2c(c1)CCN(CCCN1CCC(c3c[nH]c4ccccc34)CC1)C2 10.1016/j.bmcl.2015.07.046
11169638 16997 0 None -1 3 Rat 6.9 pKi = 6.9 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 600 11 1 8 3.3 CCOC(=O)C(C)N1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL1256344 16997 0 None -1 3 Rat 6.9 pKi = 6.9 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 600 11 1 8 3.3 CCOC(=O)C(C)N1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
9838192 110811 13 None -2 6 Rat 6.9 pKi = 6.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1007/s00044-004-0020-z
CHEMBL326702 110811 13 None -2 6 Rat 6.9 pKi = 6.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1007/s00044-004-0020-z
118717455 114624 0 None -7 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 342 5 2 4 4.9 Cc1ccc2nccc(NCCNc3ccnc4ccc(C)cc34)c2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343976 114624 0 None -7 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 342 5 2 4 4.9 Cc1ccc2nccc(NCCNc3ccnc4ccc(C)cc34)c2c1 10.1016/j.bmc.2014.09.017
9838192 110811 13 None -2 6 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1021/jm030551a
CHEMBL326702 110811 13 None -2 6 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1021/jm030551a
3034396 101155 33 None -22 17 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 mins
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.9b01465
CHEMBL299031 101155 33 None -22 17 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 mins
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.9b01465
9815005 109160 0 None 1 3 Rat 5.9 pKi = 5.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 305 3 2 3 2.6 CS(=O)(=O)Nc1cccc2c1CCCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL322492 109160 0 None 1 3 Rat 5.9 pKi = 5.9 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 305 3 2 3 2.6 CS(=O)(=O)Nc1cccc2c1CCCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
9815005 109160 0 None 1 3 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 305 3 2 3 2.6 CS(=O)(=O)Nc1cccc2c1CCCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL322492 109160 0 None 1 3 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 305 3 2 3 2.6 CS(=O)(=O)Nc1cccc2c1CCCCC2c1c[nH]cn1 10.1021/jm030551a
118717455 114624 0 None -7 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 342 5 2 4 4.9 Cc1ccc2nccc(NCCNc3ccnc4ccc(C)cc34)c2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343976 114624 0 None -7 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 342 5 2 4 4.9 Cc1ccc2nccc(NCCNc3ccnc4ccc(C)cc34)c2c1 10.1016/j.bmc.2014.09.017
9908478 193953 0 None -954 8 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 391 4 0 4 2.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)ccc2F)CC1 10.1021/jm030944+
CHEMBL556313 193953 0 None -954 8 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 391 4 0 4 2.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)ccc2F)CC1 10.1021/jm030944+
196129 67441 12 None -1698 15 Rat 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67441 12 None -1698 15 Rat 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
9938248 101723 0 None -1 3 Rat 6.9 pKi = 6.9 Binding
Binding affinity was determined against Alpha-1a adrenergic receptorBinding affinity was determined against Alpha-1a adrenergic receptor
ChEMBL 580 2 4 3 6.0 CN1C[C@H](c2c[nH]c3c(Br)c(Br)cc(O)c23)NC[C@H]1c1c[nH]c2cc(Br)ccc12 10.1016/0960-894X(96)00376-9
CHEMBL302882 101723 0 None -1 3 Rat 6.9 pKi = 6.9 Binding
Binding affinity was determined against Alpha-1a adrenergic receptorBinding affinity was determined against Alpha-1a adrenergic receptor
ChEMBL 580 2 4 3 6.0 CN1C[C@H](c2c[nH]c3c(Br)c(Br)cc(O)c23)NC[C@H]1c1c[nH]c2cc(Br)ccc12 10.1016/0960-894X(96)00376-9
11183468 109371 2 None -2 6 Bovine 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 213 1 2 2 2.5 Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL323402 109371 2 None -2 6 Bovine 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 213 1 2 2 2.5 Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
6918539 143675 2 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 minsDisplacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 mins
ChEMBL 361 2 2 5 3.4 COc1cc2c(cc1O)[C@@H]1Cc3c(Cl)cc(OC)c(O)c3CN1CC2 10.1021/acs.jmedchem.6b01217
CHEMBL3904484 143675 2 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 minsDisplacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 mins
ChEMBL 361 2 2 5 3.4 COc1cc2c(cc1O)[C@@H]1Cc3c(Cl)cc(OC)c(O)c3CN1CC2 10.1021/acs.jmedchem.6b01217
11173600 162816 0 None - 1 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 282 5 2 3 2.1 CCS(=O)(=O)Nc1cccc2c1CCCC2CNC 10.1021/jm030551a
CHEMBL419369 162816 0 None - 1 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 282 5 2 3 2.1 CCS(=O)(=O)Nc1cccc2c1CCCC2CNC 10.1021/jm030551a
CHEMBL4752561 212269 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000739a ADRA1ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000739a ADRA1A
ChEMBL None None None COc1cc(-c2cn([C@H]3CCc4ccccc4N(CC(F)(F)F)C3=O)nn2)ccc1-n1ccc(C)n1 nan
10745566 34080 0 None 61 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 566 10 1 6 5.1 CNC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)cc1F 10.1021/jm9902032
CHEMBL142719 34080 0 None 61 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 566 10 1 6 5.1 CNC(=O)C1=C(C)N=C(C)N(CCCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)cc1F 10.1021/jm9902032
44431553 87142 0 None -10 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 525 7 1 5 4.9 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL233592 87142 0 None -10 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 525 7 1 5 4.9 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
44426404 85186 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 498 7 1 6 4.4 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2007.04.098
CHEMBL228333 85186 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 498 7 1 6 4.4 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2007.04.098
18738387 162934 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 399 6 0 5 3.6 COc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)s2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL420184 162934 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 399 6 0 5 3.6 COc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)s2)CC1 10.1016/s0960-894x(02)00347-5
16041628 154799 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccc(F)cc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL403280 154799 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccc(F)cc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
49865640 15843 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 324 7 1 4 3.4 Cc1ccccc1N1CCN(CCCCNc2ccccn2)CC1 10.1016/j.bmcl.2010.07.096
CHEMBL1223681 15843 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 324 7 1 4 3.4 Cc1ccccc1N1CCN(CCCCNc2ccccn2)CC1 10.1016/j.bmcl.2010.07.096
57390117 68942 0 None 16 5 Pig 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928123 68942 0 None 16 5 Pig 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
145946714 166986 0 None 2 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4213352 166986 0 None 2 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4300399 166986 0 None 2 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
10578735 120594 0 None 28 3 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 557 8 2 7 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccc(OC)cc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL357439 120594 0 None 28 3 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 557 8 2 7 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccc(OC)cc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
53328508 63052 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 466 8 0 7 3.0 COc1ccccc1N1CCN(CCCN2C(=O)CC(c3ccc([N+](=O)[O-])cc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796042 63052 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 466 8 0 7 3.0 COc1ccccc1N1CCN(CCCN2C(=O)CC(c3ccc([N+](=O)[O-])cc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
44431620 86625 0 None -102 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 570 7 1 6 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cnc(Cl)c(Br)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL232609 86625 0 None -102 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 570 7 1 6 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cnc(Cl)c(Br)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
11782656 28855 0 None -75 6 Human 7.8 pKi = 7.8 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 336 9 1 4 3.8 COc1cccc2c(CCCNCCOc3ccccn3)cccc12 10.1021/jm010866v
CHEMBL138109 28855 0 None -75 6 Human 7.8 pKi = 7.8 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 336 9 1 4 3.8 COc1cccc2c(CCCNCCOc3ccccn3)cccc12 10.1021/jm010866v
10793963 99198 0 None 9 6 Human 7.8 pKi = 7.8 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 622 11 2 7 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL284470 99198 0 None 9 6 Human 7.8 pKi = 7.8 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 622 11 2 7 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
10793963 84832 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 622 11 2 7 6.0 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL2260147 84832 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 622 11 2 7 6.0 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
9838192 110811 13 None -2 6 Rat 6.9 pKi = 6.9 Binding
Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.12 - 0.15)Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.12 - 0.15)
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1021/jm025550h
CHEMBL326702 110811 13 None -2 6 Rat 6.9 pKi = 6.9 Binding
Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.12 - 0.15)Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (0.12 - 0.15)
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1021/jm025550h
9938248 101723 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 580 2 4 3 6.0 CN1C[C@H](c2c[nH]c3c(Br)c(Br)cc(O)c23)NC[C@H]1c1c[nH]c2cc(Br)ccc12 10.1016/0960-894X(96)00376-9
CHEMBL302882 101723 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 580 2 4 3 6.0 CN1C[C@H](c2c[nH]c3c(Br)c(Br)cc(O)c23)NC[C@H]1c1c[nH]c2cc(Br)ccc12 10.1016/0960-894X(96)00376-9
12909388 60716 0 None 14 2 Bovine 6.9 pKi = 6.9 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 303 0 0 3 3.4 CN1CCC(=C2c3cc(C#N)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
CHEMBL176365 60716 0 None 14 2 Bovine 6.9 pKi = 6.9 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 303 0 0 3 3.4 CN1CCC(=C2c3cc(C#N)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
6604117 187254 6 None -1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL2062340 187254 6 None -1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL49623 187254 6 None -1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
122187555 122526 0 None -3 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 324 5 1 1 5.7 c1ccc2c(C3CCN(CCCC4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
CHEMBL3609352 122526 0 None -3 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 324 5 1 1 5.7 c1ccc2c(C3CCN(CCCC4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
9845181 206410 1 None -1445 15 Human 4.9 pKi = 4.9 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm0491391
CHEMBL98241 206410 1 None -1445 15 Human 4.9 pKi = 4.9 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm0491391
44314198 103920 0 None -95 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCCC1NC1=NCCO1 10.1016/0960-894X(94)85032-1
CHEMBL310335 103920 0 None -95 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCCC1NC1=NCCO1 10.1016/0960-894X(94)85032-1
155557696 175855 0 None -30 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 377 11 2 4 3.8 OCC(CNCCOc1ccccc1)OC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.05.024
CHEMBL4558985 175855 0 None -30 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 377 11 2 4 3.8 OCC(CNCCOc1ccccc1)OC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.05.024
CHEMBL4596295 175855 0 None -30 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 377 11 2 4 3.8 OCC(CNCCOc1ccccc1)OC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.05.024
2477 732 54 None -218 29 Rat 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
36 732 54 None -218 29 Rat 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
437 732 54 None -218 29 Rat 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
CHEMBL49 732 54 None -218 29 Rat 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
DB00490 732 54 None -218 29 Rat 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
44311789 203018 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 345 1 2 5 3.1 Brc1c(NC2=N[C@@H]3CCCC[C@@H]3N2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL74342 203018 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 345 1 2 5 3.1 Brc1c(NC2=N[C@@H]3CCCC[C@@H]3N2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
92766 106047 30 None 1 6 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@H]12 10.1021/jm00019a001
CHEMBL31410 106047 30 None 1 6 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@H]12 10.1021/jm00019a001
191 399 92 None -107 29 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 399 92 None -107 29 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 399 92 None -107 29 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 399 92 None -107 29 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 399 92 None -107 29 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
10804826 23397 1 None -1 4 Bovine 5.8 pKi = 5.8 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL133451 23397 1 None -1 4 Bovine 5.8 pKi = 5.8 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
3823 49936 38 None -3019 11 Rat 4.8 pKi = 4.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
76973198 49936 38 None -3019 11 Rat 4.8 pKi = 4.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL157101 49936 38 None -3019 11 Rat 4.8 pKi = 4.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
44582676 189177 0 None -44 18 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned alpha1A adrenergic receptor by competitive binding experimentInhibition of human cloned alpha1A adrenergic receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 189177 0 None -44 18 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned alpha1A adrenergic receptor by competitive binding experimentInhibition of human cloned alpha1A adrenergic receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
19085836 203942 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 469 6 0 7 3.2 Cc1cccc2oc(=O)n(C3CCN(CCCCN4C(=O)c5ccccc5S4(=O)=O)CC3)c12 10.1016/s0960-894x(98)00446-6
CHEMBL82056 203942 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 469 6 0 7 3.2 Cc1cccc2oc(=O)n(C3CCN(CCCCN4C(=O)c5ccccc5S4(=O)=O)CC3)c12 10.1016/s0960-894x(98)00446-6
11140345 202461 0 None 1 6 Human 6.8 pKi = 6.8 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70692 202461 0 None 1 6 Human 6.8 pKi = 6.8 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
9900133 8882 0 None -1 4 Bovine 6.8 pKi = 6.8 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 271 2 2 3 3.1 COC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL109827 8882 0 None -1 4 Bovine 6.8 pKi = 6.8 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 271 2 2 3 3.1 COC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
185076 186497 4 None -389 7 Human 5.8 pKi = 5.8 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL49137 186497 4 None -389 7 Human 5.8 pKi = 5.8 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
13298529 100736 50 None -134 2 Bovine 5.8 pKi = 5.8 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 241 1 1 3 1.3 Brc1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL295921 100736 50 None -134 2 Bovine 5.8 pKi = 5.8 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 241 1 1 3 1.3 Brc1cccnc1N1CCNCC1 10.1021/jm00366a007
11464777 101322 0 None -363 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 437 4 0 4 4.2 CC(CN1CCN(c2cc(Cl)ccc2Cl)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1007/s00044-010-9379-1
CHEMBL300152 101322 0 None -363 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 437 4 0 4 4.2 CC(CN1CCN(c2cc(Cl)ccc2Cl)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1007/s00044-010-9379-1
9845181 206410 1 None -1445 15 Human 4.8 pKi = 4.8 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1016/s0960-894x(01)00159-7
CHEMBL98241 206410 1 None -1445 15 Human 4.8 pKi = 4.8 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1016/s0960-894x(01)00159-7
44433348 166784 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 545 10 0 7 4.6 CCN([C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1)S(=O)(=O)c1ccc(OC)c(OC)c1 10.1016/j.bmcl.2007.09.051
CHEMBL429453 166784 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 545 10 0 7 4.6 CCN([C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1)S(=O)(=O)c1ccc(OC)c(OC)c1 10.1016/j.bmcl.2007.09.051
135398737 942 89 None -5 92 Rat 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 942 89 None -5 92 Rat 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 942 89 None -5 92 Rat 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 942 89 None -5 92 Rat 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 942 89 None -5 92 Rat 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
44460423 203894 0 None 11 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 446 7 0 6 4.3 O=C1CCCCN1Cc1cc(CN2CCN(c3ccccc3Oc3ccccc3)CC2)on1 10.1016/s0960-894x(02)00436-5
CHEMBL81661 203894 0 None 11 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 446 7 0 6 4.3 O=C1CCCCN1Cc1cc(CN2CCN(c3ccccc3Oc3ccccc3)CC2)on1 10.1016/s0960-894x(02)00436-5
44431184 92404 0 None -2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 515 5 0 5 5.5 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4ccc5ccc(F)cc5c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
CHEMBL243866 92404 0 None -2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 515 5 0 5 5.5 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4ccc5ccc(F)cc5c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
44295218 188503 0 None 22 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 582 8 2 7 3.5 COC(=O)C1(c2ccccc2)CCN(CCCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
CHEMBL51019 188503 0 None 22 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 582 8 2 7 3.5 COC(=O)C1(c2ccccc2)CCN(CCCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
145947937 167151 0 None -3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4207653 167151 0 None -3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4302655 167151 0 None -3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
44447070 94195 0 None -9 4 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 500 6 1 5 5.2 O=C(NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21)c1ccc(F)cc1 10.1016/j.bmcl.2007.11.106
CHEMBL252429 94195 0 None -9 4 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 500 6 1 5 5.2 O=C(NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21)c1ccc(F)cc1 10.1016/j.bmcl.2007.11.106
124 2921 44 None -14 33 Human 7.8 pKi = 7.8 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
2032 2921 44 None -14 33 Human 7.8 pKi = 7.8 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
4636 2921 44 None -14 33 Human 7.8 pKi = 7.8 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
CHEMBL762 2921 44 None -14 33 Human 7.8 pKi = 7.8 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
DB00935 2921 44 None -14 33 Human 7.8 pKi = 7.8 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
52937222 60977 0 None -15 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 367 3 0 4 3.9 CN1CCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)CC1 10.1021/jm1013874
CHEMBL1767156 60977 0 None -15 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 367 3 0 4 3.9 CN1CCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)CC1 10.1021/jm1013874
10089254 99506 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 350 7 1 3 3.5 O=C(CCCN1CCC(NC(=O)c2ccccc2)CC1)c1ccccc1 10.1021/jm960697s
CHEMBL286591 99506 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 350 7 1 3 3.5 O=C(CCCN1CCC(NC(=O)c2ccccc2)CC1)c1ccccc1 10.1021/jm960697s
53328314 63044 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 439 7 0 4 4.2 O=C1CC(c2ccccc2)CC(=O)N1CCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796034 63044 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 439 7 0 4 4.2 O=C1CC(c2ccccc2)CC(=O)N1CCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.ejmech.2011.03.054
144096995 163933 0 None -17 3 Human 6.8 pKi = 6.8 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 371 8 1 4 3.1 CS(=O)(=O)c1ccccc1CCNCCOc1cc(F)ccc1Cl 10.1016/j.ejmech.2017.07.071
CHEMBL4214499 163933 0 None -17 3 Human 6.8 pKi = 6.8 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 371 8 1 4 3.1 CS(=O)(=O)c1ccccc1CCNCCOc1cc(F)ccc1Cl 10.1016/j.ejmech.2017.07.071
173712 123789 19 None -8 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 391 6 1 3 4.9 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
CHEMBL363548 123789 19 None -8 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 391 6 1 3 4.9 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
1862 161 14 None -1 7 Human 5.8 pKi = 5.8 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00118a019
510 161 14 None -1 7 Human 5.8 pKi = 5.8 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00118a019
CHEMBL281232 161 14 None -1 7 Human 5.8 pKi = 5.8 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00118a019
1960 2805 64 None -38 26 Human 5.8 pKi = 5.8 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
439260 2805 64 None -38 26 Human 5.8 pKi = 5.8 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
505 2805 64 None -38 26 Human 5.8 pKi = 5.8 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
CHEMBL1437 2805 64 None -38 26 Human 5.8 pKi = 5.8 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
DB00368 2805 64 None -38 26 Human 5.8 pKi = 5.8 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
18738412 203688 0 None 2 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 365 6 1 6 3.3 OCc1cc(CN2CCN(c3ccccc3Oc3ccccc3)CC2)on1 10.1016/s0960-894x(02)00436-5
CHEMBL80125 203688 0 None 2 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 365 6 1 6 3.3 OCc1cc(CN2CCN(c3ccccc3Oc3ccccc3)CC2)on1 10.1016/s0960-894x(02)00436-5
6603915 99507 25 None -446 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to alpha1A receptorBinding affinity to alpha1A receptor
ChEMBL 434 7 0 5 3.7 COc1ccccc1N1CCN(CCN(C(=O)c2ccc(F)cc2)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1775000 99507 25 None -446 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to alpha1A receptorBinding affinity to alpha1A receptor
ChEMBL 434 7 0 5 3.7 COc1ccccc1N1CCN(CCN(C(=O)c2ccc(F)cc2)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL286607 99507 25 None -446 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to alpha1A receptorBinding affinity to alpha1A receptor
ChEMBL 434 7 0 5 3.7 COc1ccccc1N1CCN(CCN(C(=O)c2ccc(F)cc2)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
2803 939 53 None -3 19 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
516 939 53 None -3 19 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
704 939 53 None -3 19 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
CHEMBL134 939 53 None -3 19 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
DB00575 939 53 None -3 19 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
11464777 101322 0 None -363 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 437 4 0 4 4.2 CC(CN1CCN(c2cc(Cl)ccc2Cl)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1007/s00044-010-9379-1
CHEMBL300152 101322 0 None -363 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 437 4 0 4 4.2 CC(CN1CCN(c2cc(Cl)ccc2Cl)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1007/s00044-010-9379-1
1220 186 46 None -407 45 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmcl.2010.01.030
31 186 46 None -407 45 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmcl.2010.01.030
7 186 46 None -407 45 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmcl.2010.01.030
CHEMBL56 186 46 None -407 45 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmcl.2010.01.030
1220 186 46 None -407 45 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm200421e
31 186 46 None -407 45 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm200421e
7 186 46 None -407 45 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm200421e
CHEMBL56 186 46 None -407 45 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm200421e
11201573 195970 0 None -3 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 442 5 0 6 1.6 COc1ccccc1N1CCN(CCN2C(=O)CC3(CCN(C(C)=O)CC3)CC2=O)CC1 10.1021/jm030944+
CHEMBL57097 195970 0 None -3 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 442 5 0 6 1.6 COc1ccccc1N1CCN(CCN2C(=O)CC3(CCN(C(C)=O)CC3)CC2=O)CC1 10.1021/jm030944+
127027077 137242 0 None -7585 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 403 7 2 4 3.9 O=C(NCCCCN1CCN(c2cccc(O)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
CHEMBL3759491 137242 0 None -7585 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 403 7 2 4 3.9 O=C(NCCCCN1CCN(c2cccc(O)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
10768423 100844 0 None 1 3 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 525 5 1 8 4.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5nc(-c6ccccc6)cnc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL296711 100844 0 None 1 3 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 525 5 1 8 4.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5nc(-c6ccccc6)cnc54)c3=O)C[C@@H]21 10.1021/jm990567u
16040907 97421 0 None -2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 466 7 2 5 4.7 COc1ccccc1NC(=O)NC1CCC(N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL272340 97421 0 None -2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 466 7 2 5 4.7 COc1ccccc1NC(=O)NC1CCC(N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.11.068
10577609 26765 0 None -10 3 Rat 6.8 pKi = 6.8 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 509 8 1 9 3.5 COc1cc2nc(N3CCN(C(=O)C(C)Oc4c(OC)cccc4C(C)C)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL136458 26765 0 None -10 3 Rat 6.8 pKi = 6.8 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 509 8 1 9 3.5 COc1cc2nc(N3CCN(C(=O)C(C)Oc4c(OC)cccc4C(C)C)CC3)nc(N)c2cc1OC 10.1021/jm9805337
3952 1849 33 None -26 12 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5353646 1849 33 None -26 12 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5443 1849 33 None -26 12 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5702063 1849 33 None -26 12 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL1331786 1849 33 None -26 12 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL420 1849 33 None -26 12 Rat 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
127027080 137315 0 None -45 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 443 7 3 4 3.3 O=C(NCCCCN1CCN(c2cccc3[nH]c(=O)[nH]c23)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
CHEMBL3760110 137315 0 None -45 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 443 7 3 4 3.3 O=C(NCCCCN1CCN(c2cccc3[nH]c(=O)[nH]c23)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
11152823 164696 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 367 5 2 6 2.6 COc1cc2nc3c(c(N)c2cc1OC)CC(CNC(=O)c1ccco1)C3 10.1021/jm030952q
CHEMBL423018 164696 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 367 5 2 6 2.6 COc1cc2nc3c(c(N)c2cc1OC)CC(CNC(=O)c1ccco1)C3 10.1021/jm030952q
76333281 84387 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 367 5 2 6 2.6 COc1cc2nc3c(c(N)c2cc1OC)CC(CNC(=O)c1ccoc1)C3 10.1007/s00044-010-9379-1
CHEMBL2234450 84387 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 367 5 2 6 2.6 COc1cc2nc3c(c(N)c2cc1OC)CC(CNC(=O)c1ccoc1)C3 10.1007/s00044-010-9379-1
11273296 169717 0 None 6 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 586 11 1 8 2.9 CCOC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL444648 169717 0 None 6 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 586 11 1 8 2.9 CCOC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
203096 60955 2 None -630 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 341 5 0 4 3.2 CN(C)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767134 60955 2 None -630 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 341 5 0 4 3.2 CN(C)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
45358442 60979 0 None -63 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 381 3 0 4 4.3 CN1CCCCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1 10.1021/jm1013874
CHEMBL1767158 60979 0 None -63 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 381 3 0 4 4.3 CN1CCCCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1 10.1021/jm1013874
24803799 60982 0 None -79 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 654 13 0 6 8.3 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
CHEMBL1767161 60982 0 None -79 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 654 13 0 6 8.3 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
25130875 187034 0 None -4 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 343 8 1 5 2.8 COc1ccccc1OCCNC[C@@H]1CO[C@@H](c2ccccc2)CO1 10.1021/jm800461k
CHEMBL494908 187034 0 None -4 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 343 8 1 5 2.8 COc1ccccc1OCCNC[C@@H]1CO[C@@H](c2ccccc2)CO1 10.1021/jm800461k
52937730 60968 0 None -794 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 363 5 0 5 3.1 COc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1 10.1021/jm1013874
CHEMBL1767147 60968 0 None -794 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 363 5 0 5 3.1 COc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1 10.1021/jm1013874
24803480 60984 0 None -199 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 614 15 0 6 7.2 CN(CCCCc1ccc(OCCCN2CCCCCC2)cc1)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767163 60984 0 None -199 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 614 15 0 6 7.2 CN(CCCCc1ccc(OCCCN2CCCCCC2)cc1)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
153287574 174665 0 None -21 10 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Prazosin from human recombinant adrenergic alpha1A receptor expressed in cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Prazosin from human recombinant adrenergic alpha1A receptor expressed in cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4572167 174665 0 None -21 10 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Prazosin from human recombinant adrenergic alpha1A receptor expressed in cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Prazosin from human recombinant adrenergic alpha1A receptor expressed in cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
11857863 85237 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 534 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccc(F)cc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL228608 85237 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 534 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccc(F)cc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
44426404 142022 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 498 7 1 6 4.4 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2007.04.098
CHEMBL389104 142022 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 498 7 1 6 4.4 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2007.04.098
124 2921 44 None -13 33 Rat 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2921 44 None -13 33 Rat 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2921 44 None -13 33 Rat 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2921 44 None -13 33 Rat 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2921 44 None -13 33 Rat 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
67753767 122525 1 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 318 5 1 1 5.0 c1ccc(CCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2015.07.046
CHEMBL3609351 122525 1 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 318 5 1 1 5.0 c1ccc(CCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2015.07.046
56649648 67498 0 None -47 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910139 67498 0 None -47 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
10816903 37445 0 None 32 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 571 8 2 7 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccc(OC)cc3C)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145756 37445 0 None 32 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 571 8 2 7 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccc(OC)cc3C)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
13507646 119096 0 None -3 2 Bovine 7.8 pKi = 7.8 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 243 0 0 2 4.0 c1ccc2c3c(sc2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL346492 119096 0 None -3 2 Bovine 7.8 pKi = 7.8 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 243 0 0 2 4.0 c1ccc2c3c(sc2c1)C1CCCCN1CC3 10.1021/jm00398a025
11801828 204808 0 None 35 6 Human 7.8 pKi = 7.8 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 606 9 3 6 5.0 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
CHEMBL88628 204808 0 None 35 6 Human 7.8 pKi = 7.8 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 606 9 3 6 5.0 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
11801828 204808 0 None 35 6 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 606 9 3 6 5.0 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1007/s00044-004-0120-9
CHEMBL88628 204808 0 None 35 6 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 606 9 3 6 5.0 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1007/s00044-004-0120-9
13507646 119096 0 None -3 2 Bovine 7.8 pKi = 7.8 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 243 0 0 2 4.0 c1ccc2c3c(sc2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL346492 119096 0 None -3 2 Bovine 7.8 pKi = 7.8 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 243 0 0 2 4.0 c1ccc2c3c(sc2c1)C1CCCCN1CC3 10.1021/jm00398a025
11994669 11710 0 None 3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1ccc(-c2ccccc2)cc1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182141 11710 0 None 3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1ccc(-c2ccccc2)cc1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL214552 11710 0 None 3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1ccc(-c2ccccc2)cc1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
52942664 17447 0 None 1 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 500 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL1258345 17447 0 None 1 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 500 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
10621590 84169 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153554 84169 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2221148 84169 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
25181488 186789 0 None -33 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNC[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm301525w
CHEMBL493486 186789 0 None -33 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNC[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm301525w
71151588 117742 0 None -169 10 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cells
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409256 117742 0 None -169 10 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cells
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
14468881 175699 0 None -14 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 347 10 1 3 4.5 c1ccc(OCCNCCOC(c2ccccc2)c2ccccc2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4462600 175699 0 None -14 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 347 10 1 3 4.5 c1ccc(OCCNCCOC(c2ccccc2)c2ccccc2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4595111 175699 0 None -14 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 347 10 1 3 4.5 c1ccc(OCCNCCOC(c2ccccc2)c2ccccc2)cc1 10.1016/j.ejmech.2019.05.024
71817859 102093 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
CHEMBL2419772 102093 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
CHEMBL3040801 102093 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 357 7 1 6 2.4 COc1ccc2c(c1OCCNC[C@@H]1COc3ccccc3O1)OCC2 10.1021/jm400867d
145962945 160784 0 None -14 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 511 5 1 7 4.6 COc1cc2nc(N3CCN(C(=O)Cc4ccc5ccccc5c4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4125846 160784 0 None -14 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 511 5 1 7 4.6 COc1cc2nc(N3CCN(C(=O)Cc4ccc5ccccc5c4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
118716699 114320 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 348 4 0 6 1.7 COc1ccccc1N1CCN(CC2COC3(CCOCC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3341769 114320 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 348 4 0 6 1.7 COc1ccccc1N1CCN(CC2COC3(CCOCC3)O2)CC1 10.1016/j.ejmech.2014.09.070
12203911 187689 20 None -54 2 Bovine 6.8 pKi = 6.8 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 255 1 0 3 1.6 CN1CCN(c2ncccc2Br)CC1 10.1021/jm00366a007
CHEMBL50017 187689 20 None -54 2 Bovine 6.8 pKi = 6.8 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 255 1 0 3 1.6 CN1CCN(c2ncccc2Br)CC1 10.1021/jm00366a007
415628 206441 89 None -13 5 Bovine 6.8 pKi = 6.8 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00366a007
CHEMBL9841 206441 89 None -13 5 Bovine 6.8 pKi = 6.8 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00366a007
127027384 137140 0 None -100 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 480 9 2 5 3.5 CS(=O)(=O)Nc1cccc(N2CCN(CCCCNC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2015.12.068
CHEMBL3758610 137140 0 None -100 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 480 9 2 5 3.5 CS(=O)(=O)Nc1cccc(N2CCN(CCCCNC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2015.12.068
11500225 100718 57 None -38 2 Bovine 5.8 pKi = 5.8 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 289 1 1 3 1.1 Ic1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL295764 100718 57 None -38 2 Bovine 5.8 pKi = 5.8 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 289 1 1 3 1.1 Ic1cccnc1N1CCNCC1 10.1021/jm00366a007
44586429 183705 0 None -1 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 514 8 1 6 3.0 COc1ccccc1N1CCN(CC(O)CN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL484102 183705 0 None -1 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 514 8 1 6 3.0 COc1ccccc1N1CCN(CC(O)CN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
44361064 31385 0 None -6 6 Bovine 6.8 pKi = 6.8 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 338 7 2 4 4.5 N=CCC(O)CC1CCN(c2ccccc2Oc2ccccc2)CC1 10.1021/jm960510x
CHEMBL140450 31385 0 None -6 6 Bovine 6.8 pKi = 6.8 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 338 7 2 4 4.5 N=CCC(O)CC1CCN(c2ccccc2Oc2ccccc2)CC1 10.1021/jm960510x
11732516 203489 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 418 5 0 7 3.0 COc1ccccc1N1CCN(c2c(C(C)=O)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL78584 203489 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 418 5 0 7 3.0 COc1ccccc1N1CCN(c2c(C(C)=O)c(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
9817256 202527 0 None 2 4 Human 5.8 pKi = 5.8 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71001 202527 0 None 2 4 Human 5.8 pKi = 5.8 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
44586483 171890 0 None 1 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 600 11 1 8 3.3 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)N(C(C)C(=O)OC)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL448198 171890 0 None 1 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 600 11 1 8 3.3 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)N(C(C)C(=O)OC)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
24894141 186816 0 None -30 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 449 10 1 6 4.0 COc1cccc(OC)c1OCCNC[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm301525w
CHEMBL493697 186816 0 None -30 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 449 10 1 6 4.0 COc1cccc(OC)c1OCCNC[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm301525w
9944467 9146 0 None 1 4 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 309 2 2 2 3.4 O=C(Nc1cccc2c1CCCC2c1c[nH]cn1)C(F)(F)F 10.1021/jm030551a
CHEMBL110751 9146 0 None 1 4 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 309 2 2 2 3.4 O=C(Nc1cccc2c1CCCC2c1c[nH]cn1)C(F)(F)F 10.1021/jm030551a
10420352 168164 10 None -63 4 Human 4.8 pKi = 4.8 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
CHEMBL43711 168164 10 None -63 4 Human 4.8 pKi = 4.8 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
24839550 136778 14 None -26 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752576 136778 14 None -26 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
127024960 137178 0 None -15 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
CHEMBL3758920 137178 0 None -15 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
11742585 162784 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 415 5 1 6 2.5 CS(=O)(=O)Nc1ccc2c(c1)OC1(CCN(CCc3ccccn3)CC1)CC2=O 10.1016/s0960-894x(98)00732-x
CHEMBL419164 162784 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 415 5 1 6 2.5 CS(=O)(=O)Nc1ccc2c(c1)OC1(CCN(CCc3ccccn3)CC1)CC2=O 10.1016/s0960-894x(98)00732-x
CHEMBL4576555 212254 3 None -1 14 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a ADRA1ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000705a ADRA1A
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 nan
76322411 84376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 375 7 1 4 4.0 c1ccc(OCCNC2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1007/s00044-010-9379-1
CHEMBL2234439 84376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 375 7 1 4 4.0 c1ccc(OCCNC2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1007/s00044-010-9379-1
11176459 101153 0 None -181 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 380 4 0 5 2.4 N#Cc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
CHEMBL299022 101153 0 None -181 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 380 4 0 5 2.4 N#Cc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
155536203 175823 0 None -2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 403 10 1 4 4.6 c1ccc(OCCNCC[C@@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4473623 175823 0 None -2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 403 10 1 4 4.6 c1ccc(OCCNCC[C@@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4596045 175823 0 None -2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 403 10 1 4 4.6 c1ccc(OCCNCC[C@@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
25131198 85819 0 None -288 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNCC2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.02.056
CHEMBL2312537 85819 0 None -288 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNCC2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.02.056
25181489 186764 0 None -158 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNC[C@@H]2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm800461k
CHEMBL493285 186764 0 None -158 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNC[C@@H]2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm800461k
25131198 85819 0 None -288 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNCC2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm301525w
CHEMBL2312537 85819 0 None -288 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNCC2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm301525w
76307951 84388 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 453 9 2 8 3.6 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNCOc1c(OC)cccc1OC)C3 10.1007/s00044-010-9379-1
CHEMBL2234451 84388 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 453 9 2 8 3.6 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNCOc1c(OC)cccc1OC)C3 10.1007/s00044-010-9379-1
11784634 36269 0 None -7 3 Human 5.8 pKi = 5.8 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 468 10 2 8 3.7 COc1cc2nc3c(c(O)c2cc1OC)CCC(CNCCOc1c(OC)cccc1OC)C3 10.1021/jm030952q
CHEMBL144779 36269 0 None -7 3 Human 5.8 pKi = 5.8 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 468 10 2 8 3.7 COc1cc2nc3c(c(O)c2cc1OC)CCC(CNCCOc1c(OC)cccc1OC)C3 10.1021/jm030952q
76307951 84388 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 453 9 2 8 3.6 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNCOc1c(OC)cccc1OC)C3 10.1007/s00044-010-9379-1
CHEMBL2234451 84388 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 453 9 2 8 3.6 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNCOc1c(OC)cccc1OC)C3 10.1007/s00044-010-9379-1
9818490 9272 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 319 5 2 3 3.0 CCCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL111391 9272 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 319 5 2 3 3.0 CCCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
53328503 63047 0 None -15 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 441 6 0 5 3.4 COc1ccccc1N1CCN(CCN2C(=O)CC(c3ccc(Cl)cc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796037 63047 0 None -15 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 441 6 0 5 3.4 COc1ccccc1N1CCN(CCN2C(=O)CC(c3ccc(Cl)cc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
9818490 9272 0 None - 1 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 319 5 2 3 3.0 CCCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL111391 9272 0 None - 1 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 319 5 2 3 3.0 CCCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
9966903 168836 0 None - 1 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 321 4 2 4 2.3 COc1ccc(NS(C)(=O)=O)c2c1C(c1c[nH]cn1)CCC2 10.1021/jm030551a
CHEMBL442394 168836 0 None - 1 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 321 4 2 4 2.3 COc1ccc(NS(C)(=O)=O)c2c1C(c1c[nH]cn1)CCC2 10.1021/jm030551a
44431562 87532 0 None 3 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(OC)c(S(=O)(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)c1 10.1016/j.bmcl.2007.04.008
CHEMBL234194 87532 0 None 3 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(OC)c(S(=O)(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)c1 10.1016/j.bmcl.2007.04.008
44431557 88834 0 None -8 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 541 8 1 6 4.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL236830 88834 0 None -8 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 541 8 1 6 4.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
49865639 15842 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 328 7 1 4 3.2 Fc1ccccc1N1CCN(CCCCNc2ccccn2)CC1 10.1016/j.bmcl.2010.07.096
CHEMBL1223680 15842 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 328 7 1 4 3.2 Fc1ccccc1N1CCN(CCCCNc2ccccn2)CC1 10.1016/j.bmcl.2010.07.096
44288485 161958 0 None 29 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 498 9 1 4 5.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C(c2ccc(C)cc2)c2ccc(C)cc2)CC1 10.1016/s0960-894x(01)00320-1
CHEMBL41677 161958 0 None 29 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 498 9 1 4 5.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C(c2ccc(C)cc2)c2ccc(C)cc2)CC1 10.1016/s0960-894x(01)00320-1
44288359 155193 0 None -2 3 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 461 5 1 6 4.0 COc1cccc2c1CCC1CN(CCCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC21 10.1021/jm990567u
CHEMBL40564 155193 0 None -2 3 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 461 5 1 6 4.0 COc1cccc2c1CCC1CN(CCCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC21 10.1021/jm990567u
44447072 94196 0 None -25 4 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 483 6 1 6 4.5 O=C(NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21)c1cccnc1 10.1016/j.bmcl.2007.11.106
CHEMBL252430 94196 0 None -25 4 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 483 6 1 6 4.5 O=C(NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21)c1cccnc1 10.1016/j.bmcl.2007.11.106
6604803 116005 2 None -7 4 Bovine 7.8 pKi = 7.8 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL336161 116005 2 None -7 4 Bovine 7.8 pKi = 7.8 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
118716705 114487 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 424 5 0 7 2.6 COc1ccccc1N1CCN(CC2COC3(CCN(c4ccccn4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342858 114487 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 424 5 0 7 2.6 COc1ccccc1N1CCN(CC2COC3(CCN(c4ccccn4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
11176459 101153 0 None -181 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 380 4 0 5 2.4 N#Cc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
CHEMBL299022 101153 0 None -181 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 380 4 0 5 2.4 N#Cc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
9934955 71917 0 None -489 6 Human 5.8 pKi = 5.8 Binding
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 482 5 2 9 2.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
CHEMBL19826 71917 0 None -489 6 Human 5.8 pKi = 5.8 Binding
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 482 5 2 9 2.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
11098175 202460 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL70691 202460 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
1220 186 46 None -407 45 Human 5.8 pKi = 5.8 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm010866v
31 186 46 None -407 45 Human 5.8 pKi = 5.8 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm010866v
7 186 46 None -407 45 Human 5.8 pKi = 5.8 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm010866v
CHEMBL56 186 46 None -407 45 Human 5.8 pKi = 5.8 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm010866v
1220 186 46 None -407 45 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm0009336
31 186 46 None -407 45 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm0009336
7 186 46 None -407 45 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm0009336
CHEMBL56 186 46 None -407 45 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm0009336
53248365 61742 0 None -186 7 Human 6.8 pKi = 6.8 Binding
Inhibition of adrenergic alpha1A receptorInhibition of adrenergic alpha1A receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
CHEMBL1774995 61742 0 None -186 7 Human 6.8 pKi = 6.8 Binding
Inhibition of adrenergic alpha1A receptorInhibition of adrenergic alpha1A receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
71817545 91678 0 None -58 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 354 7 2 5 3.0 COc1ccc2cc[nH]c2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL2419765 91678 0 None -58 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 354 7 2 5 3.0 COc1ccc2cc[nH]c2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm400867d
126720252 164112 0 None -63 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by scintillation counting methodDisplacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4216870 164112 0 None -63 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by scintillation counting methodDisplacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
18738382 15083 0 None 33 3 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 399 8 0 5 2.7 CC(C)Oc1ccccc1N1CCN(C/C=C/C(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL12127 15083 0 None 33 3 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 399 8 0 5 2.7 CC(C)Oc1ccccc1N1CCN(C/C=C/C(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
9888164 17754 1 None 25 3 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 416 8 1 5 2.1 CC(C)Oc1ccccc1N1CCN(CCNC(=O)CN2CCCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL12603 17754 1 None 25 3 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 416 8 1 5 2.1 CC(C)Oc1ccccc1N1CCN(CCNC(=O)CN2CCCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
289 240 6 None -1 14 Human 7.8 pKi = 7.8 Binding
Binding affinity to human adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to human adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 240 6 None -1 14 Human 7.8 pKi = 7.8 Binding
Binding affinity to human adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to human adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 240 6 None -1 14 Human 7.8 pKi = 7.8 Binding
Binding affinity to human adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to human adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
44431564 147815 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 501 8 1 6 4.2 COc1ccc(C)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL393725 147815 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 501 8 1 6 4.2 COc1ccc(C)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
44308443 202246 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 413 6 0 5 4.0 COc1ccccc1N1CCN(Cc2ccc(CN3CCCCCC3=O)s2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL69339 202246 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 413 6 0 5 4.0 COc1ccccc1N1CCN(Cc2ccc(CN3CCCCCC3=O)s2)CC1 10.1016/s0960-894x(02)00347-5
9864676 127273 0 None -1 5 Bovine 7.8 pKi = 7.8 Binding
Inhibition of [3H]prazosin binding to Alpha-1 adrenergic receptor in bovine frontal cortexInhibition of [3H]prazosin binding to Alpha-1 adrenergic receptor in bovine frontal cortex
ChEMBL 380 6 0 3 4.5 O=C(CCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL366388 127273 0 None -1 5 Bovine 7.8 pKi = 7.8 Binding
Inhibition of [3H]prazosin binding to Alpha-1 adrenergic receptor in bovine frontal cortexInhibition of [3H]prazosin binding to Alpha-1 adrenergic receptor in bovine frontal cortex
ChEMBL 380 6 0 3 4.5 O=C(CCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
145950240 162139 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 465 5 2 9 2.2 COc1cc2nc(N3CCC[C@H](NC(=O)[C@H]4COc5ccccc5O4)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
CHEMBL4170675 162139 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 465 5 2 9 2.2 COc1cc2nc(N3CCC[C@H](NC(=O)[C@H]4COc5ccccc5O4)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
10787126 84133 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153558 84133 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220897 84133 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
10893672 203691 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 357 6 1 7 1.3 COc1ccccc1N1CCN(CCNc2cc(C)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL80132 203691 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 357 6 1 7 1.3 COc1ccccc1N1CCN(CCNc2cc(C)nn(C)c2=O)CC1 10.1021/jm0009336
11109088 202470 0 None -3 6 Human 7.7 pKi = 7.7 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70751 202470 0 None -3 6 Human 7.7 pKi = 7.7 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
9824384 118269 1 None -17 8 Rat 7.7 pKi = 7.7 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1021/jm960510x
CHEMBL342062 118269 1 None -17 8 Rat 7.7 pKi = 7.7 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1021/jm960510x
10252540 84919 1 None -83 6 Rat 7.7 pKi = 7.7 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) CEC-treated hippocampusBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) CEC-treated hippocampus
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
CHEMBL2261604 84919 1 None -83 6 Rat 7.7 pKi = 7.7 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) CEC-treated hippocampusBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) CEC-treated hippocampus
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
3251 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2010.05.023
5684 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2010.05.023
80 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2010.05.023
CHEMBL31354 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2010.05.023
3251 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2019.05.024
5684 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2019.05.024
80 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2019.05.024
CHEMBL31354 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2019.05.024
3251 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2019.02.056
5684 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2019.02.056
80 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2019.02.056
CHEMBL31354 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2019.02.056
3251 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm200421e
5684 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm200421e
80 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm200421e
CHEMBL31354 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm200421e
118716720 114503 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 425 5 0 7 1.0 COc1ccccc1N1CCN(CC2COC3(CCN(S(C)(=O)=O)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342873 114503 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 425 5 0 7 1.0 COc1ccccc1N1CCN(CC2COC3(CCN(S(C)(=O)=O)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
10575664 118690 0 None -2 3 Rat 7.7 pKi = 7.7 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 453 7 1 9 2.0 COc1cc2nc(N3CCN(C(=O)COc4ccccc4OC)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL343283 118690 0 None -2 3 Rat 7.7 pKi = 7.7 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 453 7 1 9 2.0 COc1cc2nc(N3CCN(C(=O)COc4ccccc4OC)CC3)nc(N)c2cc1OC 10.1021/jm9805337
10575664 118690 0 None -2 3 Human 7.7 pKi = 7.7 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 453 7 1 9 2.0 COc1cc2nc(N3CCN(C(=O)COc4ccccc4OC)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL343283 118690 0 None -2 3 Human 7.7 pKi = 7.7 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 453 7 1 9 2.0 COc1cc2nc(N3CCN(C(=O)COc4ccccc4OC)CC3)nc(N)c2cc1OC 10.1021/jm9805337
16756754 91683 21 None -81 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
CHEMBL242004 91683 21 None -81 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
11412944 101026 65 None -223 2 Bovine 5.8 pKi = 5.8 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL298004 101026 65 None -223 2 Bovine 5.8 pKi = 5.8 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cccnc1N1CCNCC1 10.1021/jm00366a007
70820518 166955 0 None -104 3 Human 5.8 pKi = 5.8 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 391 7 1 4 3.7 CS(=O)(=O)c1ccc(Cl)cc1CNCCOc1cc(F)ccc1Cl 10.1016/j.ejmech.2017.07.071
CHEMBL4213747 166955 0 None -104 3 Human 5.8 pKi = 5.8 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 391 7 1 4 3.7 CS(=O)(=O)c1ccc(Cl)cc1CNCCOc1cc(F)ccc1Cl 10.1016/j.ejmech.2017.07.071
CHEMBL4300105 166955 0 None -104 3 Human 5.8 pKi = 5.8 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 391 7 1 4 3.7 CS(=O)(=O)c1ccc(Cl)cc1CNCCOc1cc(F)ccc1Cl 10.1016/j.ejmech.2017.07.071
57400562 68961 0 None -1 5 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928247 68961 0 None -1 5 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
44420419 83004 0 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 485 4 0 7 3.3 Cn1c(=O)n(CCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)c(=O)c2c1c1ccccc1n2C 10.1016/j.bmcl.2006.09.034
CHEMBL219719 83004 0 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 485 4 0 7 3.3 Cn1c(=O)n(CCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)c(=O)c2c1c1ccccc1n2C 10.1016/j.bmcl.2006.09.034
10198248 186856 35 None -83 6 Human 4.7 pKi = 4.7 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 213 1 2 5 1.0 c1cnc2cc(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
CHEMBL49395 186856 35 None -83 6 Human 4.7 pKi = 4.7 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 213 1 2 5 1.0 c1cnc2cc(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
134149777 147967 0 None -199 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 353 7 1 5 4.2 COc1ccccc1OCCNCC1CSC2(CCCCC2)S1 10.1016/j.ejmech.2016.09.050
CHEMBL3938383 147967 0 None -199 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 353 7 1 5 4.2 COc1ccccc1OCCNCC1CSC2(CCCCC2)S1 10.1016/j.ejmech.2016.09.050
11464777 101322 0 None -457 5 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 437 4 0 4 4.2 CC(CN1CCN(c2cc(Cl)ccc2Cl)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm030944+
CHEMBL300152 101322 0 None -457 5 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 437 4 0 4 4.2 CC(CN1CCN(c2cc(Cl)ccc2Cl)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm030944+
44431613 87140 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 529 10 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OCC4CC4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.008
CHEMBL233584 87140 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 529 10 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OCC4CC4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.008
10792536 205039 0 None 14 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 540 7 3 3 4.7 O=C1NC(C(F)(F)F)=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1021/jm990612y
CHEMBL90184 205039 0 None 14 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 540 7 3 3 4.7 O=C1NC(C(F)(F)F)=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1021/jm990612y
135398737 942 89 None -5 92 Human 7.7 pKi = 7.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 942 89 None -5 92 Human 7.7 pKi = 7.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 942 89 None -5 92 Human 7.7 pKi = 7.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 942 89 None -5 92 Human 7.7 pKi = 7.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 942 89 None -5 92 Human 7.7 pKi = 7.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
44431614 87595 0 None 2 4 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 533 9 1 6 4.5 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OCC3CC3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234474 87595 0 None 2 4 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 533 9 1 6 4.5 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OCC3CC3)CC2)CC1 10.1016/j.bmcl.2007.04.008
13141182 130358 1 None 10 2 Bovine 7.7 pKi = 7.7 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 354 0 0 2 4.7 CN1CCC(=C2c3cc(Br)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL368578 130358 1 None 10 2 Bovine 7.7 pKi = 7.7 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 354 0 0 2 4.7 CN1CCC(=C2c3cc(Br)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
127027078 137289 0 None -14 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 426 7 2 3 4.7 O=C(NCCCCN1CCN(c2cccc3[nH]ccc23)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
CHEMBL3759865 137289 0 None -14 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 426 7 2 3 4.7 O=C(NCCCCN1CCN(c2cccc3[nH]ccc23)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
57395341 68954 0 None 2 5 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928135 68954 0 None 2 5 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
71508682 86606 0 None 45 2 Bovine 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 371 3 0 5 4.2 CN1CCC(c2cn(-c3ccncc3)c3ccc(-c4ccnn4C)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2325927 86606 0 None 45 2 Bovine 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 371 3 0 5 4.2 CN1CCC(c2cn(-c3ccncc3)c3ccc(-c4ccnn4C)cc23)CC1 10.1016/j.bmc.2012.10.049
71508711 86614 0 None 43 2 Bovine 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 369 3 0 5 4.3 CN1CCC(c2cn(-c3ccncc3)c3ccc(-c4cncnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2325934 86614 0 None 43 2 Bovine 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 369 3 0 5 4.3 CN1CCC(c2cn(-c3ccncc3)c3ccc(-c4cncnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
10698974 90677 0 None 102 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 610 5 1 7 4.3 COC(=O)C1=C(C)NC(=O)N(C(=O)N2CCC(N3CCC(C(=O)OC)(c4ccccc4)CC3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL239806 90677 0 None 102 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 610 5 1 7 4.3 COC(=O)C1=C(C)NC(=O)N(C(=O)N2CCC(N3CCC(C(=O)OC)(c4ccccc4)CC3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
135398737 942 89 None -5 92 Human 7.7 pKi = 7.7 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
38 942 89 None -5 92 Human 7.7 pKi = 7.7 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
722 942 89 None -5 92 Human 7.7 pKi = 7.7 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
CHEMBL42 942 89 None -5 92 Human 7.7 pKi = 7.7 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
DB00363 942 89 None -5 92 Human 7.7 pKi = 7.7 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
42631003 197927 10 None -97 8 Human 7.7 pKi = 7.7 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592752 197927 10 None -97 8 Human 7.7 pKi = 7.7 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
50905588 56044 0 None -1 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 406 7 2 6 2.1 COc1ccc(C[C@@H](C)NC[C@H]2Oc3ccccc3O[C@H]2C)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
CHEMBL1630941 56044 0 None -1 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 406 7 2 6 2.1 COc1ccc(C[C@@H](C)NC[C@H]2Oc3ccccc3O[C@H]2C)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
10575494 165183 0 None -4 3 Human 7.7 pKi = 7.7 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 449 7 1 8 2.5 COc1cc2nc(N3CCN(C(=O)CCC(=O)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL424658 165183 0 None -4 3 Human 7.7 pKi = 7.7 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 449 7 1 8 2.5 COc1cc2nc(N3CCN(C(=O)CCC(=O)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
44329027 4089 0 None 9 6 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 637 13 3 7 4.9 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COC)N1 10.1016/s0960-894x(99)00484-9
CHEMBL100045 4089 0 None 9 6 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 637 13 3 7 4.9 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COC)N1 10.1016/s0960-894x(99)00484-9
10363912 6445 0 None -36 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL1082862 6445 0 None -36 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL286003 6445 0 None -36 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
10363912 6445 0 None -36 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
CHEMBL1082862 6445 0 None -36 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
CHEMBL286003 6445 0 None -36 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
10363912 6445 0 None -36 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm200421e
CHEMBL1082862 6445 0 None -36 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm200421e
CHEMBL286003 6445 0 None -36 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm200421e
11653915 123481 0 None -5 6 Human 7.7 pKi = 7.7 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 296 4 2 5 2.6 COc1cccc(N(NC2=NCCN2)c2ccc(C)cc2)c1 10.1016/j.bmcl.2005.07.083
CHEMBL362954 123481 0 None -5 6 Human 7.7 pKi = 7.7 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 296 4 2 5 2.6 COc1cccc(N(NC2=NCCN2)c2ccc(C)cc2)c1 10.1016/j.bmcl.2005.07.083
52945156 16862 0 None -7 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 455 13 1 6 4.1 COc1cccc(OC)c1[S+]([O-])CCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1254660 16862 0 None -7 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 455 13 1 6 4.1 COc1cccc(OC)c1[S+]([O-])CCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
118716722 114505 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 446 7 1 6 2.5 CCCCNC(=O)N1CCC2(CC1)OCC(CN1CCN(c3ccccc3OC)CC1)O2 10.1016/j.ejmech.2014.09.070
CHEMBL3342875 114505 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 446 7 1 6 2.5 CCCCNC(=O)N1CCC2(CC1)OCC(CN1CCN(c3ccccc3OC)CC1)O2 10.1016/j.ejmech.2014.09.070
44298747 101525 0 None -3 2 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 480 7 1 6 2.7 O=c1[nH]cc(C(F)(F)F)c(=O)n1CCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
CHEMBL301650 101525 0 None -3 2 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 480 7 1 6 2.7 O=c1[nH]cc(C(F)(F)F)c(=O)n1CCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
9887458 193990 0 None -512 4 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 403 4 0 4 3.5 Cc1ccc(Cl)cc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
CHEMBL55654 193990 0 None -512 4 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 403 4 0 4 3.5 Cc1ccc(Cl)cc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
53328313 63042 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 455 7 0 5 3.8 COc1ccc(Cl)cc1N1CCN(CCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796032 63042 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 455 7 0 5 3.8 COc1ccc(Cl)cc1N1CCN(CCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
145958538 161703 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 303 3 2 7 1.2 COc1cc2nc(N3CCC[C@H](N)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
CHEMBL4163810 161703 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 303 3 2 7 1.2 COc1cc2nc(N3CCC[C@H](N)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
9905929 12689 0 None -26 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 339 5 1 2 4.5 Cc1[nH]c2ccccc2c1C1CCN(CCCN2CCCCC2)CC1 10.1016/j.bmcl.2006.05.002
CHEMBL1188265 12689 0 None -26 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 339 5 1 2 4.5 Cc1[nH]c2ccccc2c1C1CCN(CCCN2CCCCC2)CC1 10.1016/j.bmcl.2006.05.002
CHEMBL535837 12689 0 None -26 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 339 5 1 2 4.5 Cc1[nH]c2ccccc2c1C1CCN(CCCN2CCCCC2)CC1 10.1016/j.bmcl.2006.05.002
9904117 9297 3 None -1 5 Rat 6.7 pKi = 6.7 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL111554 9297 3 None -1 5 Rat 6.7 pKi = 6.7 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
44531812 193006 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 374 7 2 6 4.3 COc1cccc2c(NCCNc3ccnc4c(OC)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
CHEMBL532818 193006 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 374 7 2 6 4.3 COc1cccc2c(NCCNc3ccnc4c(OC)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
9904117 9297 3 None -1 5 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL111554 9297 3 None -1 5 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
44314200 102466 0 None -81 4 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 230 1 1 3 2.4 c1ccc2c(c1)CCCC2NC1=NCCCO1 10.1016/0960-894X(94)85032-1
CHEMBL306377 102466 0 None -81 4 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 230 1 1 3 2.4 c1ccc2c(c1)CCCC2NC1=NCCCO1 10.1016/0960-894X(94)85032-1
44531812 193006 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 374 7 2 6 4.3 COc1cccc2c(NCCNc3ccnc4c(OC)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
CHEMBL532818 193006 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 374 7 2 6 4.3 COc1cccc2c(NCCNc3ccnc4c(OC)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
44586479 188032 0 None 1 3 Rat 6.7 pKi = 6.7 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 572 10 1 8 2.6 COC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL503007 188032 0 None 1 3 Rat 6.7 pKi = 6.7 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 572 10 1 8 2.6 COC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3OC)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
52937732 60970 0 None -794 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 369 4 0 4 3.4 CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)c(F)c2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767149 60970 0 None -794 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 369 4 0 4 3.4 CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)c(F)c2)c2ccccc2c1=O 10.1021/jm1013874
52937828 60973 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 347 5 0 4 3.3 CN1CCC[C@@H]1Cn1nc(CCc2ccccc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767152 60973 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 347 5 0 4 3.3 CN1CCC[C@@H]1Cn1nc(CCc2ccccc2)c2ccccc2c1=O 10.1021/jm1013874
25130879 172656 0 None -47 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 343 8 1 5 2.8 COc1ccccc1OCCNC[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm800461k
CHEMBL452437 172656 0 None -47 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 343 8 1 5 2.8 COc1ccccc1OCCNC[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm800461k
134138438 146798 0 None -66 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 378 4 0 5 4.3 COc1ccccc1N1CCN(CC2CSC3(CCCCC3)S2)CC1 10.1016/j.ejmech.2016.09.050
CHEMBL3929328 146798 0 None -66 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 378 4 0 5 4.3 COc1ccccc1N1CCN(CC2CSC3(CCCCC3)S2)CC1 10.1016/j.ejmech.2016.09.050
25025581 200302 0 None -3 8 Human 6.7 pKi = 6.7 Binding
Inhibition of adrenergic alpha1A receptorInhibition of adrenergic alpha1A receptor
ChEMBL 285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1 10.1021/jm901818u
CHEMBL608151 200302 0 None -3 8 Human 6.7 pKi = 6.7 Binding
Inhibition of adrenergic alpha1A receptorInhibition of adrenergic alpha1A receptor
ChEMBL 285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1 10.1021/jm901818u
43260 5393 61 None -1 5 Rat 5.7 pKi = 5.7 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1007/s00044-004-0020-z
CHEMBL1076 5393 61 None -1 5 Rat 5.7 pKi = 5.7 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1007/s00044-004-0020-z
294234 102407 3 None -512 4 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 182 1 1 3 1.7 C1CCCC(NC2=NCCO2)CC1 10.1016/0960-894X(94)85032-1
CHEMBL305928 102407 3 None -512 4 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 182 1 1 3 1.7 C1CCCC(NC2=NCCO2)CC1 10.1016/0960-894X(94)85032-1
25164129 160601 0 None -3715 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4088036 160601 0 None -3715 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117406 160601 0 None -3715 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
43260 5393 61 None -1 5 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1021/jm030551a
CHEMBL1076 5393 61 None -1 5 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1021/jm030551a
3584 3706 60 None -2 14 Human 8.7 pKi = 8.7 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
5401 3706 60 None -2 14 Human 8.7 pKi = 8.7 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
7302 3706 60 None -2 14 Human 8.7 pKi = 8.7 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
CHEMBL611 3706 60 None -2 14 Human 8.7 pKi = 8.7 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
DB01162 3706 60 None -2 14 Human 8.7 pKi = 8.7 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
44431560 145033 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL391530 145033 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
11081136 203505 0 None 1 3 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 467 8 1 7 3.7 COc1ccc(Cl)cc1N1CCN(CCCNc2cc(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL78676 203505 0 None 1 3 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 467 8 1 7 3.7 COc1ccc(Cl)cc1N1CCN(CCCNc2cc(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
4431 2679 18 None 1 12 Human 8.7 pKi = 8.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.bmcl.2004.11.032
73 2679 18 None 1 12 Human 8.7 pKi = 8.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.bmcl.2004.11.032
CHEMBL8618 2679 18 None 1 12 Human 8.7 pKi = 8.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.bmcl.2004.11.032
9909211 93761 1 None 1 3 Human 8.7 pKi = 8.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 404 8 2 7 1.9 COc1ccc(Cl)cc1N1CCN(CCCNc2nccc(C(N)=O)n2)CC1 10.1016/j.bmcl.2004.11.032
CHEMBL24981 93761 1 None 1 3 Human 8.7 pKi = 8.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 404 8 2 7 1.9 COc1ccc(Cl)cc1N1CCN(CCCNc2nccc(C(N)=O)n2)CC1 10.1016/j.bmcl.2004.11.032
3584 3706 60 None -2 14 Human 8.7 pKi = 8.7 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
5401 3706 60 None -2 14 Human 8.7 pKi = 8.7 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
7302 3706 60 None -2 14 Human 8.7 pKi = 8.7 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
CHEMBL611 3706 60 None -2 14 Human 8.7 pKi = 8.7 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
DB01162 3706 60 None -2 14 Human 8.7 pKi = 8.7 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
181743 177987 3 None 24 22 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Prazosin from human adrenergic alpha1A receptorDisplacement of [3H]Prazosin from human adrenergic alpha1A receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 177987 3 None 24 22 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Prazosin from human adrenergic alpha1A receptorDisplacement of [3H]Prazosin from human adrenergic alpha1A receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
49781681 17689 0 None -1 4 Bovine 8.7 pKi = 8.7 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 428 2 0 3 6.3 Cc1cc(C)c(-c2ccc3c(c2)C(N2CCN(C)CC2)Cc2ccccc2S3)c(C)c1 10.1021/jm100652h
CHEMBL1259098 17689 0 None -1 4 Bovine 8.7 pKi = 8.7 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 428 2 0 3 6.3 Cc1cc(C)c(-c2ccc3c(c2)C(N2CCN(C)CC2)Cc2ccccc2S3)c(C)c1 10.1021/jm100652h
10097317 198391 0 None 288 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 495 8 2 4 4.9 Cc1ccc(C(O)(C(=O)NCCCN2CCC(C#N)(c3ccccc3C)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(01)00320-1
CHEMBL59590 198391 0 None 288 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 495 8 2 4 4.9 Cc1ccc(C(O)(C(=O)NCCCN2CCC(C#N)(c3ccccc3C)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(01)00320-1
10026936 162894 0 None 114 3 Human 8.7 pKi = 8.7 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 453 8 1 3 5.1 Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2ccc(F)c(F)c2)C(C)C)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL41994 162894 0 None 114 3 Human 8.7 pKi = 8.7 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 453 8 1 3 5.1 Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2ccc(F)c(F)c2)C(C)C)CC1 10.1016/s0960-894x(00)00307-3
11200086 194740 0 None -1 4 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 388 4 0 3 4.2 O=C1CC2(CCCC2)CC(=O)N1CCN1CCC(c2ccccc2Cl)CC1 10.1021/jm030944+
CHEMBL56292 194740 0 None -1 4 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 388 4 0 3 4.2 O=C1CC2(CCCC2)CC(=O)N1CCN1CCC(c2ccccc2Cl)CC1 10.1021/jm030944+
44312563 203202 2 None -1 7 Bovine 8.7 pKi = 8.7 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]-prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]-prazosin as radioligand
ChEMBL 401 7 1 8 1.0 COc1ccc(C)cc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1021/jm960069a
CHEMBL76168 203202 2 None -1 7 Bovine 8.7 pKi = 8.7 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]-prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]-prazosin as radioligand
ChEMBL 401 7 1 8 1.0 COc1ccc(C)cc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1021/jm960069a
10531 1387 18 None -5 24 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1387 18 None -5 24 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1387 18 None -5 24 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1387 18 None -5 24 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1387 18 None -5 24 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
46934945 16504 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 533 7 0 7 3.8 COc1ccccc1N1CCN(C[C@H]2CO[C@@](CN3C(=O)CC4(CCCC4)CC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242912 16504 0 None 1 4 Human 8.7 pKi = 8.7 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 533 7 0 7 3.8 COc1ccccc1N1CCN(C[C@H]2CO[C@@](CN3C(=O)CC4(CCCC4)CC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
100 3733 52 None 1 56 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3733 52 None 1 56 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3733 52 None 1 56 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3733 52 None 1 56 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3733 52 None 1 56 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
6761 67442 17 None 1 18 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67442 17 None 1 18 Rat 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
46882034 5709 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 433 10 1 5 4.8 CC(C)Oc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
CHEMBL1078773 5709 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 433 10 1 5 4.8 CC(C)Oc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
121102 143422 1 None -3 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 370 8 0 5 3.5 CCOc1ccccc1N1CCN(CCc2ccc(OC)c(OC)c2)CC1 10.1016/j.ejmech.2016.06.052
CHEMBL3902626 143422 1 None -3 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 370 8 0 5 3.5 CCOc1ccccc1N1CCN(CCc2ccc(OC)c(OC)c2)CC1 10.1016/j.ejmech.2016.06.052
11801214 101738 0 None 25 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 572 10 2 8 3.2 COc1ccc(N2C(=O)c3ccc(C(=O)NC[C@@H](O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
CHEMBL302942 101738 0 None 25 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 572 10 2 8 3.2 COc1ccc(N2C(=O)c3ccc(C(=O)NC[C@@H](O)CN4CCN(c5ccccc5OC(C)C)CC4)cc3C2=O)cc1 10.1021/jm9905918
9844511 104104 0 None 85 3 Human 8.7 pKi = 8.7 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 411 7 1 5 3.0 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)n[nH]2)CC1 10.1016/s0960-894x(00)00472-8
CHEMBL310471 104104 0 None 85 3 Human 8.7 pKi = 8.7 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 411 7 1 5 3.0 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)n[nH]2)CC1 10.1016/s0960-894x(00)00472-8
56961460 120911 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 477 4 2 10 2.0 COc1cc2nc(N3CCN(C(=O)c4cc5ccc(O)cc5oc4=O)CC3)nc(N)c2cc1OC 10.1021/ml5004298
CHEMBL3582268 120911 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 477 4 2 10 2.0 COc1cc2nc(N3CCN(C(=O)c4cc5ccc(O)cc5oc4=O)CC3)nc(N)c2cc1OC 10.1021/ml5004298
10393665 33685 0 None 47 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 593 9 2 9 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
CHEMBL142383 33685 0 None 47 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 593 9 2 9 3.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
10627279 36967 0 None 47 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 592 9 3 8 3.0 CNC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
CHEMBL145334 36967 0 None 47 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 592 9 3 8 3.0 CNC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
10767626 154772 0 None -2 3 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 461 4 1 6 3.9 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(C)cc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL40310 154772 0 None -2 3 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 461 4 1 6 3.9 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccc(C)cc54)c3=O)C[C@@H]21 10.1021/jm990567u
10502807 162583 0 None -3 3 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 431 4 1 6 3.1 COc1cccc2c1CCC1CN(CCn3c(=O)[nH]c4c(oc5ccccc54)c3=O)CC21 10.1021/jm990567u
CHEMBL417890 162583 0 None -3 3 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 431 4 1 6 3.1 COc1cccc2c1CCC1CN(CCn3c(=O)[nH]c4c(oc5ccccc54)c3=O)CC21 10.1021/jm990567u
71454865 84166 0 None -2 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153551 84166 0 None -2 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2221145 84166 0 None -2 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
10698630 44167 0 None 1230 3 Human 8.7 pKi = 8.7 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 589 11 3 8 3.4 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
CHEMBL151878 44167 0 None 1230 3 Human 8.7 pKi = 8.7 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 589 11 3 8 3.4 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
11857791 85199 0 None 10 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 554 7 1 6 4.9 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2007.04.098
CHEMBL228390 85199 0 None 10 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 554 7 1 6 4.9 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2007.04.098
11857638 143266 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 516 9 1 6 5.0 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL390129 143266 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 516 9 1 6 5.0 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
10792591 205086 0 None 15 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 542 7 1 4 4.7 CC(=O)N1C(=O)N(C)C(C)=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1016/j.ejmech.2017.03.025
CHEMBL90453 205086 0 None 15 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hrDisplacement of [125I]L-762,459 from recombinant human alpha1a adrenergic receptor expressed in mammalian cells measured after 1 hr
ChEMBL 542 7 1 4 4.7 CC(=O)N1C(=O)N(C)C(C)=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1016/j.ejmech.2017.03.025
11071135 206258 0 None 3 9 Bovine 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
CHEMBL97333 206258 0 None 3 9 Bovine 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
56837419 68947 0 None -9 5 Pig 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928128 68947 0 None -9 5 Pig 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
10792591 205086 0 None 15 3 Human 8.7 pKi = 8.7 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 542 7 1 4 4.7 CC(=O)N1C(=O)N(C)C(C)=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm990612y
CHEMBL90453 205086 0 None 15 3 Human 8.7 pKi = 8.7 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 542 7 1 4 4.7 CC(=O)N1C(=O)N(C)C(C)=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm990612y
44447005 94275 0 None -7 4 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 446 6 1 5 4.2 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)C1CC1 10.1016/j.bmcl.2007.11.106
CHEMBL253024 94275 0 None -7 4 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 446 6 1 5 4.2 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)C1CC1 10.1016/j.bmcl.2007.11.106
6604803 116005 2 None 7 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL336161 116005 2 None 7 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
10406315 192712 0 None 120 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membraneDisplacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membrane
ChEMBL 361 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(Cl)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL524439 192712 0 None 120 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membraneDisplacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membrane
ChEMBL 361 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(Cl)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
134152568 152541 0 None 1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 354 7 0 4 3.8 COc1ccc(CCN2CCN(c3ccccc3OC(C)C)CC2)cc1 10.1016/j.ejmech.2016.06.052
CHEMBL3976144 152541 0 None 1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 354 7 0 4 3.8 COc1ccc(CCN2CCN(c3ccccc3OC(C)C)CC2)cc1 10.1016/j.ejmech.2016.06.052
11014848 203404 0 None 1 4 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 399 7 1 8 1.5 COc1ccccc1N1CCN(CCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL77901 203404 0 None 1 4 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 399 7 1 8 1.5 COc1ccccc1N1CCN(CCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
10791843 162836 0 None 138 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 511 7 2 4 3.7 CN1C=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@H](c2ccc(F)c(F)c2)NC1=O 10.1021/jm990612y
CHEMBL419497 162836 0 None 138 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 511 7 2 4 3.7 CN1C=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@H](c2ccc(F)c(F)c2)NC1=O 10.1021/jm990612y
2389 3267 114 None -14 68 Human 8.6 pKi = 8.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3267 114 None -14 68 Human 8.6 pKi = 8.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3267 114 None -14 68 Human 8.6 pKi = 8.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3267 114 None -14 68 Human 8.6 pKi = 8.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3267 114 None -14 68 Human 8.6 pKi = 8.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
44299945 101443 0 None 41 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.3 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@H](N3CCC(C#N)(c4ccccc4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL301024 101443 0 None 41 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.3 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@H](N3CCC(C#N)(c4ccccc4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
44294958 187737 0 None 151 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 554 7 3 7 1.9 NC(=O)c1ccccc1N1CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
CHEMBL50081 187737 0 None 151 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 554 7 3 7 1.9 NC(=O)c1ccccc1N1CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
71508687 86612 0 None 33 2 Bovine 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 385 3 0 3 5.6 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cccnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2325932 86612 0 None 33 2 Bovine 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 385 3 0 3 5.6 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cccnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
489 145 22 None -3 13 Human 8.6 pKi = 8.6 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
5640 145 22 None -3 13 Human 8.6 pKi = 8.6 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
CHEMBL420060 145 22 None -3 13 Human 8.6 pKi = 8.6 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
76333280 84379 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 421 8 1 5 5.3 COc1cccc(OC)c1OCCN[C@H]1C[C@H](c2ccccc2)c2ccccc2S1 10.1007/s00044-010-9379-1
CHEMBL2234442 84379 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 421 8 1 5 5.3 COc1cccc(OC)c1OCCN[C@H]1C[C@H](c2ccccc2)c2ccccc2S1 10.1007/s00044-010-9379-1
11133868 154791 0 None 4 7 Human 8.6 pKi = 8.6 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNC[C@H]1C[C@H](c2ccccc2)c2ccccc2S1 10.1021/jm011066n
CHEMBL40325 154791 0 None 4 7 Human 8.6 pKi = 8.6 Binding
Affinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptorAffinity constant on CHO cells expressing Human recombinant Alpha-1A adrenergic receptor
ChEMBL 435 9 1 5 5.4 COc1cccc(OC)c1OCCNC[C@H]1C[C@H](c2ccccc2)c2ccccc2S1 10.1021/jm011066n
76333280 84379 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 421 8 1 5 5.3 COc1cccc(OC)c1OCCN[C@H]1C[C@H](c2ccccc2)c2ccccc2S1 10.1007/s00044-010-9379-1
CHEMBL2234442 84379 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 421 8 1 5 5.3 COc1cccc(OC)c1OCCN[C@H]1C[C@H](c2ccccc2)c2ccccc2S1 10.1007/s00044-010-9379-1
132266 1247 9 None -9 9 Bovine 8.6 pKi = 8.6 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm960510x
486 1247 9 None -9 9 Bovine 8.6 pKi = 8.6 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm960510x
CHEMBL423294 1247 9 None -9 9 Bovine 8.6 pKi = 8.6 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm960510x
19085894 203837 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in COS-7 cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in COS-7 cells
ChEMBL 533 7 0 9 2.3 CS(=O)(=O)c1ccc2c(c1)S(=O)(=O)N(CCCCN1CCC(n3c(=O)oc4ccccc43)CC1)C2=O 10.1016/s0960-894x(98)00446-6
CHEMBL81173 203837 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in COS-7 cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in COS-7 cells
ChEMBL 533 7 0 9 2.3 CS(=O)(=O)c1ccc2c(c1)S(=O)(=O)N(CCCCN1CCC(n3c(=O)oc4ccccc43)CC1)C2=O 10.1016/s0960-894x(98)00446-6
3037308 43814 19 None -1 7 Rat 8.6 pKi = 8.6 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
CHEMBL151475 43814 19 None -1 7 Rat 8.6 pKi = 8.6 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
3584 3706 60 None -2 14 Human 8.6 pKi = 8.6 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
5401 3706 60 None -2 14 Human 8.6 pKi = 8.6 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
7302 3706 60 None -2 14 Human 8.6 pKi = 8.6 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
CHEMBL611 3706 60 None -2 14 Human 8.6 pKi = 8.6 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
DB01162 3706 60 None -2 14 Human 8.6 pKi = 8.6 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
44300159 101352 0 None 275 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.3 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@@H](N3CCC(C#N)(c4ccccc4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL300355 101352 0 None 275 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.3 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@@H](N3CCC(C#N)(c4ccccc4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
44300170 167686 0 None 4 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.5 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL433832 167686 0 None 4 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 607 7 2 7 4.5 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
10793261 120527 0 None 2290 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 575 10 3 8 3.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm990200p
CHEMBL356829 120527 0 None 2290 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 575 10 3 8 3.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm990200p
10326069 39044 1 None 23 9 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
CHEMBL147077 39044 1 None 23 9 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
490 190 5 None -36 12 Rat 8.6 pKi = 8.6 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
9890547 190 5 None -36 12 Rat 8.6 pKi = 8.6 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
CHEMBL268758 190 5 None -36 12 Rat 8.6 pKi = 8.6 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
10647424 205044 0 None 741 2 Human 8.6 pKi = 8.6 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 455 7 3 4 3.0 O=C1NC=C(C(=O)NCCCN2CCC(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1021/jm990612y
CHEMBL90210 205044 0 None 741 2 Human 8.6 pKi = 8.6 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 455 7 3 4 3.0 O=C1NC=C(C(=O)NCCCN2CCC(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1021/jm990612y
9909211 93761 1 None 1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 404 8 2 7 1.9 COc1ccc(Cl)cc1N1CCN(CCCNc2nccc(C(N)=O)n2)CC1 10.1021/jm960697s
CHEMBL24981 93761 1 None 1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 404 8 2 7 1.9 COc1ccc(Cl)cc1N1CCN(CCCNc2nccc(C(N)=O)n2)CC1 10.1021/jm960697s
52940951 16883 0 None -3 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 427 12 1 5 5.0 COc1cccc(Cl)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1254828 16883 0 None -3 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 427 12 1 5 5.0 COc1cccc(Cl)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
52943356 16884 0 None -2 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 407 12 1 5 4.6 COc1cccc(C)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1254829 16884 0 None -2 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 407 12 1 5 4.6 COc1cccc(C)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
3584 3706 60 None -3 14 Bovine 8.6 pKi = 8.6 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970166j
5401 3706 60 None -3 14 Bovine 8.6 pKi = 8.6 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970166j
7302 3706 60 None -3 14 Bovine 8.6 pKi = 8.6 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970166j
CHEMBL611 3706 60 None -3 14 Bovine 8.6 pKi = 8.6 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970166j
DB01162 3706 60 None -3 14 Bovine 8.6 pKi = 8.6 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970166j
44298735 196773 0 None 39 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 472 8 1 6 3.0 CC(C)c1c[nH]c(=O)n(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
CHEMBL57740 196773 0 None 39 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 472 8 1 6 3.0 CC(C)c1c[nH]c(=O)n(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
10674647 38725 0 None 457 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 574 10 2 8 4.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
CHEMBL146815 38725 0 None 457 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 574 10 2 8 4.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
10674647 38725 0 None 457 3 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 574 10 2 8 4.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
CHEMBL146815 38725 0 None 457 3 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 574 10 2 8 4.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
11144555 203517 0 None 2 4 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 433 8 1 7 3.1 COc1ccccc1N1CCN(CCCNc2cc(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL78785 203517 0 None 2 4 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 433 8 1 7 3.1 COc1ccccc1N1CCN(CCCNc2cc(-c3ccccc3)nn(C)c2=O)CC1 10.1021/jm0009336
3157 1437 69 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm00018a001
7170 1437 69 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm00018a001
954 1437 69 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm00018a001
CHEMBL707 1437 69 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm00018a001
DB00590 1437 69 None -2 12 Human 8.6 pKi = 8.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm00018a001
490 190 5 None -25 12 Human 8.6 pKi = 8.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/j.bmcl.2004.11.032
9890547 190 5 None -25 12 Human 8.6 pKi = 8.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/j.bmcl.2004.11.032
CHEMBL268758 190 5 None -25 12 Human 8.6 pKi = 8.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/j.bmcl.2004.11.032
10576280 110916 0 None - 1 Human 8.6 pKi = 8.6 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 469 7 3 4 3.4 CC1=C(C(=O)NCCCN2CCC(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
CHEMBL327327 110916 0 None - 1 Human 8.6 pKi = 8.6 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 469 7 3 4 3.4 CC1=C(C(=O)NCCCN2CCC(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)NC(=O)N1 10.1021/jm990612y
9891166 33377 0 None -6 5 Rat 8.6 pKi = 8.6 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 476 6 0 8 3.3 COc1ccccc1N1CCN(CCn2c(=O)c3c(-c4ccccc4)csc3n(C)c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL14213 33377 0 None -6 5 Rat 8.6 pKi = 8.6 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 476 6 0 8 3.3 COc1ccccc1N1CCN(CCn2c(=O)c3c(-c4ccccc4)csc3n(C)c2=O)CC1 10.1016/s0960-894x(01)00159-7
490 190 5 None -25 12 Human 8.6 pKi = 8.6 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
9890547 190 5 None -25 12 Human 8.6 pKi = 8.6 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
CHEMBL268758 190 5 None -25 12 Human 8.6 pKi = 8.6 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
9847845 28226 0 None -10 6 Human 8.6 pKi = 8.6 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(C)c(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL13754 28226 0 None -10 6 Human 8.6 pKi = 8.6 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3sc(C)c(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
155532148 171125 0 None -1 7 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(CC2COCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2019.02.056
CHEMBL4466677 171125 0 None -1 7 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(CC2COCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2019.02.056
44431545 87639 0 None 12 4 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 457 7 1 5 3.9 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234669 87639 0 None 12 4 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 457 7 1 5 3.9 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
44431174 92357 0 None -8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 515 5 0 5 5.5 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4cc(Cl)c(Cl)cc4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
CHEMBL243692 92357 0 None -8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 515 5 0 5 5.5 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4cc(Cl)c(Cl)cc4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
71508683 86607 0 None 56 2 Bovine 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 388 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cnn(C)c4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2325928 86607 0 None 56 2 Bovine 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 388 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cnn(C)c4)cc23)CC1 10.1016/j.bmc.2012.10.049
44447001 154923 0 None -30 4 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 378 4 1 5 3.6 NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
CHEMBL404000 154923 0 None -30 4 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 378 4 1 5 3.6 NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
10716964 100113 0 None 1 3 Rat 8.6 pKi = 8.6 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 419 4 1 5 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(C)cc(C)cc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL291769 100113 0 None 1 3 Rat 8.6 pKi = 8.6 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 419 4 1 5 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(C)cc(C)cc4c3=O)C[C@@H]21 10.1021/jm000541z
11655728 16451 7 None -39 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor by filtration binding assayDisplacement of [3H]prazosin from human adrenergic alpha1A receptor by filtration binding assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241913 16451 7 None -39 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptor by filtration binding assayDisplacement of [3H]prazosin from human adrenergic alpha1A receptor by filtration binding assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
134147055 149030 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 354 7 0 4 3.8 COc1cccc(CCN2CCN(c3ccccc3OC(C)C)CC2)c1 10.1016/j.ejmech.2016.06.052
CHEMBL3946843 149030 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 354 7 0 4 3.8 COc1cccc(CCN2CCN(c3ccccc3OC(C)C)CC2)c1 10.1016/j.ejmech.2016.06.052
2389 3267 114 None -14 68 Human 8.6 pKi = 8.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2004.11.032
5073 3267 114 None -14 68 Human 8.6 pKi = 8.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2004.11.032
96 3267 114 None -14 68 Human 8.6 pKi = 8.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2004.11.032
CHEMBL85 3267 114 None -14 68 Human 8.6 pKi = 8.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2004.11.032
DB00734 3267 114 None -14 68 Human 8.6 pKi = 8.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2004.11.032
31101 719 39 None -4 36 Rat 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 719 39 None -4 36 Rat 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 719 39 None -4 36 Rat 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 719 39 None -4 36 Rat 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 719 39 None -4 36 Rat 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
11154198 199919 0 None -5 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 413 6 0 5 3.3 CC(C)Oc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
CHEMBL60583 199919 0 None -5 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 413 6 0 5 3.3 CC(C)Oc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
11994797 12193 0 None 1 7 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 369 7 1 5 3.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)CCCC2 10.1021/jm060358r
CHEMBL1185017 12193 0 None 1 7 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 369 7 1 5 3.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)CCCC2 10.1021/jm060358r
CHEMBL383938 12193 0 None 1 7 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 369 7 1 5 3.4 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)CCCC2 10.1021/jm060358r
45268939 194975 0 None -4 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 505 4 1 9 3.0 COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1021/jm8016046
CHEMBL564481 194975 0 None -4 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 505 4 1 9 3.0 COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1021/jm8016046
11154198 199919 0 None -5 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 413 6 0 5 3.3 CC(C)Oc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
CHEMBL60583 199919 0 None -5 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 413 6 0 5 3.3 CC(C)Oc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
11487449 193807 0 None -1 4 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 437 5 0 4 4.2 O=C1CC2(CCCC2)CC(=O)N1CCCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL55319 193807 0 None -1 4 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 437 5 0 4 4.2 O=C1CC2(CCCC2)CC(=O)N1CCCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
10506674 119206 0 None 354 3 Human 8.5 pKi = 8.5 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 542 9 3 7 3.4 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
CHEMBL347559 119206 0 None 354 3 Human 8.5 pKi = 8.5 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 542 9 3 7 3.4 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
46934787 16492 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 465 7 0 7 2.2 COc1ccccc1N1CCN(C[C@H]2CO[C@@](CN3C(=O)CCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242724 16492 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 465 7 0 7 2.2 COc1ccccc1N1CCN(C[C@H]2CO[C@@](CN3C(=O)CCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
3584 3706 60 None -2 14 Human 8.5 pKi = 8.5 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
5401 3706 60 None -2 14 Human 8.5 pKi = 8.5 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
7302 3706 60 None -2 14 Human 8.5 pKi = 8.5 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
CHEMBL611 3706 60 None -2 14 Human 8.5 pKi = 8.5 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
DB01162 3706 60 None -2 14 Human 8.5 pKi = 8.5 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
134147929 149097 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 340 7 0 4 3.5 CCOc1ccccc1N1CCN(CCc2cccc(OC)c2)CC1 10.1016/j.ejmech.2016.06.052
CHEMBL3947302 149097 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 340 7 0 4 3.5 CCOc1ccccc1N1CCN(CCc2cccc(OC)c2)CC1 10.1016/j.ejmech.2016.06.052
11145007 163530 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 461 9 1 8 3.0 COc1ccc(Cl)cc1N1CCN(CCCCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL420959 163530 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligandBinding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
ChEMBL 461 9 1 8 3.0 COc1ccc(Cl)cc1N1CCN(CCCCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
19085832 163213 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 483 6 0 7 3.5 Cc1cc(C)c2oc(=O)n(C3CCN(CCCCN4C(=O)c5ccccc5S4(=O)=O)CC3)c2c1 10.1016/s0960-894x(98)00446-6
CHEMBL420578 163213 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 483 6 0 7 3.5 Cc1cc(C)c2oc(=O)n(C3CCN(CCCCN4C(=O)c5ccccc5S4(=O)=O)CC3)c2c1 10.1016/s0960-894x(98)00446-6
2337 3193 72 None -5 63 Human 7.7 pKi = 7.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3193 72 None -5 63 Human 7.7 pKi = 7.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3193 72 None -5 63 Human 7.7 pKi = 7.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3193 72 None -5 63 Human 7.7 pKi = 7.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3193 72 None -5 63 Human 7.7 pKi = 7.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
10578926 118448 0 None 75 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 1 7 4.5 COC(=O)C1=C(C)N=C(C)N(CCC[C@@H](C)CN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL342347 118448 0 None 75 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 1 7 4.5 COC(=O)C1=C(C)N=C(C)N(CCC[C@@H](C)CN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
9890459 16735 0 None 13 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 460 10 1 7 1.3 CCOC(=O)C1CCC(=O)N1CC(=O)NCCN1CCN(c2ccccc2OC(C)C)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL12529 16735 0 None 13 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 460 10 1 7 1.3 CCOC(=O)C1CCC(=O)N1CC(=O)NCCN1CCN(c2ccccc2OC(C)C)CC1 10.1016/s0960-894x(00)00169-4
45560410 1065 0 None -891 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 340 6 1 5 1.6 COc1ccccc1N1CCN(CC1)CCNC(=O)c1ccccn1 10.1021/acs.jmedchem.2c00633
9825 1065 0 None -891 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 340 6 1 5 1.6 COc1ccccc1N1CCN(CC1)CCNC(=O)c1ccccn1 10.1021/acs.jmedchem.2c00633
CHEMBL4205290 1065 0 None -891 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 340 6 1 5 1.6 COc1ccccc1N1CCN(CC1)CCNC(=O)c1ccccn1 10.1021/acs.jmedchem.2c00633
10640907 4828 0 None -21 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 340 6 1 5 1.6 COc1ccccc1N1CCN(CCNC(=O)c2ccncc2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL104593 4828 0 None -21 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 340 6 1 5 1.6 COc1ccccc1N1CCN(CCNC(=O)c2ccncc2)CC1 10.1021/acs.jmedchem.2c00633
56971026 68885 0 None -12 4 Human 7.7 pKi = 7.7 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 378 7 1 6 2.1 COc1ccccc1N1CCN(CCCN/C(=N\C#N)c2ccccn2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL1927088 68885 0 None -12 4 Human 7.7 pKi = 7.7 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 378 7 1 6 2.1 COc1ccccc1N1CCN(CCCN/C(=N\C#N)c2ccccn2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5172506 68885 0 None -12 4 Human 7.7 pKi = 7.7 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 378 7 1 6 2.1 COc1ccccc1N1CCN(CCCN/C(=N\C#N)c2ccccn2)CC1 10.1021/acs.jmedchem.2c00633
44431553 87044 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 525 7 1 5 4.9 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL233416 87044 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 525 7 1 5 4.9 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
44390704 64207 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 445 7 2 10 -0.2 Cn1c(NCCCN2CCN(c3ccc4c(c3)OCC(CO)O4)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2004.11.032
CHEMBL181475 64207 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 445 7 2 10 -0.2 Cn1c(NCCCN2CCN(c3ccc4c(c3)OCC(CO)O4)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2004.11.032
44331090 206642 0 None 6 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 464 5 1 5 4.3 CS(=O)(=O)Nc1ccc2c(c1)OC1(CCN(CCc3cccc4ccccc34)CC1)CC2=O 10.1016/s0960-894x(98)00732-x
CHEMBL99614 206642 0 None 6 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 464 5 1 5 4.3 CS(=O)(=O)Nc1ccc2c(c1)OC1(CCN(CCc3cccc4ccccc34)CC1)CC2=O 10.1016/s0960-894x(98)00732-x
13141183 161402 1 None 15 2 Bovine 7.7 pKi = 7.7 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 310 0 0 2 4.6 CN1CCC(=C2c3cc(Cl)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL415761 161402 1 None 15 2 Bovine 7.7 pKi = 7.7 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 310 0 0 2 4.6 CN1CCC(=C2c3cc(Cl)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
3251 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
5684 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
80 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
CHEMBL31354 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
10839106 111092 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 500 7 2 3 4.5 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1021/jm990612y
CHEMBL328268 111092 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 500 7 2 3 4.5 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H](c2ccc(F)c(F)c2)NC(=O)N1C 10.1021/jm990612y
11800744 205590 0 None 10 3 Human 7.7 pKi = 7.7 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 547 7 3 4 4.4 N#Cc1ccccc1C1CCN(CCCNC(=O)C2=C(C(F)(F)F)NC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
CHEMBL93523 205590 0 None 10 3 Human 7.7 pKi = 7.7 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 547 7 3 4 4.4 N#Cc1ccccc1C1CCN(CCCNC(=O)C2=C(C(F)(F)F)NC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
24854106 160502 1 None 2 8 Human 7.7 pKi = 7.7 Binding
Inhibition of adrenergic alpha-1 receptorInhibition of adrenergic alpha-1 receptor
ChEMBL 367 6 1 3 3.9 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm070279v
CHEMBL411663 160502 1 None 2 8 Human 7.7 pKi = 7.7 Binding
Inhibition of adrenergic alpha-1 receptorInhibition of adrenergic alpha-1 receptor
ChEMBL 367 6 1 3 3.9 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm070279v
3251 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Inhibition of adrenergic alpha1A receptorInhibition of adrenergic alpha1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
5684 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Inhibition of adrenergic alpha1A receptorInhibition of adrenergic alpha1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
80 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Inhibition of adrenergic alpha1A receptorInhibition of adrenergic alpha1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
CHEMBL31354 3997 50 None -64 12 Human 7.7 pKi = 7.7 Binding
Inhibition of adrenergic alpha1A receptorInhibition of adrenergic alpha1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
10603951 204780 0 None 11 6 Human 7.7 pKi = 7.7 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 622 10 1 7 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)N(C)CCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL88448 204780 0 None 11 6 Human 7.7 pKi = 7.7 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 622 10 1 7 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)N(C)CCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
10603951 84833 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 622 10 1 7 5.9 COC(=O)C1=C(C)NC(C)=C(C(=O)N(C)CCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL2260148 84833 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 622 10 1 7 5.9 COC(=O)C1=C(C)NC(C)=C(C(=O)N(C)CCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
11097789 102511 0 None -4 6 Human 7.7 pKi = 7.7 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL306792 102511 0 None -4 6 Human 7.7 pKi = 7.7 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
10934575 202771 0 None -1 6 Human 7.7 pKi = 7.7 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72441 202771 0 None -1 6 Human 7.7 pKi = 7.7 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
9894818 98455 0 None 83 7 Human 7.7 pKi = 7.7 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL279436 98455 0 None 83 7 Human 7.7 pKi = 7.7 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
9894818 98455 0 None 83 7 Human 7.7 pKi = 7.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
CHEMBL279436 98455 0 None 83 7 Human 7.7 pKi = 7.7 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
53328684 63053 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 480 9 0 7 3.4 COc1ccccc1N1CCN(CCCCN2C(=O)CC(c3ccc([N+](=O)[O-])cc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796043 63053 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 480 9 0 7 3.4 COc1ccccc1N1CCN(CCCCN2C(=O)CC(c3ccc([N+](=O)[O-])cc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
46881494 6515 0 None -20 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 421 9 1 5 4.7 COc1ccccc1OCCNCC1CSC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
CHEMBL1083182 6515 0 None -20 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 421 9 1 5 4.7 COc1ccccc1OCCNCC1CSC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
10106205 205398 1 None -12 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards alpha-1-adrenergic receptorBinding affinity towards alpha-1-adrenergic receptor
ChEMBL 251 2 2 3 3.0 Cc1c(NC2=NCCN2)cccc1-c1ccccc1 10.1021/jm030030n
CHEMBL92221 205398 1 None -12 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards alpha-1-adrenergic receptorBinding affinity towards alpha-1-adrenergic receptor
ChEMBL 251 2 2 3 3.0 Cc1c(NC2=NCCN2)cccc1-c1ccccc1 10.1021/jm030030n
10183297 92867 0 None -109 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245231 92867 0 None -109 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
102 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00375a017
3659 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00375a017
8969 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00375a017
CHEMBL15245 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00375a017
DB01392 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00375a017
57393634 68962 0 None -1 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928248 68962 0 None -1 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
2737203 183332 76 None -141 2 Bovine 5.7 pKi = 5.7 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 188 1 1 4 0.4 N#Cc1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL48137 183332 76 None -141 2 Bovine 5.7 pKi = 5.7 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 188 1 1 4 0.4 N#Cc1cccnc1N1CCNCC1 10.1021/jm00366a007
1028 287 69 None -30 30 Human 5.7 pKi = 5.7 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
139148732 287 69 None -30 30 Human 5.7 pKi = 5.7 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
479 287 69 None -30 30 Human 5.7 pKi = 5.7 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
5816 287 69 None -30 30 Human 5.7 pKi = 5.7 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
CHEMBL679 287 69 None -30 30 Human 5.7 pKi = 5.7 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
DB00668 287 69 None -30 30 Human 5.7 pKi = 5.7 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
43260 5393 61 None -1 5 Rat 5.7 pKi = 5.7 Binding
Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (1.6 -2.5)Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (1.6 -2.5)
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1021/jm025550h
CHEMBL1076 5393 61 None -1 5 Rat 5.7 pKi = 5.7 Binding
Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (1.6 -2.5)Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (1.6 -2.5)
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1021/jm025550h
10892762 78396 0 None -52 6 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 326 7 1 4 3.8 COc1cccc(C2CCC(NCCOc3ccccn3)CC2)c1 10.1021/jm010866v
CHEMBL2112774 78396 0 None -52 6 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 326 7 1 4 3.8 COc1cccc(C2CCC(NCCOc3ccccn3)CC2)c1 10.1021/jm010866v
12134995 101659 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 318 5 1 5 2.6 COc1ccccc1N1CCN(Cc2ccc(CO)s2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL302495 101659 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 318 5 1 5 2.6 COc1ccccc1N1CCN(Cc2ccc(CO)s2)CC1 10.1016/s0960-894x(02)00347-5
9885114 119086 3 None -47 12 Rat 6.7 pKi = 6.7 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
CHEMBL346389 119086 3 None -47 12 Rat 6.7 pKi = 6.7 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
218362 203082 5 None -75 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 216 1 1 3 2.0 c1ccc2c(c1)CCCC2NC1=NCCO1 10.1016/0960-894X(94)85032-1
CHEMBL75030 203082 5 None -75 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 216 1 1 3 2.0 c1ccc2c(c1)CCCC2NC1=NCCO1 10.1016/0960-894X(94)85032-1
9904606 9281 0 None -2 4 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 305 3 1 3 2.3 CN(c1cccc2c1CCCC2c1c[nH]cn1)S(C)(=O)=O 10.1021/jm030551a
CHEMBL111463 9281 0 None -2 4 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 305 3 1 3 2.3 CN(c1cccc2c1CCCC2c1c[nH]cn1)S(C)(=O)=O 10.1021/jm030551a
11347303 110879 0 None -91 5 Bovine 5.7 pKi = 5.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1ccc2c(c1)C(c1c[nH]cn1)CCC2 10.1021/jm030551a
CHEMBL327116 110879 0 None -91 5 Bovine 5.7 pKi = 5.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1ccc2c(c1)C(c1c[nH]cn1)CCC2 10.1021/jm030551a
1220 186 46 None -1659 45 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030944+
31 186 46 None -1659 45 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030944+
7 186 46 None -1659 45 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030944+
CHEMBL56 186 46 None -1659 45 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030944+
11857709 85198 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 556 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL228389 85198 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 556 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
11857709 85198 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 556 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL228389 85198 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 556 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
26987 934 29 None -75 21 Rat 7.7 pKi = 7.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 934 29 None -75 21 Rat 7.7 pKi = 7.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 934 29 None -75 21 Rat 7.7 pKi = 7.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 934 29 None -75 21 Rat 7.7 pKi = 7.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 934 29 None -75 21 Rat 7.7 pKi = 7.7 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
9798183 13014 0 None -33 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 343 5 1 2 4.4 Fc1ccc2c(C3CCN(CCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
CHEMBL1190579 13014 0 None -33 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 343 5 1 2 4.4 Fc1ccc2c(C3CCN(CCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
CHEMBL541129 13014 0 None -33 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 343 5 1 2 4.4 Fc1ccc2c(C3CCN(CCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
11496213 15883 0 None -35 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 454 8 1 4 6.1 Clc1cccc(N2CCN(CCCCNc3ccc(-c4ccccc4)cn3)CC2)c1Cl 10.1016/j.bmcl.2010.07.096
CHEMBL1223800 15883 0 None -35 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 454 8 1 4 6.1 Clc1cccc(N2CCN(CCCCNc3ccc(-c4ccccc4)cn3)CC2)c1Cl 10.1016/j.bmcl.2010.07.096
46934789 16497 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 479 7 0 7 2.6 COc1ccccc1N1CCN(C[C@@H]2CO[C@@](CN3C(=O)CCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242819 16497 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 479 7 0 7 2.6 COc1ccccc1N1CCN(C[C@@H]2CO[C@@](CN3C(=O)CCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
118716708 114491 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 441 5 0 7 2.5 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)c4ccco4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342861 114491 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 441 5 0 7 2.5 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)c4ccco4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
73346042 91388 3 None -213 17 Human 7.7 pKi = 7.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91388 3 None -213 17 Human 7.7 pKi = 7.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
73346042 91388 3 None -213 17 Human 7.7 pKi = 7.7 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1021/acs.jmedchem.2c00633
CHEMBL2413153 91388 3 None -213 17 Human 7.7 pKi = 7.7 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1021/acs.jmedchem.2c00633
53328316 63046 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 449 9 0 5 3.9 COc1ccccc1N1CCN(CCCCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796036 63046 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 449 9 0 5 3.9 COc1ccccc1N1CCN(CCCCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
13938356 184485 0 None -154 2 Bovine 6.7 pKi = 6.7 Binding
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortexEvaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN(C1CCN2CCc3c(oc4ccccc34)C2C1)S(=O)(=O)CCO 10.1021/jm00150a002
CHEMBL48558 184485 0 None -154 2 Bovine 6.7 pKi = 6.7 Binding
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortexEvaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN(C1CCN2CCc3c(oc4ccccc34)C2C1)S(=O)(=O)CCO 10.1021/jm00150a002
127027079 137238 0 None -416 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 442 7 2 4 3.7 O=C1Cc2c(cccc2N2CCN(CCCCNC(=O)c3ccc4ccccc4c3)CC2)N1 10.1016/j.bmcl.2015.12.068
CHEMBL3759441 137238 0 None -416 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 442 7 2 4 3.7 O=C1Cc2c(cccc2N2CCN(CCCCNC(=O)c3ccc4ccccc4c3)CC2)N1 10.1016/j.bmcl.2015.12.068
145946733 167008 0 None -14 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 368 7 0 4 4.2 COc1ccc(N2CCN(CCCOc3c(C)cc(C)cc3C)CC2)cc1 10.1016/j.bmcl.2018.04.059
CHEMBL4205526 167008 0 None -14 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 368 7 0 4 4.2 COc1ccc(N2CCN(CCCOc3c(C)cc(C)cc3C)CC2)cc1 10.1016/j.bmcl.2018.04.059
CHEMBL4300710 167008 0 None -14 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 368 7 0 4 4.2 COc1ccc(N2CCN(CCCOc3c(C)cc(C)cc3C)CC2)cc1 10.1016/j.bmcl.2018.04.059
11176459 101153 0 None -229 5 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 380 4 0 5 2.4 N#Cc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
CHEMBL299022 101153 0 None -229 5 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 380 4 0 5 2.4 N#Cc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
44312037 202903 1 None -2 6 Human 4.7 pKi = 4.7 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 308 1 1 5 2.9 Brc1c(NC2=NCCS2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL73392 202903 1 None -2 6 Human 4.7 pKi = 4.7 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 308 1 1 5 2.9 Brc1c(NC2=NCCS2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
179268 101683 6 None -4 2 Human 5.7 pKi = 5.7 Binding
Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 454 2 3 1 6.2 Brc1ccc2c(-c3c[nH]c(-c4c[nH]c5cc(Br)ccc45)n3)c[nH]c2c1 10.1016/0960-894X(96)00376-9
CHEMBL302637 101683 6 None -4 2 Human 5.7 pKi = 5.7 Binding
Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 454 2 3 1 6.2 Brc1ccc2c(-c3c[nH]c(-c4c[nH]c5cc(Br)ccc45)n3)c[nH]c2c1 10.1016/0960-894X(96)00376-9
11959098 178946 50 None -79 2 Bovine 6.7 pKi = 6.7 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 211 1 0 3 1.5 CN1CCN(c2ncccc2Cl)CC1 10.1021/jm00366a007
CHEMBL47415 178946 50 None -79 2 Bovine 6.7 pKi = 6.7 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 211 1 0 3 1.5 CN1CCN(c2ncccc2Cl)CC1 10.1021/jm00366a007
10737133 204925 0 None -15 2 Rat 6.7 pKi = 6.7 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 358 6 0 5 2.3 COc1ccccc1N1CCN(CCCN2CC3CCCCN3C2)CC1 10.1021/jm970216k
CHEMBL89380 204925 0 None -15 2 Rat 6.7 pKi = 6.7 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 358 6 0 5 2.3 COc1ccccc1N1CCN(CCCN2CC3CCCCN3C2)CC1 10.1021/jm970216k
10028436 3463 3 None -109 12 Human 6.7 pKi = 6.7 Binding
Compound was tested for its binding affinity for Alpha 1B adrenergic receptorCompound was tested for its binding affinity for Alpha 1B adrenergic receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 3463 3 None -109 12 Human 6.7 pKi = 6.7 Binding
Compound was tested for its binding affinity for Alpha 1B adrenergic receptorCompound was tested for its binding affinity for Alpha 1B adrenergic receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 3463 3 None -109 12 Human 6.7 pKi = 6.7 Binding
Compound was tested for its binding affinity for Alpha 1B adrenergic receptorCompound was tested for its binding affinity for Alpha 1B adrenergic receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
10903226 13643 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 281 6 2 5 1.3 CCCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1195368 13643 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 281 6 2 5 1.3 CCCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL554416 13643 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 281 6 2 5 1.3 CCCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44314200 102466 0 None -81 4 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 230 1 1 3 2.4 c1ccc2c(c1)CCCC2NC1=NCCCO1 10.1016/0960-894X(94)85032-1
CHEMBL306377 102466 0 None -81 4 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 230 1 1 3 2.4 c1ccc2c(c1)CCCC2NC1=NCCCO1 10.1016/0960-894X(94)85032-1
10626453 121488 0 None 72 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 548 9 0 6 6.2 COC(=O)C1=C(C)N=C(C)N(CCC[C@@H](C)CN2CCC(C#N)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL359430 121488 0 None 72 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 548 9 0 6 6.2 COC(=O)C1=C(C)N=C(C)N(CCC[C@@H](C)CN2CCC(C#N)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
135398737 942 89 None -5 92 Rat 7.7 pKi = 7.7 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
38 942 89 None -5 92 Rat 7.7 pKi = 7.7 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
722 942 89 None -5 92 Rat 7.7 pKi = 7.7 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
CHEMBL42 942 89 None -5 92 Rat 7.7 pKi = 7.7 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
DB00363 942 89 None -5 92 Rat 7.7 pKi = 7.7 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
10768610 202065 0 None 24 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 532 8 2 7 2.5 COc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
CHEMBL68045 202065 0 None 24 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 532 8 2 7 2.5 COc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
9888164 17754 1 None 25 3 Human 7.7 pKi = 7.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 416 8 1 5 2.1 CC(C)Oc1ccccc1N1CCN(CCNC(=O)CN2CCCCCC2=O)CC1 10.1016/j.bmcl.2004.11.032
CHEMBL12603 17754 1 None 25 3 Human 7.7 pKi = 7.7 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 416 8 1 5 2.1 CC(C)Oc1ccccc1N1CCN(CCNC(=O)CN2CCCCCC2=O)CC1 10.1016/j.bmcl.2004.11.032
16041264 94986 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 470 6 2 4 5.4 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL257077 94986 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 470 6 2 4 5.4 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
71508710 86613 0 None 50 2 Bovine 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 368 3 0 4 4.9 CN1CCC(c2cn(-c3ccncc3)c3ccc(-c4cccnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2325933 86613 0 None 50 2 Bovine 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 368 3 0 4 4.9 CN1CCC(c2cn(-c3ccncc3)c3ccc(-c4cccnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
44289026 165822 0 None 87 3 Human 7.7 pKi = 7.7 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 533 8 1 3 6.5 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3C(F)(F)F)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
CHEMBL42763 165822 0 None 87 3 Human 7.7 pKi = 7.7 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 533 8 1 3 6.5 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3C(F)(F)F)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
9879119 9340 0 None 4 5 Rat 7.7 pKi = 7.7 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL111771 9340 0 None 4 5 Rat 7.7 pKi = 7.7 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
53327991 63056 0 None -9 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 449 8 0 5 3.7 COc1ccccc1N1CCN(CCCCN2C(=O)CC(C)(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796046 63056 0 None -9 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 449 8 0 5 3.7 COc1ccccc1N1CCN(CCCCN2C(=O)CC(C)(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
145962368 160898 0 None -74 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 521 9 0 8 5.1 CCCN(CCC)c1nc(N2CCN(C(=O)c3ccco3)[C@H]3CCCC[C@H]32)nc2cc(OC)c(OC)cc12 10.1016/j.bmc.2018.05.023
CHEMBL4127483 160898 0 None -74 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 521 9 0 8 5.1 CCCN(CCC)c1nc(N2CCN(C(=O)c3ccco3)[C@H]3CCCC[C@H]32)nc2cc(OC)c(OC)cc12 10.1016/j.bmc.2018.05.023
9879119 9340 0 None 4 5 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL111771 9340 0 None 4 5 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1c[nH]cn1 10.1021/jm030551a
102 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00366a007
3659 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00366a007
8969 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00366a007
CHEMBL15245 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00366a007
DB01392 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00366a007
145947545 167122 0 None -199 3 Human 6.7 pKi = 6.7 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 341 4 2 4 3.1 CSc1ccc(Cl)cc1Cn1cc(Cl)cc(C(N)=O)c1=N 10.1016/j.ejmech.2017.07.071
CHEMBL4208816 167122 0 None -199 3 Human 6.7 pKi = 6.7 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 341 4 2 4 3.1 CSc1ccc(Cl)cc1Cn1cc(Cl)cc(C(N)=O)c1=N 10.1016/j.ejmech.2017.07.071
CHEMBL4302269 167122 0 None -199 3 Human 6.7 pKi = 6.7 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 341 4 2 4 3.1 CSc1ccc(Cl)cc1Cn1cc(Cl)cc(C(N)=O)c1=N 10.1016/j.ejmech.2017.07.071
102 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortexEvaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00150a002
3659 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortexEvaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00150a002
8969 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortexEvaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00150a002
CHEMBL15245 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortexEvaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00150a002
DB01392 4051 44 None -85 50 Bovine 6.7 pKi = 6.7 Binding
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortexEvaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00150a002
44301572 199680 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 555 7 0 4 6.8 Cc1ccc(C2(c3ccc(C)cc3)CC(=S)N(CCCN3CCC(C#N)(c4ccccc4Cl)CC3)C2=O)cc1 10.1016/s0960-894x(01)00320-1
CHEMBL60452 199680 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 555 7 0 4 6.8 Cc1ccc(C2(c3ccc(C)cc3)CC(=S)N(CCCN3CCC(C#N)(c4ccccc4Cl)CC3)C2=O)cc1 10.1016/s0960-894x(01)00320-1
3303 2204 41 None -3162 15 Human 5.7 pKi = 5.7 Binding
Inhibition of alpha1C adrenergic receptor (unknown origin)Inhibition of alpha1C adrenergic receptor (unknown origin)
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
5311200 2204 41 None -3162 15 Human 5.7 pKi = 5.7 Binding
Inhibition of alpha1C adrenergic receptor (unknown origin)Inhibition of alpha1C adrenergic receptor (unknown origin)
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
CHEMBL267014 2204 41 None -3162 15 Human 5.7 pKi = 5.7 Binding
Inhibition of alpha1C adrenergic receptor (unknown origin)Inhibition of alpha1C adrenergic receptor (unknown origin)
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
76307952 84392 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 375 7 1 4 4.0 c1ccc(OCCNC2COC(c3ccccc3)(c3ccccc3)CO2)cc1 10.1007/s00044-010-9379-1
CHEMBL2234455 84392 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 375 7 1 4 4.0 c1ccc(OCCNC2COC(c3ccccc3)(c3ccccc3)CO2)cc1 10.1007/s00044-010-9379-1
145962817 160960 0 None -74 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 385 3 1 7 2.2 COc1cc2nc(N3CCN(C(C)=O)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4128311 160960 0 None -74 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 385 3 1 7 2.2 COc1cc2nc(N3CCN(C(C)=O)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
44568818 187112 0 None -6 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNC[C@@H]2COC(c3ccccc3)(c3ccccc3)CO2)cc1 10.1021/jm800461k
CHEMBL495289 187112 0 None -6 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNC[C@@H]2COC(c3ccccc3)(c3ccccc3)CO2)cc1 10.1021/jm800461k
6917970 3622 54 None -512 34 Rat 5.7 pKi = 5.7 Binding
Displacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 minsDisplacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 mins
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1021/acs.jmedchem.6b01217
8370 3622 54 None -512 34 Rat 5.7 pKi = 5.7 Binding
Displacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 minsDisplacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 mins
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1021/acs.jmedchem.6b01217
CHEMBL487387 3622 54 None -512 34 Rat 5.7 pKi = 5.7 Binding
Displacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 minsDisplacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 mins
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1021/acs.jmedchem.6b01217
44271903 62939 0 None - 1 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 208 1 0 2 2.5 CN1CC=C(c2ncccc2Cl)CC1 10.1021/jm00375a017
CHEMBL17926 62939 0 None - 1 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 208 1 0 2 2.5 CN1CC=C(c2ncccc2Cl)CC1 10.1021/jm00375a017
11655403 15884 0 None -208 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 454 8 1 4 5.8 FC(F)(F)c1cccc(N2CCN(CCCCNc3ccc(-c4ccccc4)cn3)CC2)c1 10.1016/j.bmcl.2010.07.096
CHEMBL1223801 15884 0 None -208 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 454 8 1 4 5.8 FC(F)(F)c1cccc(N2CCN(CCCCNc3ccc(-c4ccccc4)cn3)CC2)c1 10.1016/j.bmcl.2010.07.096
73347826 92096 0 None -1 7 Human 5.6 pKi = 5.6 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 266 4 1 2 2.4 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)nc1 10.1016/j.bmc.2013.07.045
CHEMBL2432049 92096 0 None -1 7 Human 5.6 pKi = 5.6 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 266 4 1 2 2.4 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)nc1 10.1016/j.bmc.2013.07.045
134157330 153158 0 None -75 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 321 7 1 5 2.7 COc1ccccc1OCCNCC1COC2(CCCCC2)O1 10.1016/j.ejmech.2016.09.050
CHEMBL3981480 153158 0 None -75 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 321 7 1 5 2.7 COc1ccccc1OCCNCC1COC2(CCCCC2)O1 10.1016/j.ejmech.2016.09.050
115 340 66 None -2 7 Bovine 7.6 pKi = 7.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm00018a001
2092 340 66 None -2 7 Bovine 7.6 pKi = 7.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm00018a001
7109 340 66 None -2 7 Bovine 7.6 pKi = 7.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm00018a001
CHEMBL709 340 66 None -2 7 Bovine 7.6 pKi = 7.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm00018a001
DB00346 340 66 None -2 7 Bovine 7.6 pKi = 7.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm00018a001
44431560 88720 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL236621 88720 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
44433348 89818 0 None -8 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 545 10 0 7 4.6 CCN([C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1)S(=O)(=O)c1ccc(OC)c(OC)c1 10.1016/j.bmcl.2007.09.051
CHEMBL238401 89818 0 None -8 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 545 10 0 7 4.6 CCN([C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1)S(=O)(=O)c1ccc(OC)c(OC)c1 10.1016/j.bmcl.2007.09.051
44431560 88720 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.008
CHEMBL236621 88720 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.008
11857863 85242 0 None 2 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 534 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccc(F)cc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL228658 85242 0 None 2 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 534 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccc(F)cc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
1531 2226 64 None -3 15 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
3869 2226 64 None -3 15 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
7207 2226 64 None -3 15 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
CHEMBL429 2226 64 None -3 15 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
DB00598 2226 64 None -3 15 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
49865599 15829 0 None -28 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 340 8 1 5 3.1 COc1ccccc1N1CCN(CCCCNc2ccccn2)CC1 10.1016/j.bmcl.2010.07.096
CHEMBL1223615 15829 0 None -28 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 340 8 1 5 3.1 COc1ccccc1N1CCN(CCCCNc2ccccn2)CC1 10.1016/j.bmcl.2010.07.096
11303180 196539 0 None -7 5 Human 7.6 pKi = 7.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 369 5 0 4 3.1 COc1ccccc1N1CCN(CCN2C=CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
CHEMBL57540 196539 0 None -7 5 Human 7.6 pKi = 7.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 369 5 0 4 3.1 COc1ccccc1N1CCN(CCN2C=CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
11303180 196539 0 None -7 5 Human 7.6 pKi = 7.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 369 5 0 4 3.1 COc1ccccc1N1CCN(CCN2C=CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
CHEMBL57540 196539 0 None -7 5 Human 7.6 pKi = 7.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 369 5 0 4 3.1 COc1ccccc1N1CCN(CCN2C=CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
76323010 105754 0 None -26 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 451 4 1 8 3.4 COc1cc2nc(N3CCN(C(=O)c4ccc(C)o4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
CHEMBL2261606 105754 0 None -26 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 451 4 1 8 3.4 COc1cc2nc(N3CCN(C(=O)c4ccc(C)o4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
CHEMBL3138929 105754 0 None -26 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 451 4 1 8 3.4 COc1cc2nc(N3CCN(C(=O)c4ccc(C)o4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
16721032 91742 0 None -26 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 451 4 1 8 3.4 COc1cc2nc(N3CCN(C(=O)c4ccc(C)o4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
CHEMBL242507 91742 0 None -26 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 451 4 1 8 3.4 COc1cc2nc(N3CCN(C(=O)c4ccc(C)o4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
10790988 115587 0 None -2 3 Human 7.6 pKi = 7.6 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 483 8 1 10 2.0 COc1cc2nc(N3CCN(C(=O)COc4c(OC)cccc4OC)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL335731 115587 0 None -2 3 Human 7.6 pKi = 7.6 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 483 8 1 10 2.0 COc1cc2nc(N3CCN(C(=O)COc4c(OC)cccc4OC)CC3)nc(N)c2cc1OC 10.1021/jm9805337
10621592 84134 0 None -4 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153559 84134 0 None -4 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220898 84134 0 None -4 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
4011 81982 43 None -125 24 Rat 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81982 43 None -125 24 Rat 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
127025258 137156 0 None -173 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 415 7 1 3 4.8 Cc1cccc(N2CCN(CCCCNC(=O)c3ccc4ccccc4c3)CC2)c1C 10.1016/j.bmcl.2015.12.068
CHEMBL3758741 137156 0 None -173 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 415 7 1 3 4.8 Cc1cccc(N2CCN(CCCCNC(=O)c3ccc4ccccc4c3)CC2)c1C 10.1016/j.bmcl.2015.12.068
9844022 122532 0 None -32 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 401 6 1 2 5.6 c1ccc(C2CCN(CCCN3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1016/j.bmcl.2015.07.046
CHEMBL3609358 122532 0 None -32 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 401 6 1 2 5.6 c1ccc(C2CCN(CCCN3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1016/j.bmcl.2015.07.046
12134991 203990 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 412 7 0 6 3.3 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3CCCCC3=O)co2)CC1 10.1016/s0960-894x(02)00436-5
CHEMBL82480 203990 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 412 7 0 6 3.3 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3CCCCC3=O)co2)CC1 10.1016/s0960-894x(02)00436-5
11486511 101100 0 None -691 5 Human 6.6 pKi = 6.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 403 4 0 4 3.6 O=C1CC2(CCCC2)CC(=O)N1CCN1CCCN(c2ccccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL298595 101100 0 None -691 5 Human 6.6 pKi = 6.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 403 4 0 4 3.6 O=C1CC2(CCCC2)CC(=O)N1CCN1CCCN(c2ccccc2Cl)CC1 10.1007/s00044-010-9379-1
11994671 11709 0 None 1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cc(-c2ccccc2)ccc1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182138 11709 0 None 1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cc(-c2ccccc2)ccc1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL214506 11709 0 None 1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cc(-c2ccccc2)ccc1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
2162 41258 97 None -3 6 Human 5.6 pKi = 5.6 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1016/s0960-894x(99)00484-9
CHEMBL1491 41258 97 None -3 6 Human 5.6 pKi = 5.6 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1016/s0960-894x(99)00484-9
11486511 101100 0 None -691 5 Human 6.6 pKi = 6.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 403 4 0 4 3.6 O=C1CC2(CCCC2)CC(=O)N1CCN1CCCN(c2ccccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL298595 101100 0 None -691 5 Human 6.6 pKi = 6.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 403 4 0 4 3.6 O=C1CC2(CCCC2)CC(=O)N1CCN1CCCN(c2ccccc2Cl)CC1 10.1007/s00044-010-9379-1
21509921 103966 0 None -234 24 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103966 0 None -234 24 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
21509921 103966 0 None -234 24 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103966 0 None -234 24 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
14004033 48952 5 None -2 2 Bovine 4.6 pKi = 4.6 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 177 0 1 2 1.5 c1[nH]nc2c1CCN1CCCCC21 10.1021/jm00398a025
CHEMBL156283 48952 5 None -2 2 Bovine 4.6 pKi = 4.6 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 177 0 1 2 1.5 c1[nH]nc2c1CCN1CCCCC21 10.1021/jm00398a025
9930376 122534 0 None -38 3 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 391 5 1 2 4.9 Fc1ccc2c(C3CCN(CCCN4CCc5ccccc5C4)CC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
CHEMBL3609360 122534 0 None -38 3 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 391 5 1 2 4.9 Fc1ccc2c(C3CCN(CCCN4CCc5ccccc5C4)CC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
71508686 86611 0 None 10 2 Bovine 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 368 3 0 4 4.9 CN1CCC(c2cn(-c3ccncc3)c3ccc(-c4ccncc4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2325931 86611 0 None 10 2 Bovine 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 368 3 0 4 4.9 CN1CCC(c2cn(-c3ccncc3)c3ccc(-c4ccncc4)cc23)CC1 10.1016/j.bmc.2012.10.049
44288995 162322 0 None 39 3 Human 7.6 pKi = 7.6 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 435 8 1 3 4.9 Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2ccc(F)cc2)C(C)C)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL417350 162322 0 None 39 3 Human 7.6 pKi = 7.6 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 435 8 1 3 4.9 Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2ccc(F)cc2)C(C)C)CC1 10.1016/s0960-894x(00)00307-3
10962489 11071 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 8 0 3 4.5 C[N+](C)(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
CHEMBL1178679 11071 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 8 0 3 4.5 C[N+](C)(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
CHEMBL37212 11071 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 8 0 3 4.5 C[N+](C)(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
10363912 6445 0 None -36 7 Human 7.6 pKi = 7.6 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
CHEMBL1082862 6445 0 None -36 7 Human 7.6 pKi = 7.6 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
CHEMBL286003 6445 0 None -36 7 Human 7.6 pKi = 7.6 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 405 9 1 5 4.0 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
155532835 175870 0 None -31 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 9 1 5 4.4 COc1ccccc1OCCNCC1CCOC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4467585 175870 0 None -31 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 9 1 5 4.4 COc1ccccc1OCCNCC1CCOC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4596417 175870 0 None -31 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 9 1 5 4.4 COc1ccccc1OCCNCC1CCOC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
10386062 205035 0 None -19 2 Rat 6.6 pKi = 6.6 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 396 6 0 4 3.3 FC(F)(F)c1cccc(N2CCN(CCCCN3CC4CCCN4C3)CC2)c1 10.1021/jm970216k
CHEMBL90165 205035 0 None -19 2 Rat 6.6 pKi = 6.6 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 396 6 0 4 3.3 FC(F)(F)c1cccc(N2CCN(CCCCN3CC4CCCN4C3)CC2)c1 10.1021/jm970216k
9817327 122527 0 None -50 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 285 5 1 2 3.3 CN(C)CCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2015.07.046
CHEMBL3609353 122527 0 None -50 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 285 5 1 2 3.3 CN(C)CCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2015.07.046
44289089 164022 0 None 3 3 Human 6.6 pKi = 6.6 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 453 10 1 6 3.2 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL42156 164022 0 None 3 3 Human 6.6 pKi = 6.6 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 453 10 1 6 3.2 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(00)00307-3
94459 63928 121 None -64 2 Bovine 5.6 pKi = 5.6 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 163 1 1 3 0.5 c1ccc(N2CCNCC2)nc1 10.1021/jm00366a007
CHEMBL18094 63928 121 None -64 2 Bovine 5.6 pKi = 5.6 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 163 1 1 3 0.5 c1ccc(N2CCNCC2)nc1 10.1021/jm00366a007
94459 63928 121 None -64 2 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 163 1 1 3 0.5 c1ccc(N2CCNCC2)nc1 10.1021/jm00375a017
CHEMBL18094 63928 121 None -64 2 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 163 1 1 3 0.5 c1ccc(N2CCNCC2)nc1 10.1021/jm00375a017
14004033 48952 5 None -2 2 Bovine 4.6 pKi = 4.6 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 177 0 1 2 1.5 c1[nH]nc2c1CCN1CCCCC21 10.1021/jm00398a025
CHEMBL156283 48952 5 None -2 2 Bovine 4.6 pKi = 4.6 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 177 0 1 2 1.5 c1[nH]nc2c1CCN1CCCCC21 10.1021/jm00398a025
165413025 189763 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-prazosin from human adrenergic alpha1A receptor expressed in human HEK293 cellsDisplacement of [3H]-prazosin from human adrenergic alpha1A receptor expressed in human HEK293 cells
ChEMBL 364 6 2 6 1.3 NC(CCOc1ccc(S(N)(=O)=O)cc1)C1COc2ccccc2O1 10.1021/acs.jmedchem.2c01192
CHEMBL5177166 189763 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-prazosin from human adrenergic alpha1A receptor expressed in human HEK293 cellsDisplacement of [3H]-prazosin from human adrenergic alpha1A receptor expressed in human HEK293 cells
ChEMBL 364 6 2 6 1.3 NC(CCOc1ccc(S(N)(=O)=O)cc1)C1COc2ccccc2O1 10.1021/acs.jmedchem.2c01192
2291 3123 52 None -446 12 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3123 52 None -446 12 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3123 52 None -446 12 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3123 52 None -446 12 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3123 52 None -446 12 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
44431590 87538 0 None -13 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 555 8 1 6 4.9 COc1ccc(C(F)(F)F)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234232 87538 0 None -13 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 555 8 1 6 4.9 COc1ccc(C(F)(F)F)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
44289346 167471 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 466 8 1 4 4.9 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccn3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
CHEMBL432302 167471 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 466 8 1 4 4.9 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccn3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
135398745 2858 108 None -13 66 Rat 7.6 pKi = 7.6 Binding
Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2858 108 None -13 66 Rat 7.6 pKi = 7.6 Binding
Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2858 108 None -13 66 Rat 7.6 pKi = 7.6 Binding
Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2858 108 None -13 66 Rat 7.6 pKi = 7.6 Binding
Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
15254720 60957 0 None -204 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767136 60957 0 None -204 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
24803483 60988 0 None -63 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 654 15 0 6 8.2 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767167 60988 0 None -63 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 654 15 0 6 8.2 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
132266 1247 9 None -48 9 Human 7.6 pKi = 7.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm960697s
486 1247 9 None -48 9 Human 7.6 pKi = 7.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm960697s
CHEMBL423294 1247 9 None -48 9 Human 7.6 pKi = 7.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm960697s
126225 94522 4 None -13 8 Human 7.6 pKi = 7.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm960697s
CHEMBL25467 94522 4 None -13 8 Human 7.6 pKi = 7.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm960697s
11281005 11723 0 None 13 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 399 8 1 6 3.4 COc1cccc(OC)c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL1182191 11723 0 None 13 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 399 8 1 6 3.4 COc1cccc(OC)c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL218079 11723 0 None 13 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 399 8 1 6 3.4 COc1cccc(OC)c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
76326562 105712 0 None -18 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 479 5 1 9 3.3 COc1cc2nc(N3CCN(C(=O)c4ccc(C(C)=O)o4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
CHEMBL2261608 105712 0 None -18 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 479 5 1 9 3.3 COc1cc2nc(N3CCN(C(=O)c4ccc(C(C)=O)o4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
CHEMBL3138761 105712 0 None -18 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 479 5 1 9 3.3 COc1cc2nc(N3CCN(C(=O)c4ccc(C(C)=O)o4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
44428847 91847 0 None -18 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 479 5 1 9 3.3 COc1cc2nc(N3CCN(C(=O)c4ccc(C(C)=O)o4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
CHEMBL242723 91847 0 None -18 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 479 5 1 9 3.3 COc1cc2nc(N3CCN(C(=O)c4ccc(C(C)=O)o4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
12841596 116944 19 None -3 2 Bovine 6.6 pKi = 6.6 Binding
Binding affinity against alpha-1 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]prazosin as radioligandBinding affinity against alpha-1 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]prazosin as radioligand
ChEMBL 237 1 1 5 0.8 Clc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL2448004 116944 19 None -3 2 Bovine 6.6 pKi = 6.6 Binding
Binding affinity against alpha-1 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]prazosin as radioligandBinding affinity against alpha-1 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]prazosin as radioligand
ChEMBL 237 1 1 5 0.8 Clc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL339883 116944 19 None -3 2 Bovine 6.6 pKi = 6.6 Binding
Binding affinity against alpha-1 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]prazosin as radioligandBinding affinity against alpha-1 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]prazosin as radioligand
ChEMBL 237 1 1 5 0.8 Clc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
2419 687 22 None -275 12 Human 6.6 pKi = 6.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.bmcl.2004.11.032
9 687 22 None -275 12 Human 6.6 pKi = 6.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.bmcl.2004.11.032
CHEMBL13647 687 22 None -275 12 Human 6.6 pKi = 6.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.bmcl.2004.11.032
134987 186089 43 None -309 2 Bovine 5.6 pKi = 5.6 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 181 1 1 3 0.6 Fc1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL48833 186089 43 None -309 2 Bovine 5.6 pKi = 5.6 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 181 1 1 3 0.6 Fc1cccnc1N1CCNCC1 10.1021/jm00366a007
3386873 64229 3 None - 1 Human 5.6 pKi = 5.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 338 6 2 3 3.9 N=C(CC(O)COc1ccccc1-c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2004.11.032
CHEMBL181583 64229 3 None - 1 Human 5.6 pKi = 5.6 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 338 6 2 3 3.9 N=C(CC(O)COc1ccccc1-c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2004.11.032
44271616 59349 0 None - 1 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 188 1 0 2 2.1 Cc1cccnc1C1=CCN(C)CC1 10.1021/jm00375a017
CHEMBL17223 59349 0 None - 1 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 188 1 0 2 2.1 Cc1cccnc1C1=CCN(C)CC1 10.1021/jm00375a017
15357024 60340 3 None - 1 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 174 1 0 2 1.8 CN1CC=C(c2ccccn2)CC1 10.1021/jm00375a017
CHEMBL17605 60340 3 None - 1 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 174 1 0 2 1.8 CN1CC=C(c2ccccn2)CC1 10.1021/jm00375a017
3020566 60735 14 None - 1 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 176 1 0 2 1.9 CN1CCC(c2ccccn2)CC1 10.1021/jm00375a017
CHEMBL17648 60735 14 None - 1 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 176 1 0 2 1.9 CN1CCC(c2ccccn2)CC1 10.1021/jm00375a017
2419 687 22 None -275 12 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Alpha-1A adrenergic receptor.In vitro binding affinity at human Alpha-1A adrenergic receptor.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm0307741
9 687 22 None -275 12 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Alpha-1A adrenergic receptor.In vitro binding affinity at human Alpha-1A adrenergic receptor.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm0307741
CHEMBL13647 687 22 None -275 12 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Alpha-1A adrenergic receptor.In vitro binding affinity at human Alpha-1A adrenergic receptor.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm0307741
9950711 108706 0 None 5 4 Rat 6.6 pKi = 6.6 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 359 4 2 3 3.2 O=S(=O)(CC(F)(F)F)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL321644 108706 0 None 5 4 Rat 6.6 pKi = 6.6 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 359 4 2 3 3.2 O=S(=O)(CC(F)(F)F)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
52937527 60959 0 None -1584 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 349 4 1 5 2.8 CN1CCC[C@@H]1Cn1nc(Cc2ccc(O)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767138 60959 0 None -1584 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 349 4 1 5 2.8 CN1CCC[C@@H]1Cn1nc(Cc2ccc(O)cc2)c2ccccc2c1=O 10.1021/jm1013874
2419 687 22 None -275 12 Human 6.6 pKi = 6.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm960697s
9 687 22 None -275 12 Human 6.6 pKi = 6.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm960697s
CHEMBL13647 687 22 None -275 12 Human 6.6 pKi = 6.6 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm960697s
119204 183677 37 None 2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-HEAT from human adrenergic alpha1A receptor expressed in rat-1 cellsDisplacement of [125I]-HEAT from human adrenergic alpha1A receptor expressed in rat-1 cells
ChEMBL 279 0 0 3 3.2 CN1CCc2cc3c(c4c2[C@H]1Cc1ccccc1-4)OCO3 10.1039/C7MD00629B
CHEMBL483825 183677 37 None 2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-HEAT from human adrenergic alpha1A receptor expressed in rat-1 cellsDisplacement of [125I]-HEAT from human adrenergic alpha1A receptor expressed in rat-1 cells
ChEMBL 279 0 0 3 3.2 CN1CCc2cc3c(c4c2[C@H]1Cc1ccccc1-4)OCO3 10.1039/C7MD00629B
10337773 101101 0 None -63 10 Human 4.6 pKi = 4.6 Binding
Binding affinity against Alpha-1A adrenergic receptorBinding affinity against Alpha-1A adrenergic receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
CHEMBL298612 101101 0 None -63 10 Human 4.6 pKi = 4.6 Binding
Binding affinity against Alpha-1A adrenergic receptorBinding affinity against Alpha-1A adrenergic receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
11800278 38939 0 None 15 3 Human 5.6 pKi = 5.6 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 527 10 3 8 2.4 CCOC(=O)C1CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)NC)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
CHEMBL146983 38939 0 None 15 3 Human 5.6 pKi = 5.6 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 527 10 3 8 2.4 CCOC(=O)C1CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)NC)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
1599 2299 47 None -3019 16 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
3955 2299 47 None -3019 16 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
7215 2299 47 None -3019 16 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
CHEMBL841 2299 47 None -3019 16 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
DB00836 2299 47 None -3019 16 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
1028 287 69 None -47 30 Rat 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
139148732 287 69 None -47 30 Rat 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
479 287 69 None -47 30 Rat 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
5816 287 69 None -47 30 Rat 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL679 287 69 None -47 30 Rat 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
DB00668 287 69 None -47 30 Rat 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
2435 713 98 None -436 12 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
395 713 98 None -436 12 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
520 713 98 None -436 12 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
5386 713 98 None -436 12 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
CHEMBL844 713 98 None -436 12 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
DB00484 713 98 None -436 12 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
118717461 114632 0 None -7 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 444 12 2 6 6.3 COc1ccc2c(NCCCCCCCNc3ccnc4cc(OC)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343983 114632 0 None -7 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 444 12 2 6 6.3 COc1ccc2c(NCCCCCCCNc3ccnc4cc(OC)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
118717461 114632 0 None -7 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 444 12 2 6 6.3 COc1ccc2c(NCCCCCCCNc3ccnc4cc(OC)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343983 114632 0 None -7 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 444 12 2 6 6.3 COc1ccc2c(NCCCCCCCNc3ccnc4cc(OC)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
56852956 111538 1 None -66 10 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human adrenergic-alpha1A receptor by PDSP assayDisplacement of [3H]prazosin from human adrenergic-alpha1A receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 111538 1 None -66 10 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human adrenergic-alpha1A receptor by PDSP assayDisplacement of [3H]prazosin from human adrenergic-alpha1A receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
137640201 156407 2 None -204 13 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156407 2 None -204 13 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
71521479 85818 0 None -831 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNC[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm301525w
CHEMBL2312536 85818 0 None -831 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNC[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm301525w
11164948 37495 0 None -8 3 Human 5.6 pKi = 5.6 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 382 5 2 6 3.1 COc1cc2nc3c(c(O)c2cc1OC)CCC(CNC(=O)c1ccco1)C3 10.1021/jm030952q
CHEMBL145793 37495 0 None -8 3 Human 5.6 pKi = 5.6 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 382 5 2 6 3.1 COc1cc2nc3c(c(O)c2cc1OC)CCC(CNC(=O)c1ccco1)C3 10.1021/jm030952q
76318763 84386 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 381 5 2 6 3.0 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccoc1)C3 10.1007/s00044-010-9379-1
CHEMBL2234449 84386 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 381 5 2 6 3.0 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccoc1)C3 10.1007/s00044-010-9379-1
56852956 111538 1 None -66 10 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human adrenergic-alpha1A receptor by PDSP assayDisplacement of [3H]prazosin from human adrenergic-alpha1A receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 111538 1 None -66 10 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human adrenergic-alpha1A receptor by PDSP assayDisplacement of [3H]prazosin from human adrenergic-alpha1A receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
242 467 117 None -14 52 Human 7.6 pKi = 7.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
34 467 117 None -14 52 Human 7.6 pKi = 7.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
60795 467 117 None -14 52 Human 7.6 pKi = 7.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL1112 467 117 None -14 52 Human 7.6 pKi = 7.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
DB01238 467 117 None -14 52 Human 7.6 pKi = 7.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
3584 3706 60 None -3 14 Bovine 7.6 pKi = 7.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
5401 3706 60 None -3 14 Bovine 7.6 pKi = 7.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
7302 3706 60 None -3 14 Bovine 7.6 pKi = 7.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
CHEMBL611 3706 60 None -3 14 Bovine 7.6 pKi = 7.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
DB01162 3706 60 None -3 14 Bovine 7.6 pKi = 7.6 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
180707 114623 1 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 314 5 2 4 4.3 c1ccc2c(NCCNc3ccnc4ccccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343975 114623 1 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 314 5 2 4 4.3 c1ccc2c(NCCNc3ccnc4ccccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
135398745 2858 108 None -13 66 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2858 108 None -13 66 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2858 108 None -13 66 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2858 108 None -13 66 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
16041629 94989 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3cc(F)ccc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL257097 94989 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3cc(F)ccc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
180707 114623 1 None 1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 314 5 2 4 4.3 c1ccc2c(NCCNc3ccnc4ccccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343975 114623 1 None 1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 314 5 2 4 4.3 c1ccc2c(NCCNc3ccnc4ccccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
9883506 70205 0 None -2 6 Human 7.6 pKi = 7.6 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 282 3 3 5 2.3 Cc1ccc(N(NC2=NCCN2)c2cccc(O)c2)cc1 10.1016/j.bmcl.2005.07.083
CHEMBL194849 70205 0 None -2 6 Human 7.6 pKi = 7.6 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 282 3 3 5 2.3 Cc1ccc(N(NC2=NCCN2)c2cccc(O)c2)cc1 10.1016/j.bmcl.2005.07.083
46934641 16484 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 479 7 0 6 3.5 COc1ccccc1N1CCN(C[C@@H]2CO[C@@](CN3CCCCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242633 16484 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 479 7 0 6 3.5 COc1ccccc1N1CCN(C[C@@H]2CO[C@@](CN3CCCCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
56946474 71157 0 None -32 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 403 9 1 4 4.8 COc1ccccc1OCCNCC1CCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm200421e
CHEMBL1946779 71157 0 None -32 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 403 9 1 4 4.8 COc1ccccc1OCCNCC1CCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm200421e
CHEMBL1962769 71157 0 None -32 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 403 9 1 4 4.8 COc1ccccc1OCCNCC1CCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm200421e
44207909 16505 1 None 2 9 Human 6.6 pKi = 6.6 Binding
Binding affinity to human adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to human adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1242923 16505 1 None 2 9 Human 6.6 pKi = 6.6 Binding
Binding affinity to human adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to human adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
44538690 109350 0 None -295 7 Human 6.6 pKi = 6.6 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 380 5 0 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCO3)c1ccc(F)cc1 10.1021/jm401958n
CHEMBL3233432 109350 0 None -295 7 Human 6.6 pKi = 6.6 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 380 5 0 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCO3)c1ccc(F)cc1 10.1021/jm401958n
10219 188200 30 None -467 5 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 nan
CHEMBL493439 188200 30 None -467 5 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 nan
CHEMBL50588 188200 30 None -467 5 Rat 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 nan
12840734 100449 3 None -630 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 355 4 0 4 2.5 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2)CC1 10.1007/s00044-010-9379-1
CHEMBL293968 100449 3 None -630 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 355 4 0 4 2.5 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2)CC1 10.1007/s00044-010-9379-1
134133829 143281 0 None -120 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 337 7 1 5 3.5 COc1ccccc1OCCNCC1CSC2(CCCCC2)O1 10.1016/j.ejmech.2016.09.050
CHEMBL3901382 143281 0 None -120 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 337 7 1 5 3.5 COc1ccccc1OCCNCC1CSC2(CCCCC2)O1 10.1016/j.ejmech.2016.09.050
10221830 9316 0 None 1 3 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 387 5 2 3 4.7 CCS(=O)(=O)Nc1cc(C2CCCCC2)cc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL111685 9316 0 None 1 3 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 387 5 2 3 4.7 CCS(=O)(=O)Nc1cc(C2CCCCC2)cc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
11811395 202985 0 None -2 4 Human 5.6 pKi = 5.6 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 281 5 2 5 1.3 CC(C)S(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74071 202985 0 None -2 4 Human 5.6 pKi = 5.6 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 281 5 2 5 1.3 CC(C)S(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
12840734 100449 3 None -630 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 355 4 0 4 2.5 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2)CC1 10.1007/s00044-010-9379-1
CHEMBL293968 100449 3 None -630 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 355 4 0 4 2.5 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2)CC1 10.1007/s00044-010-9379-1
10721586 119203 0 None 141 3 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 559 10 3 7 3.4 CC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
CHEMBL347522 119203 0 None 141 3 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 559 10 3 7 3.4 CC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
11198145 9707 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL113830 9707 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
44289047 99905 0 None 25 3 Human 7.6 pKi = 7.6 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 441 8 1 3 5.2 Cc1ccc(C(C(=O)NCCCN2CCC(c3ccccn3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
CHEMBL289916 99905 0 None 25 3 Human 7.6 pKi = 7.6 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 441 8 1 3 5.2 Cc1ccc(C(C(=O)NCCCN2CCC(c3ccccn3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
9822705 100208 0 None -19 4 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 407 4 0 3 4.4 O=C1CC2(C=CN1CCN1CCN(c3cc(Cl)ccc3Cl)CC1)CCCC2 10.1021/jm030944+
CHEMBL292366 100208 0 None -19 4 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 407 4 0 3 4.4 O=C1CC2(C=CN1CCN1CCN(c3cc(Cl)ccc3Cl)CC1)CCCC2 10.1021/jm030944+
25131876 85751 0 None -41 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.02.056
CHEMBL2312227 85751 0 None -41 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.02.056
76308474 105740 0 None -31 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 467 5 1 9 3.1 COc1ccc(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)[C@H]3CCCC[C@@H]32)o1 10.1007/s00044-004-0024-8
CHEMBL2261607 105740 0 None -31 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 467 5 1 9 3.1 COc1ccc(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)[C@H]3CCCC[C@@H]32)o1 10.1007/s00044-004-0024-8
CHEMBL3138856 105740 0 None -31 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 467 5 1 9 3.1 COc1ccc(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)[C@H]3CCCC[C@@H]32)o1 10.1007/s00044-004-0024-8
44428846 91743 0 None -31 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 467 5 1 9 3.1 COc1ccc(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)[C@@H]3CCCC[C@@H]32)o1 10.1016/j.bmc.2007.01.028
CHEMBL242508 91743 0 None -31 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 467 5 1 9 3.1 COc1ccc(C(=O)N2CCN(c3nc(N)c4cc(OC)c(OC)cc4n3)[C@@H]3CCCC[C@@H]32)o1 10.1016/j.bmc.2007.01.028
25181488 186789 0 None -33 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNC[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm800461k
CHEMBL493486 186789 0 None -33 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNC[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm800461k
25131876 85751 0 None -41 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm301525w
CHEMBL2312227 85751 0 None -41 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm301525w
10427137 35806 4 None -512 3 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]prazosin from rat whole brain alpha1 adrenergic receptorDisplacement of [3H]prazosin from rat whole brain alpha1 adrenergic receptor
ChEMBL 336 2 0 2 5.3 Cc1ccc2c(c1)c(-c1ccc(F)cc1)c(C)n2C1CCN(C)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL144362 35806 4 None -512 3 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]prazosin from rat whole brain alpha1 adrenergic receptorDisplacement of [3H]prazosin from rat whole brain alpha1 adrenergic receptor
ChEMBL 336 2 0 2 5.3 Cc1ccc2c(c1)c(-c1ccc(F)cc1)c(C)n2C1CCN(C)CC1 10.1021/acs.jmedchem.2c00633
11711943 15909 0 None -28 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 444 8 1 5 5.4 FC(F)(F)c1cccc(N2CCN(CCCCNc3ncc(-c4ccccc4)o3)CC2)c1 10.1016/j.bmcl.2010.07.096
CHEMBL1223858 15909 0 None -28 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 444 8 1 5 5.4 FC(F)(F)c1cccc(N2CCN(CCCCNc3ncc(-c4ccccc4)o3)CC2)c1 10.1016/j.bmcl.2010.07.096
71062646 148999 0 None -4466 13 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
CHEMBL3946661 148999 0 None -4466 13 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
9796525 9302 0 None 5 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 305 3 1 4 2.3 Cn1cnc(C2CCCc3c(NS(C)(=O)=O)cccc32)c1 10.1007/s00044-004-0020-z
CHEMBL111584 9302 0 None 5 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 305 3 1 4 2.3 Cn1cnc(C2CCCc3c(NS(C)(=O)=O)cccc32)c1 10.1007/s00044-004-0020-z
9796525 9302 0 None 5 3 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 305 3 1 4 2.3 Cn1cnc(C2CCCc3c(NS(C)(=O)=O)cccc32)c1 10.1021/jm030551a
CHEMBL111584 9302 0 None 5 3 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 305 3 1 4 2.3 Cn1cnc(C2CCCc3c(NS(C)(=O)=O)cccc32)c1 10.1021/jm030551a
10763305 106466 0 None -11 2 Rat 6.6 pKi = 6.6 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 396 5 0 4 3.3 FC(F)(F)c1cccc(N2CCN(CCCN3CC4CCCCN4C3)CC2)c1 10.1021/jm970216k
CHEMBL314997 106466 0 None -11 2 Rat 6.6 pKi = 6.6 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 396 5 0 4 3.3 FC(F)(F)c1cccc(N2CCN(CCCN3CC4CCCCN4C3)CC2)c1 10.1021/jm970216k
18738380 11821 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 417 9 1 6 1.9 CC(C)Oc1ccccc1N1CCN(CC(O)CC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL11828 11821 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 417 9 1 6 1.9 CC(C)Oc1ccccc1N1CCN(CC(O)CC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
11857638 141611 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 516 9 1 6 5.0 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL388361 141611 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 516 9 1 6 5.0 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
11857638 141611 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 516 9 1 6 5.0 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL388361 141611 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 516 9 1 6 5.0 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
1353 1872 85 None -10 86 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1872 85 None -10 86 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1872 85 None -10 86 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1872 85 None -10 86 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1872 85 None -10 86 Rat 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
44460477 203686 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 432 7 0 6 3.9 O=C1CCCN1Cc1cc(CN2CCN(c3ccccc3Oc3ccccc3)CC2)on1 10.1016/s0960-894x(02)00436-5
CHEMBL80109 203686 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 432 7 0 6 3.9 O=C1CCCN1Cc1cc(CN2CCN(c3ccccc3Oc3ccccc3)CC2)on1 10.1016/s0960-894x(02)00436-5
145987771 166525 0 None -8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting methodDisplacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting method
ChEMBL 431 6 1 2 5.9 Fc1ccc(N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccccc2)c1 10.1016/j.ejmech.2017.12.063
CHEMBL4289783 166525 0 None -8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting methodDisplacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting method
ChEMBL 431 6 1 2 5.9 Fc1ccc(N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccccc2)c1 10.1016/j.ejmech.2017.12.063
44288740 100872 0 None 29 3 Human 7.6 pKi = 7.6 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 437 8 1 3 4.9 N#CC1(c2ccccc2)CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL296965 100872 0 None 29 3 Human 7.6 pKi = 7.6 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 437 8 1 3 4.9 N#CC1(c2ccccc2)CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(00)00307-3
53328505 63049 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 455 7 0 5 3.8 COc1ccccc1N1CCN(CCCN2C(=O)CC(c3ccc(Cl)cc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796039 63049 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 455 7 0 5 3.8 COc1ccccc1N1CCN(CCCN2C(=O)CC(c3ccc(Cl)cc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
76322412 84384 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 354 5 0 5 2.9 COc1ccccc1N1CCN(CC2CO[C@H](c3ccccc3)O2)CC1 10.1007/s00044-010-9379-1
CHEMBL2234447 84384 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 354 5 0 5 2.9 COc1ccccc1N1CCN(CC2CO[C@H](c3ccccc3)O2)CC1 10.1007/s00044-010-9379-1
14004037 53474 2 None -8 2 Bovine 5.6 pKi = 5.6 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 209 0 1 4 1.8 Nc1nc2c(s1)CCN1CCCCC21 10.1021/jm00398a025
CHEMBL160388 53474 2 None -8 2 Bovine 5.6 pKi = 5.6 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 209 0 1 4 1.8 Nc1nc2c(s1)CCN1CCCCC21 10.1021/jm00398a025
1960 2805 64 None -57 26 Rat 6.6 pKi = 6.6 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
439260 2805 64 None -57 26 Rat 6.6 pKi = 6.6 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
505 2805 64 None -57 26 Rat 6.6 pKi = 6.6 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
CHEMBL1437 2805 64 None -57 26 Rat 6.6 pKi = 6.6 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
DB00368 2805 64 None -57 26 Rat 6.6 pKi = 6.6 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
2435 713 98 None -21 12 Human 5.6 pKi = 5.6 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
395 713 98 None -21 12 Human 5.6 pKi = 5.6 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
520 713 98 None -21 12 Human 5.6 pKi = 5.6 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
5386 713 98 None -21 12 Human 5.6 pKi = 5.6 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
CHEMBL844 713 98 None -21 12 Human 5.6 pKi = 5.6 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
DB00484 713 98 None -21 12 Human 5.6 pKi = 5.6 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
14004037 53474 2 None -8 2 Bovine 5.6 pKi = 5.6 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 209 0 1 4 1.8 Nc1nc2c(s1)CCN1CCCCC21 10.1021/jm00398a025
CHEMBL160388 53474 2 None -8 2 Bovine 5.6 pKi = 5.6 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 209 0 1 4 1.8 Nc1nc2c(s1)CCN1CCCCC21 10.1021/jm00398a025
127027076 137149 0 None -257 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 455 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
CHEMBL3758711 137149 0 None -257 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 455 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
2777786 174395 77 None -29 2 Bovine 5.5 pKi = 5.5 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 231 1 1 3 1.5 FC(F)(F)c1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL45663 174395 77 None -29 2 Bovine 5.5 pKi = 5.5 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 231 1 1 3 1.5 FC(F)(F)c1cccnc1N1CCNCC1 10.1021/jm00366a007
73213196 103968 1 None -2 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to adrenergic alpha 1A receptor (unknown origin)Binding affinity to adrenergic alpha 1A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2014.05.016
CHEMBL3104093 103968 1 None -2 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to adrenergic alpha 1A receptor (unknown origin)Binding affinity to adrenergic alpha 1A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2014.05.016
73213196 103968 1 None -2 13 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 103968 1 None -2 13 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
11282574 37484 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 459 5 2 5 4.4 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccccc1C(F)(F)F)C3 10.1021/jm030952q
CHEMBL145785 37484 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 459 5 2 5 4.4 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccccc1C(F)(F)F)C3 10.1021/jm030952q
76319344 84899 0 None 29 3 Rat 6.5 pKi = 6.5 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 289 2 3 5 2.0 COC(=O)Nc1c(O)ccc2c1CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
CHEMBL2261351 84899 0 None 29 3 Rat 6.5 pKi = 6.5 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 289 2 3 5 2.0 COC(=O)Nc1c(O)ccc2c1CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
73213196 103968 1 None -2 13 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 103968 1 None -2 13 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
155552821 176099 0 None -12 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 8 1 4 4.2 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)OC2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4544457 176099 0 None -12 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 8 1 4 4.2 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)OC2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4598345 176099 0 None -12 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 8 1 4 4.2 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)OC2)cc1 10.1016/j.ejmech.2019.05.024
92766 106047 30 None 1 6 Human 7.5 pKi = 7.5 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@H]12 10.1016/j.bmcl.2004.11.032
CHEMBL31410 106047 30 None 1 6 Human 7.5 pKi = 7.5 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@H]12 10.1016/j.bmcl.2004.11.032
12909385 60093 1 None 7 2 Bovine 7.5 pKi = 7.5 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 276 0 0 2 4.0 CN1CCC(=C2c3ccccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL175154 60093 1 None 7 2 Bovine 7.5 pKi = 7.5 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 276 0 0 2 4.0 CN1CCC(=C2c3ccccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
11303180 196539 0 None -9 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 369 5 0 4 3.1 COc1ccccc1N1CCN(CCN2C=CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
CHEMBL57540 196539 0 None -9 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 369 5 0 4 3.1 COc1ccccc1N1CCN(CCN2C=CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
122179431 120916 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 585 9 1 13 3.1 CCN(CC)c1ccc2cc(-n3cc(CN4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)nn3)c(=O)oc2c1 10.1021/ml5004298
CHEMBL3582272 120916 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 585 9 1 13 3.1 CCN(CC)c1ccc2cc(-n3cc(CN4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)nn3)c(=O)oc2c1 10.1021/ml5004298
11384664 82685 0 None -35 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
CHEMBL218203 82685 0 None -35 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
127026123 137173 0 None -41 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 401 7 1 3 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2015.12.068
CHEMBL3758881 137173 0 None -41 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 401 7 1 3 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2015.12.068
2419 687 22 None -275 12 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm0491391
9 687 22 None -275 12 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm0491391
CHEMBL13647 687 22 None -275 12 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm0491391
9845181 206410 1 None -1445 15 Human 6.5 pKi = 6.5 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1016/j.bmcl.2004.11.032
CHEMBL98241 206410 1 None -1445 15 Human 6.5 pKi = 6.5 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1016/j.bmcl.2004.11.032
10643994 76888 0 None -2 3 Rat 5.5 pKi = 5.5 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 388 4 3 8 0.9 COc1cc2nc(N3CCN[C@@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
CHEMBL2079655 76888 0 None -2 3 Rat 5.5 pKi = 5.5 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 388 4 3 8 0.9 COc1cc2nc(N3CCN[C@@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
146025727 171109 0 None -107 27 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171109 0 None -107 27 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
2419 687 22 None -275 12 Human 6.5 pKi = 6.5 Binding
Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor (n >= 2)Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor (n >= 2)
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm980053f
9 687 22 None -275 12 Human 6.5 pKi = 6.5 Binding
Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor (n >= 2)Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor (n >= 2)
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm980053f
CHEMBL13647 687 22 None -275 12 Human 6.5 pKi = 6.5 Binding
Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor (n >= 2)Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor (n >= 2)
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm980053f
9845181 206410 1 None -1445 15 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human Alpha-1A adrenergic receptor.In vitro binding affinity at human Alpha-1A adrenergic receptor.
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm0307741
CHEMBL98241 206410 1 None -1445 15 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human Alpha-1A adrenergic receptor.In vitro binding affinity at human Alpha-1A adrenergic receptor.
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm0307741
11191047 200122 0 None -8 3 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 490 7 0 6 3.2 COc1ccccc1N1CCN(CCN2C(=O)CC3(CCN(Cc4ccccc4)CC3)CC2=O)CC1 10.1021/jm030944+
CHEMBL60699 200122 0 None -8 3 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 490 7 0 6 3.2 COc1ccccc1N1CCN(CCN2C(=O)CC3(CCN(Cc4ccccc4)CC3)CC2=O)CC1 10.1021/jm030944+
11486511 101100 0 None -870 5 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 403 4 0 4 3.6 O=C1CC2(CCCC2)CC(=O)N1CCN1CCCN(c2ccccc2Cl)CC1 10.1021/jm030944+
CHEMBL298595 101100 0 None -870 5 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 403 4 0 4 3.6 O=C1CC2(CCCC2)CC(=O)N1CCN1CCCN(c2ccccc2Cl)CC1 10.1021/jm030944+
11346205 9171 0 None -8 2 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 268 4 3 5 0.8 CCS(=O)(=O)Nc1cccc(NC2=NCCN2)c1 10.1021/jm030551a
CHEMBL110852 9171 0 None -8 2 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 268 4 3 5 0.8 CCS(=O)(=O)Nc1cccc(NC2=NCCN2)c1 10.1021/jm030551a
44460522 203666 0 None 3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 460 7 0 7 3.6 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3C(=O)c4ccccc4C3=O)co2)CC1 10.1016/s0960-894x(02)00436-5
CHEMBL79990 203666 0 None 3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 460 7 0 7 3.6 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3C(=O)c4ccccc4C3=O)co2)CC1 10.1016/s0960-894x(02)00436-5
136680385 205906 0 None 85 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 694 16 4 8 4.9 CCNC(=O)C1=C(COCCN)NC(CC)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
44328824 205906 0 None 85 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 694 16 4 8 4.9 CCNC(=O)C1=C(COCCN)NC(CC)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
CHEMBL95253 205906 0 None 85 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 694 16 4 8 4.9 CCNC(=O)C1=C(COCCN)NC(CC)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
44213782 10425 0 None 309 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 504 8 0 6 3.9 CCOC(=O)C1CN(CCCCN2C(=O)c3cc(Cl)ccc3S2(=O)=O)CCC1c1ccccc1 10.1016/s0960-894x(98)00451-x
CHEMBL1169493 10425 0 None 309 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 504 8 0 6 3.9 CCOC(=O)C1CN(CCCCN2C(=O)c3cc(Cl)ccc3S2(=O)=O)CCC1c1ccccc1 10.1016/s0960-894x(98)00451-x
44431611 87139 0 None 6 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 509 7 1 5 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL233582 87139 0 None 6 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 509 7 1 5 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
11857639 143340 0 None 2 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 492 7 1 4 5.2 CC(C)Oc1ccccc1C1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.098
CHEMBL390184 143340 0 None 2 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 492 7 1 4 5.2 CC(C)Oc1ccccc1C1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.098
9848303 111079 0 None 1 11 Bovine 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 487 6 1 6 3.8 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1016/j.bmc.2012.10.049
CHEMBL328187 111079 0 None 1 11 Bovine 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 487 6 1 6 3.8 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1016/j.bmc.2012.10.049
9848303 111079 0 None 1 11 Bovine 8.5 pKi = 8.5 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 487 6 1 6 3.8 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm100652h
CHEMBL328187 111079 0 None 1 11 Bovine 8.5 pKi = 8.5 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
ChEMBL 487 6 1 6 3.8 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm100652h
10971791 206567 0 None -7 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 417 5 1 7 3.4 COc1ccccc1N1CCN(CCn2c(C)nc3c4ccccc4nc-3c2O)CC1 10.1016/j.bmcl.2006.09.034
CHEMBL99142 206567 0 None -7 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 417 5 1 7 3.4 COc1ccccc1N1CCN(CCn2c(C)nc3c4ccccc4nc-3c2O)CC1 10.1016/j.bmcl.2006.09.034
118716718 114501 0 None -3 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 532 7 0 9 2.3 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4cccc([N+](=O)[O-])c4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342871 114501 0 None -3 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 532 7 0 9 2.3 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4cccc([N+](=O)[O-])c4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
44447002 94274 0 None -301 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 434 6 1 5 4.2 CCC(=O)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
CHEMBL253022 94274 0 None -301 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 434 6 1 5 4.2 CCC(=O)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
9960311 202157 0 None 25 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 598 9 2 7 4.5 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(C(C)(C)C)cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL68699 202157 0 None 25 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 598 9 2 7 4.5 CC(C)Oc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(C(C)(C)C)cc2)C3=O)CC1 10.1021/jm9905918
19085839 204058 0 None 97 3 Human 8.5 pKi = 8.5 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 469 6 0 7 3.2 Cc1ccc2c(c1)oc(=O)n2C1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL83041 204058 0 None 97 3 Human 8.5 pKi = 8.5 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 469 6 0 7 3.2 Cc1ccc2c(c1)oc(=O)n2C1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/s0960-894x(98)00446-6
4188516 99900 8 None 1 2 Rat 8.5 pKi = 8.5 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 372 6 0 5 1.6 COc1ccccc1N1CCN(CCCN2C(=O)C3CCCN3C2=O)CC1 10.1021/jm970216k
CHEMBL289873 99900 8 None 1 2 Rat 8.5 pKi = 8.5 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 372 6 0 5 1.6 COc1ccccc1N1CCN(CCCN2C(=O)C3CCCN3C2=O)CC1 10.1021/jm970216k
9891166 33377 0 None -7 5 Human 8.5 pKi = 8.5 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 476 6 0 8 3.3 COc1ccccc1N1CCN(CCn2c(=O)c3c(-c4ccccc4)csc3n(C)c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL14213 33377 0 None -7 5 Human 8.5 pKi = 8.5 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 476 6 0 8 3.3 COc1ccccc1N1CCN(CCn2c(=O)c3c(-c4ccccc4)csc3n(C)c2=O)CC1 10.1016/s0960-894x(01)00159-7
16041628 154799 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccc(F)cc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL403280 154799 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccc(F)cc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
10841387 99144 0 None 91 6 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
CHEMBL284103 99144 0 None 91 6 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
10624665 99855 0 None 1 3 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 482 4 1 7 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5c(Cl)ccnc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL289437 99855 0 None 1 3 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 482 4 1 7 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5c(Cl)ccnc54)c3=O)C[C@@H]21 10.1021/jm990567u
10416624 109149 0 None 263 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 634 14 4 10 2.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(COCCN)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(99)00484-9
136806219 109149 0 None 263 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 634 14 4 10 2.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(COCCN)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(99)00484-9
CHEMBL322405 109149 0 None 263 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 634 14 4 10 2.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(COCCN)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(99)00484-9
2585 788 100 None -5 22 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 788 100 None -5 22 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 788 100 None -5 22 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 788 100 None -5 22 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 788 100 None -5 22 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
3157 1437 69 None -2 12 Human 8.5 pKi = 8.5 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm960697s
7170 1437 69 None -2 12 Human 8.5 pKi = 8.5 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm960697s
954 1437 69 None -2 12 Human 8.5 pKi = 8.5 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm960697s
CHEMBL707 1437 69 None -2 12 Human 8.5 pKi = 8.5 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm960697s
DB00590 1437 69 None -2 12 Human 8.5 pKi = 8.5 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm960697s
10841387 99144 0 None 91 6 Human 8.5 pKi = 8.5 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm960697s
CHEMBL284103 99144 0 None 91 6 Human 8.5 pKi = 8.5 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm960697s
52947579 16854 0 None -17 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 439 13 1 6 5.0 COc1cccc(OC)c1SCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1254582 16854 0 None -17 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 439 13 1 6 5.0 COc1cccc(OC)c1SCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
52945803 16870 0 None -8 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 451 15 1 6 5.1 CCOc1cccc(OCC)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1254742 16870 0 None -8 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 451 15 1 6 5.1 CCOc1cccc(OCC)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
52941624 16896 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 393 12 1 5 4.3 COc1ccccc1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1254915 16896 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 393 12 1 5 4.3 COc1ccccc1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
10693026 105460 0 None 5 2 Bovine 8.5 pKi = 8.5 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 412 9 1 6 2.8 CCOc1ccccc1OCCNC1CCN(c2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL312935 105460 0 None 5 2 Bovine 8.5 pKi = 8.5 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 412 9 1 6 2.8 CCOc1ccccc1OCCNC1CCN(c2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
25032525 94133 0 None -9 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 420 5 1 5 3.8 CC(=O)NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21 10.1016/j.bmcl.2007.11.106
CHEMBL252030 94133 0 None -9 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 420 5 1 5 3.8 CC(=O)NC1CCc2cc(CCN3CCN(c4nsc5ccccc45)CC3)ccc21 10.1016/j.bmcl.2007.11.106
10769037 36962 0 None 70 3 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 551 7 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL145332 36962 0 None 70 3 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 551 7 2 6 4.1 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
1043 1545 13 None -35 29 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1545 13 None -35 29 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1545 13 None -35 29 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1545 13 None -35 29 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1545 13 None -35 29 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
15853467 206383 0 None 29 6 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Alpha-1A adrenergic receptorBinding affinity against human Alpha-1A adrenergic receptor
ChEMBL 692 16 3 8 5.6 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN=[N+]=[N-])N1 10.1016/s0960-894x(99)00484-9
CHEMBL98063 206383 0 None 29 6 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Alpha-1A adrenergic receptorBinding affinity against human Alpha-1A adrenergic receptor
ChEMBL 692 16 3 8 5.6 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN=[N+]=[N-])N1 10.1016/s0960-894x(99)00484-9
11857864 85243 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 534 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4cc(F)ccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL228659 85243 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 534 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4cc(F)ccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
10553701 99819 0 None 1 3 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 472 4 1 7 3.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccc(C#N)c54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL289166 99819 0 None 1 3 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 472 4 1 7 3.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccc(C#N)c54)c3=O)C[C@@H]21 10.1021/jm990567u
9960497 116561 0 None 25 6 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(C)=C(C(=O)OCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
CHEMBL3392246 116561 0 None 25 6 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(C)=C(C(=O)OCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
44447015 153695 0 None -3 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 483 6 1 6 4.5 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1cccnc1 10.1016/j.bmcl.2007.11.106
CHEMBL398619 153695 0 None -3 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 483 6 1 6 4.5 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1cccnc1 10.1016/j.bmcl.2007.11.106
10071710 83703 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 436 5 1 7 2.7 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccccc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL220781 83703 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 436 5 1 7 2.7 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccccc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
10071710 83703 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 436 5 1 7 2.7 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
CHEMBL220781 83703 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 436 5 1 7 2.7 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
45268939 194975 0 None -4 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to alpha1A adrenergic receptor (unknown origin)Binding affinity to alpha1A adrenergic receptor (unknown origin)
ChEMBL 505 4 1 9 3.0 COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL564481 194975 0 None -4 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to alpha1A adrenergic receptor (unknown origin)Binding affinity to alpha1A adrenergic receptor (unknown origin)
ChEMBL 505 4 1 9 3.0 COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
90645603 111931 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 567 8 1 8 4.9 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccc(NC(=O)Cc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298021 111931 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 567 8 1 8 4.9 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccc(NC(=O)Cc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
24894147 194198 0 None -6 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 505 4 1 9 3.0 COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1021/jm8016046
CHEMBL558890 194198 0 None -6 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 505 4 1 9 3.0 COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1021/jm8016046
11465618 101913 18 None -12 19 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 101913 18 None -12 19 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 101913 18 None -12 19 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]prazosin from recombinant human alpha1A receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
44289034 165389 0 None 199 3 Human 8.5 pKi = 8.5 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 435 8 1 3 4.9 Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2cccc(F)c2)C(C)C)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL42514 165389 0 None 199 3 Human 8.5 pKi = 8.5 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 435 8 1 3 4.9 Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2cccc(F)c2)C(C)C)CC1 10.1016/s0960-894x(00)00307-3
2726 904 64 None -2 73 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 904 64 None -2 73 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 904 64 None -2 73 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 904 64 None -2 73 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 904 64 None -2 73 Rat 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
44420431 84299 0 None -4 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 468 5 0 7 4.4 COc1ccc(Cl)cc1N1CCN(CCn2c(C)nc3c(sc4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
CHEMBL222896 84299 0 None -4 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 468 5 0 7 4.4 COc1ccc(Cl)cc1N1CCN(CCn2c(C)nc3c(sc4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
76330229 105741 0 None -11 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 515 4 1 8 3.9 COc1cc2nc(N3CCN(C(=O)c4ccc(Br)o4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
CHEMBL2261605 105741 0 None -11 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 515 4 1 8 3.9 COc1cc2nc(N3CCN(C(=O)c4ccc(Br)o4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
CHEMBL3138857 105741 0 None -11 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptorDisplacement of [3H]prazosin from Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 515 4 1 8 3.9 COc1cc2nc(N3CCN(C(=O)c4ccc(Br)o4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1007/s00044-004-0024-8
44428845 141818 0 None -11 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 515 4 1 8 3.9 COc1cc2nc(N3CCN(C(=O)c4ccc(Br)o4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
CHEMBL388884 141818 0 None -11 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 515 4 1 8 3.9 COc1cc2nc(N3CCN(C(=O)c4ccc(Br)o4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
11638677 84152 0 None -138 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 340 5 0 5 2.8 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2016.06.052
CHEMBL2153423 84152 0 None -138 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 340 5 0 5 2.8 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2016.06.052
CHEMBL2220978 84152 0 None -138 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 340 5 0 5 2.8 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2016.06.052
491 191 4 None -44 12 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
9891167 191 4 None -44 12 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
CHEMBL13856 191 4 None -44 12 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
10816832 120977 0 None 234 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 1 7 4.5 COC(=O)C1=C(C)N=C(C)N(CCC[C@H](C)CN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL358313 120977 0 None 234 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 567 10 1 7 4.5 COC(=O)C1=C(C)N=C(C)N(CCC[C@H](C)CN2CCN(c3ccccc3C(N)=O)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
44431551 86768 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cccc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL232779 86768 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cccc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
44431620 87356 0 None 4 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 570 7 1 6 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3cnc(Cl)c(Br)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL233790 87356 0 None 4 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 570 7 1 6 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3cnc(Cl)c(Br)c3)CC2)CC1 10.1016/j.bmcl.2007.04.008
56837635 68951 0 None -11 5 Pig 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928132 68951 0 None -11 5 Pig 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
57398875 68957 0 None 1 5 Pig 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928138 68957 0 None 1 5 Pig 8.5 pKi = 8.5 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
11154198 199919 0 None -6 5 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 413 6 0 5 3.3 CC(C)Oc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
CHEMBL60583 199919 0 None -6 5 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 413 6 0 5 3.3 CC(C)Oc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
11801562 84846 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 590 10 2 9 3.7 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL2260362 84846 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 590 10 2 9 3.7 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
90645604 111932 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 652 12 2 9 5.2 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccc(NC(=O)CCCC(=O)NCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298022 111932 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 652 12 2 9 5.2 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccc(NC(=O)CCCC(=O)NCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
10582623 101285 0 None -1 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 392 4 1 6 1.8 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cccnc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL299907 101285 0 None -1 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 392 4 1 6 1.8 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cccnc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL41844 162669 0 None 194 4 Human 8.5 pKi = 8.5 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 590 10 2 9 4.6 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)N=C(C)/C(=C(/O)OC)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
10745305 36890 0 None 120 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 553 9 0 7 5.2 COC(=O)C1=C(C)N=C(C)N(CCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL145278 36890 0 None 120 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 553 9 0 7 5.2 COC(=O)C1=C(C)N=C(C)N(CCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
102 4051 44 None -85 50 Bovine 8.4 pKi = 8.4 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00018a001
3659 4051 44 None -85 50 Bovine 8.4 pKi = 8.4 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00018a001
8969 4051 44 None -85 50 Bovine 8.4 pKi = 8.4 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00018a001
CHEMBL15245 4051 44 None -85 50 Bovine 8.4 pKi = 8.4 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00018a001
DB01392 4051 44 None -85 50 Bovine 8.4 pKi = 8.4 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00018a001
16041092 94923 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccc(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL256804 94923 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccc(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
136048765 62991 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranesInhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranes
ChEMBL 502 9 3 8 4.9 COc1ccccc1N1CCN(CCCNc2cc(O)nc(Nc3c(Cl)cccc3Cl)n2)CC1 10.1021/jm0491804
CHEMBL179401 62991 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranesInhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranes
ChEMBL 502 9 3 8 4.9 COc1ccccc1N1CCN(CCCNc2cc(O)nc(Nc3c(Cl)cccc3Cl)n2)CC1 10.1021/jm0491804
CHEMBL41844 162669 0 None 194 4 Human 8.4 pKi = 8.4 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 590 10 2 9 4.6 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)N=C(C)/C(=C(/O)OC)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(00)00307-3
44447007 154247 0 None -4 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 448 6 1 5 4.4 CC(C)C(=O)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
CHEMBL400236 154247 0 None -4 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 448 6 1 5 4.4 CC(C)C(=O)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
10817661 84848 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 620 12 3 10 3.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)OCCO)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
CHEMBL2260364 84848 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 620 12 3 10 3.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)OCCO)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
CHEMBL347501 119198 0 None 436 3 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 620 12 3 10 3.9 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)N=C(C)/C(=C(/O)OCCO)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
4418 33985 80 None -1 7 Human 8.4 pKi = 8.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2004.11.032
CHEMBL142635 33985 80 None -1 7 Human 8.4 pKi = 8.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2004.11.032
44316098 168589 0 None 14 3 Human 8.4 pKi = 8.4 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 425 7 0 6 3.0 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)n(C)n2)CC1 10.1016/s0960-894x(00)00472-8
CHEMBL440499 168589 0 None 14 3 Human 8.4 pKi = 8.4 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 425 7 0 6 3.0 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)n(C)n2)CC1 10.1016/s0960-894x(00)00472-8
1443 1989 30 None 1 11 Human 8.4 pKi = 8.4 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
33625 1989 30 None 1 11 Human 8.4 pKi = 8.4 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
501 1989 30 None 1 11 Human 8.4 pKi = 8.4 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
CHEMBL279516 1989 30 None 1 11 Human 8.4 pKi = 8.4 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
DB08950 1989 30 None 1 11 Human 8.4 pKi = 8.4 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
10555618 84847 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 604 11 2 9 4.1 CCOC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL2260363 84847 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 604 11 2 9 4.1 CCOC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
4418 33985 80 None -1 7 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-HEAT from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes incubated for 60 minsDisplacement of [125I-HEAT from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes incubated for 60 mins
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2018.01.068
CHEMBL142635 33985 80 None -1 7 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-HEAT from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes incubated for 60 minsDisplacement of [125I-HEAT from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes incubated for 60 mins
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2018.01.068
CHEMBL346649 119111 0 None 104 3 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 604 11 2 9 4.9 CCO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
2284 3121 27 None -1 29 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3121 27 None -1 29 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3121 27 None -1 29 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3121 27 None -1 29 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3121 27 None -1 29 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
10526419 197360 0 None 7 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 425 7 2 6 2.7 COc1cc(N)c(C(=O)NCCN2C[C@@H]3CCc4c(OC)cccc4[C@@H]3C2)cc1OC 10.1021/jm000541z
CHEMBL58612 197360 0 None 7 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 425 7 2 6 2.7 COc1cc(N)c(C(=O)NCCN2C[C@@H]3CCc4c(OC)cccc4[C@@H]3C2)cc1OC 10.1021/jm000541z
44328654 106688 0 None 47 6 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 663 14 3 6 6.7 CCCC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCC)=C(CC)N1 10.1016/s0960-894x(99)00484-9
CHEMBL316495 106688 0 None 47 6 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 663 14 3 6 6.7 CCCC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCC)=C(CC)N1 10.1016/s0960-894x(99)00484-9
136806212 205988 0 None 47 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 636 13 4 7 4.6 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CCCN)N1 10.1016/s0960-894x(99)00484-9
44328639 205988 0 None 47 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 636 13 4 7 4.6 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CCCN)N1 10.1016/s0960-894x(99)00484-9
CHEMBL95736 205988 0 None 47 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 636 13 4 7 4.6 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CCCN)N1 10.1016/s0960-894x(99)00484-9
17753379 87621 0 None 2 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 521 8 1 6 4.5 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234607 87621 0 None 2 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 521 8 1 6 4.5 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
11857711 85185 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 506 7 1 4 5.5 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1)c1cc(Cl)ccc1F 10.1016/j.bmcl.2007.04.098
CHEMBL228332 85185 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 506 7 1 4 5.5 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1)c1cc(Cl)ccc1F 10.1016/j.bmcl.2007.04.098
12134986 163831 0 None 70 3 Human 8.4 pKi = 8.4 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 412 7 0 6 3.3 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)on2)CC1 10.1016/s0960-894x(00)00472-8
CHEMBL421324 163831 0 None 70 3 Human 8.4 pKi = 8.4 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 412 7 0 6 3.3 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)on2)CC1 10.1016/s0960-894x(00)00472-8
71817549 102094 0 None -4 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
CHEMBL3040803 102094 0 None -4 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
CHEMBL3216590 102094 0 None -4 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
2894 206321 4 None -8 6 Rat 8.4 pKi = 8.4 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)C4CCCCC43)nc(N)c2cc1OC 10.1021/jm960510x
CHEMBL97698 206321 4 None -8 6 Rat 8.4 pKi = 8.4 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)C4CCCCC43)nc(N)c2cc1OC 10.1021/jm960510x
90645602 111930 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 553 7 1 8 5.0 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccc(NC(=O)c5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298020 111930 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 553 7 1 8 5.0 COc1ccccc1N1CCN(CCn2c(C)nc3c(sc4ccc(NC(=O)c5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
44431616 87635 0 None 3 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 471 8 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234650 87635 0 None 3 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 471 8 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
3584 3706 60 None -2 14 Rat 8.4 pKi = 8.4 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980053f
5401 3706 60 None -2 14 Rat 8.4 pKi = 8.4 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980053f
7302 3706 60 None -2 14 Rat 8.4 pKi = 8.4 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980053f
CHEMBL611 3706 60 None -2 14 Rat 8.4 pKi = 8.4 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980053f
DB01162 3706 60 None -2 14 Rat 8.4 pKi = 8.4 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980053f
44431184 92404 0 None -2 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 515 5 0 5 5.5 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4ccc5ccc(F)cc5c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
CHEMBL243866 92404 0 None -2 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 515 5 0 5 5.5 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4ccc5ccc(F)cc5c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
10310103 106815 0 None 1 10 Bovine 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL317333 106815 0 None 1 10 Bovine 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
10602180 168404 0 None 5 3 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 525 5 1 8 4.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ncc(-c6ccccc6)nc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL43909 168404 0 None 5 3 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 525 5 1 8 4.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ncc(-c6ccccc6)nc54)c3=O)C[C@@H]21 10.1021/jm990567u
10326069 39044 1 None 23 9 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
CHEMBL147077 39044 1 None 23 9 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
44447003 154246 0 None -8 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 448 7 1 5 4.6 CCCC(=O)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
CHEMBL400235 154246 0 None -8 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 448 7 1 5 4.6 CCCC(=O)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
10326069 39044 1 None 23 9 Human 8.4 pKi = 8.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL147077 39044 1 None 23 9 Human 8.4 pKi = 8.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
1443 1989 30 None 1 11 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm960697s
33625 1989 30 None 1 11 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm960697s
501 1989 30 None 1 11 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm960697s
CHEMBL279516 1989 30 None 1 11 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm960697s
DB08950 1989 30 None 1 11 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm960697s
129211 3680 75 None -1 16 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm960697s
2562 3680 75 None -1 16 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm960697s
488 3680 75 None -1 16 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm960697s
CHEMBL836 3680 75 None -1 16 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm960697s
DB00706 3680 75 None -1 16 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm960697s
9817640 98858 0 None 9 3 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 295 6 1 2 3.6 COc1ccc(CCNCC2CCc3ccccc3C2)cc1 10.1021/jm960697s
CHEMBL282214 98858 0 None 9 3 Human 8.4 pKi = 8.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 295 6 1 2 3.6 COc1ccc(CCNCC2CCc3ccccc3C2)cc1 10.1021/jm960697s
44298644 162565 0 None 31 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 454 7 1 6 2.6 Cc1c[nH]c(=O)n(CC(C)(C)CN2CCN(c3ccccc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
CHEMBL417758 162565 0 None 31 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 454 7 1 6 2.6 Cc1c[nH]c(=O)n(CC(C)(C)CN2CCN(c3ccccc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
12909387 62293 0 None 33 2 Bovine 7.5 pKi = 7.5 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 301 0 0 3 3.8 CN1CCC(=C2c3cc(C#N)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL178376 62293 0 None 33 2 Bovine 7.5 pKi = 7.5 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 301 0 0 3 3.8 CN1CCC(=C2c3cc(C#N)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
102012413 78231 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Tested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assayTested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assay
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H]1c1ccc(F)c(F)c1 10.1016/s0960-894x(00)00524-2
CHEMBL2112365 78231 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Tested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assayTested for binding affinity against recombinant human Alpha-1A adrenergic receptor using [125I]HEAT in competition binding assay
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H]1c1ccc(F)c(F)c1 10.1016/s0960-894x(00)00524-2
240 929 39 None -4 25 Rat 7.5 pKi = 7.5 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
2769 929 39 None -4 25 Rat 7.5 pKi = 7.5 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
44279790 929 39 None -4 25 Rat 7.5 pKi = 7.5 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
660 929 39 None -4 25 Rat 7.5 pKi = 7.5 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
CHEMBL1729 929 39 None -4 25 Rat 7.5 pKi = 7.5 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
CHEMBL560739 929 39 None -4 25 Rat 7.5 pKi = 7.5 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
DB00604 929 39 None -4 25 Rat 7.5 pKi = 7.5 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
4038180 202 11 None -2 6 Bovine 7.5 pKi = 7.5 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
480 202 11 None -2 6 Bovine 7.5 pKi = 7.5 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
CHEMBL109783 202 11 None -2 6 Bovine 7.5 pKi = 7.5 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
44420423 83577 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 455 4 1 5 4.3 Cc1nc2c([nH]c3ccccc32)c(=O)n1CCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2006.09.034
CHEMBL220717 83577 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 455 4 1 5 4.3 Cc1nc2c([nH]c3ccccc32)c(=O)n1CCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2006.09.034
127040157 136391 0 None -10 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNC[C@@H]2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1039/C4MD00484A
CHEMBL3739897 136391 0 None -10 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNC[C@@H]2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1039/C4MD00484A
CHEMBL3742490 136391 0 None -10 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNC[C@@H]2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1039/C4MD00484A
155563002 176084 0 None -15 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 10 1 5 4.2 COc1ccccc1OCCNC[C@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4570387 176084 0 None -15 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 10 1 5 4.2 COc1ccccc1OCCNC[C@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4598207 176084 0 None -15 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 10 1 5 4.2 COc1ccccc1OCCNC[C@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
118716709 114492 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 457 5 0 6 3.1 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)C4CCCCC4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342862 114492 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 457 5 0 6 3.1 COc1ccccc1N1CCN(CC2COC3(CCN(C(=O)C4CCCCC4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
44388493 62760 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranesInhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranes
ChEMBL 500 8 0 6 4.3 Clc1ccc(C2(Cn3ccnc3)OCC(CN3CCN(CCc4ccccc4)CC3)O2)c(Cl)c1 10.1021/jm0491804
CHEMBL178921 62760 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranesInhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranes
ChEMBL 500 8 0 6 4.3 Clc1ccc(C2(Cn3ccnc3)OCC(CN3CCN(CCc4ccccc4)CC3)O2)c(Cl)c1 10.1021/jm0491804
46882086 5724 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 435 10 1 6 4.0 COc1cc(OC)cc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)c1 10.1016/j.bmcl.2010.01.030
CHEMBL1078954 5724 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 435 10 1 6 4.0 COc1cc(OC)cc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)c1 10.1016/j.bmcl.2010.01.030
9796667 108965 0 None 9 2 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 309 3 2 3 2.4 CS(=O)(=O)Nc1ccc(F)c2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL322042 108965 0 None 9 2 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 309 3 2 3 2.4 CS(=O)(=O)Nc1ccc(F)c2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
11857862 85236 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 538 10 1 6 4.8 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCC(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL228607 85236 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 538 10 1 6 4.8 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCC(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
11857862 85236 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 538 10 1 6 4.8 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCC(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL228607 85236 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 538 10 1 6 4.8 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCC(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
44331174 4090 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 355 3 0 2 4.9 O=C1c2ccccc2CC12CCN(CCc1cccc3ccccc13)CC2 10.1016/s0960-894x(98)00732-x
CHEMBL100052 4090 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 355 3 0 2 4.9 O=C1c2ccccc2CC12CCN(CCc1cccc3ccccc13)CC2 10.1016/s0960-894x(98)00732-x
9981635 36664 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 459 5 2 5 4.4 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1cccc(C(F)(F)F)c1)C3 10.1021/jm030952q
CHEMBL145098 36664 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 459 5 2 5 4.4 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1cccc(C(F)(F)F)c1)C3 10.1021/jm030952q
CHEMBL2112853 36664 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 459 5 2 5 4.4 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1cccc(C(F)(F)F)c1)C3 10.1021/jm030952q
24803797 60739 0 None -7 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 626 11 0 6 7.6 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
CHEMBL1765111 60739 0 None -7 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 626 11 0 6 7.6 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
24803482 60989 0 None -125 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767168 60989 0 None -125 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
71817861 101920 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
CHEMBL3039699 101920 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
CHEMBL3217244 101920 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 356 7 2 6 2.5 COc1ccc2c(c1OCCNC[C@@H]1COc3ccccc3O1)NCC2 10.1021/jm400867d
3826471 97016 12 None -17 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 296 5 0 3 3.1 COc1ccccc1N1CCN(CCc2ccccc2)CC1 10.1016/j.ejmech.2016.06.052
CHEMBL27021 97016 12 None -17 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 296 5 0 3 3.1 COc1ccccc1N1CCN(CCc2ccccc2)CC1 10.1016/j.ejmech.2016.06.052
702235 52916 93 None -7 4 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
CHEMBL15988 52916 93 None -7 4 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
CHEMBL2011564 52916 93 None -7 4 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
10397358 174405 39 None -70 2 Bovine 4.5 pKi = 4.5 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 178 1 2 4 0.1 Nc1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL45665 174405 39 None -70 2 Bovine 4.5 pKi = 4.5 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 178 1 2 4 0.1 Nc1cccnc1N1CCNCC1 10.1021/jm00366a007
132060812 161475 0 None -831 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4160064 161475 0 None -831 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
10287924 109332 0 None -95 5 Human 6.5 pKi = 6.5 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 388 4 0 5 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCc3noc4ccccc34)CC[C@@H]12 10.1021/jm401958n
CHEMBL3233411 109332 0 None -95 5 Human 6.5 pKi = 6.5 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 388 4 0 5 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCc3noc4ccccc34)CC[C@@H]12 10.1021/jm401958n
155770281 177163 0 None -3 9 Human 5.5 pKi = 5.5 Binding
Binding affinity to alpha1a (unknown origin)Binding affinity to alpha1a (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4642592 177163 0 None -3 9 Human 5.5 pKi = 5.5 Binding
Binding affinity to alpha1a (unknown origin)Binding affinity to alpha1a (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
118717459 114630 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 444 12 2 6 6.3 COc1ccc2nccc(NCCCCCCCNc3ccnc4ccc(OC)cc34)c2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343981 114630 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 444 12 2 6 6.3 COc1ccc2nccc(NCCCCCCCNc3ccnc4ccc(OC)cc34)c2c1 10.1016/j.bmc.2014.09.017
10579368 105511 0 None -1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 593 9 3 6 5.3 CC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL313251 105511 0 None -1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 593 9 3 6 5.3 CC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
10579368 105511 0 None -1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 593 9 3 6 5.3 CC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
CHEMBL313251 105511 0 None -1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 593 9 3 6 5.3 CC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
52937018 60956 0 None -31 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 355 6 0 4 3.6 CN(C)CCCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767135 60956 0 None -31 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 355 6 0 4 3.6 CN(C)CCCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
52937223 60978 19 None -5 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 381 5 0 4 4.1 CN1CCCC1CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767157 60978 19 None -5 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 381 5 0 4 4.1 CN1CCCC1CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
24803316 60983 0 None -794 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 600 15 1 6 6.9 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1CCNCCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767162 60983 0 None -794 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 600 15 1 6 6.9 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1CCNCCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
250 3322 5 None -8912 13 Human 6.5 pKi = 6.5 Binding
Compound was evaluated for binding affinity against Alpha-1C adrenergic receptor using radioligand binding assayCompound was evaluated for binding affinity against Alpha-1C adrenergic receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
5311416 3322 5 None -8912 13 Human 6.5 pKi = 6.5 Binding
Compound was evaluated for binding affinity against Alpha-1C adrenergic receptor using radioligand binding assayCompound was evaluated for binding affinity against Alpha-1C adrenergic receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
CHEMBL69733 3322 5 None -8912 13 Human 6.5 pKi = 6.5 Binding
Compound was evaluated for binding affinity against Alpha-1C adrenergic receptor using radioligand binding assayCompound was evaluated for binding affinity against Alpha-1C adrenergic receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
118717459 114630 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 444 12 2 6 6.3 COc1ccc2nccc(NCCCCCCCNc3ccnc4ccc(OC)cc34)c2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343981 114630 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 444 12 2 6 6.3 COc1ccc2nccc(NCCCCCCCNc3ccnc4ccc(OC)cc34)c2c1 10.1016/j.bmc.2014.09.017
3584 3706 60 None -2 14 Human 7.5 pKi = 7.5 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
5401 3706 60 None -2 14 Human 7.5 pKi = 7.5 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
7302 3706 60 None -2 14 Human 7.5 pKi = 7.5 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
CHEMBL611 3706 60 None -2 14 Human 7.5 pKi = 7.5 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
DB01162 3706 60 None -2 14 Human 7.5 pKi = 7.5 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparations
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
2286 3122 48 None -10 30 Rat 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3122 48 None -10 30 Rat 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3122 48 None -10 30 Rat 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3122 48 None -10 30 Rat 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3122 48 None -10 30 Rat 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
10043148 204804 0 None -26 2 Rat 6.5 pKi = 6.5 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 344 6 0 5 1.9 COc1ccccc1N1CCN(CCCN2CC3CCCN3C2)CC1 10.1021/jm970216k
CHEMBL88594 204804 0 None -26 2 Rat 6.5 pKi = 6.5 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 344 6 0 5 1.9 COc1ccccc1N1CCN(CCCN2CC3CCCN3C2)CC1 10.1021/jm970216k
11995036 11724 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL1182196 11724 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL218732 11724 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
14004032 119316 2 None -1 2 Bovine 5.5 pKi = 5.5 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 188 0 0 2 2.2 c1cnc2c(c1)CCN1CCCCC21 10.1021/jm00398a025
CHEMBL348538 119316 2 None -1 2 Bovine 5.5 pKi = 5.5 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 188 0 0 2 2.2 c1cnc2c(c1)CCN1CCCCC21 10.1021/jm00398a025
53328116 63039 0 None -5 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 411 5 0 4 3.4 O=C1CC(c2ccccc2)CC(=O)N1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796029 63039 0 None -5 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 411 5 0 4 3.4 O=C1CC(c2ccccc2)CC(=O)N1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.ejmech.2011.03.054
14004032 119316 2 None -1 2 Bovine 5.5 pKi = 5.5 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 188 0 0 2 2.2 c1cnc2c(c1)CCN1CCCCC21 10.1021/jm00398a025
CHEMBL348538 119316 2 None -1 2 Bovine 5.5 pKi = 5.5 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 188 0 0 2 2.2 c1cnc2c(c1)CCN1CCCCC21 10.1021/jm00398a025
11732785 163157 0 None -38 6 Rat 7.5 pKi = 7.5 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 432 7 0 5 3.7 COc1ccccc1N1CCN(CCCCN2CCn3c(cc4ccccc43)C2=O)CC1 10.1021/jm0211220
CHEMBL420510 163157 0 None -38 6 Rat 7.5 pKi = 7.5 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 432 7 0 5 3.7 COc1ccccc1N1CCN(CCCCN2CCn3c(cc4ccccc43)C2=O)CC1 10.1021/jm0211220
10020855 78398 0 None -165 6 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 351 4 0 4 3.9 COc1cccc(C2CCC(N3CCN(c4ccccn4)CC3)CC2)c1 10.1021/jm010866v
CHEMBL2112778 78398 0 None -165 6 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 351 4 0 4 3.9 COc1cccc(C2CCC(N3CCN(c4ccccn4)CC3)CC2)c1 10.1021/jm010866v
16041265 94880 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 504 6 2 4 6.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(Cl)cccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL256597 94880 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 504 6 2 4 6.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(Cl)cccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
49865600 15830 0 None -83 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 378 7 1 4 4.4 Clc1cccc(N2CCN(CCCCNc3ccccn3)CC2)c1Cl 10.1016/j.bmcl.2010.07.096
CHEMBL1223616 15830 0 None -83 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 378 7 1 4 4.4 Clc1cccc(N2CCN(CCCCNc3ccccn3)CC2)c1Cl 10.1016/j.bmcl.2010.07.096
122295 9760 6 None 1 9 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00019a001
CHEMBL114166 9760 6 None 1 9 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00019a001
11140347 202818 0 None -5 6 Human 7.5 pKi = 7.5 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72768 202818 0 None -5 6 Human 7.5 pKi = 7.5 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
9824384 118269 1 None -177 8 Bovine 7.5 pKi = 7.5 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1021/jm960510x
CHEMBL342062 118269 1 None -177 8 Bovine 7.5 pKi = 7.5 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1021/jm960510x
145963755 161473 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 465 5 2 9 2.2 COc1cc2nc(N3CCC[C@H](NC(=O)[C@@H]4COc5ccccc5O4)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
CHEMBL4160032 161473 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 465 5 2 9 2.2 COc1cc2nc(N3CCC[C@H](NC(=O)[C@@H]4COc5ccccc5O4)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
10962489 11071 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 404 8 0 3 4.5 C[N+](C)(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
CHEMBL1178679 11071 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 404 8 0 3 4.5 C[N+](C)(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
CHEMBL37212 11071 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 404 8 0 3 4.5 C[N+](C)(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
10962489 11071 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 8 0 3 4.5 C[N+](C)(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
CHEMBL1178679 11071 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 8 0 3 4.5 C[N+](C)(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
CHEMBL37212 11071 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 8 0 3 4.5 C[N+](C)(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
11049096 11077 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 389 8 0 4 4.3 CN(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
CHEMBL1178700 11077 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 389 8 0 4 4.3 CN(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
CHEMBL37962 11077 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 389 8 0 4 4.3 CN(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
9822814 101466 0 None -346 5 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 409 4 0 3 4.3 O=C1CC2(CCCC2)CCN1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL301224 101466 0 None -346 5 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 409 4 0 3 4.3 O=C1CC2(CCCC2)CCN1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
155567201 175644 0 None -20 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 9 1 5 4.2 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)OC1 10.1016/j.ejmech.2019.05.024
CHEMBL4588223 175644 0 None -20 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 9 1 5 4.2 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)OC1 10.1016/j.ejmech.2019.05.024
CHEMBL4594654 175644 0 None -20 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 9 1 5 4.2 COc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)OC1 10.1016/j.ejmech.2019.05.024
44417706 11715 0 None 5 7 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 395 8 1 6 3.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cc3ccccc3cc2O1 10.1021/jm060358r
CHEMBL1182152 11715 0 None 5 7 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 395 8 1 6 3.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cc3ccccc3cc2O1 10.1021/jm060358r
CHEMBL215188 11715 0 None 5 7 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 395 8 1 6 3.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cc3ccccc3cc2O1 10.1021/jm060358r
9822814 101466 0 None -346 5 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 409 4 0 3 4.3 O=C1CC2(CCCC2)CCN1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL301224 101466 0 None -346 5 Human 7.5 pKi = 7.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 409 4 0 3 4.3 O=C1CC2(CCCC2)CCN1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
44435219 91346 0 None 6 4 Human 6.5 pKi = 6.5 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 367 2 0 2 6.2 O=C(Cc1ccc2ccccc2c1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL241115 91346 0 None 6 4 Human 6.5 pKi = 6.5 Binding
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 367 2 0 2 6.2 O=C(Cc1ccc2ccccc2c1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
9932835 100313 0 None -151 4 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 437 4 0 4 4.2 O=C1CC2(CCCCC2)CC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL293111 100313 0 None -151 4 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 437 4 0 4 4.2 O=C1CC2(CCCCC2)CC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
518 3542 1 None -234 6 Human 5.5 pKi = 5.5 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1016/j.bmcl.2004.11.032
9839317 3542 1 None -234 6 Human 5.5 pKi = 5.5 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1016/j.bmcl.2004.11.032
CHEMBL123138 3542 1 None -234 6 Human 5.5 pKi = 5.5 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1016/j.bmcl.2004.11.032
44271624 64429 3 None - 1 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 192 1 0 2 1.9 CN1CC=C(c2ncccc2F)CC1 10.1021/jm00375a017
CHEMBL18194 64429 3 None - 1 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 192 1 0 2 1.9 CN1CC=C(c2ncccc2F)CC1 10.1021/jm00375a017
518 3542 1 None -234 6 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1021/jm00019a001
9839317 3542 1 None -234 6 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1021/jm00019a001
CHEMBL123138 3542 1 None -234 6 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1021/jm00019a001
20750645 101824 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 346 6 1 5 3.4 CC(C)Oc1ccccc1N1CCN(Cc2cc(CO)cs2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL303485 101824 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 346 6 1 5 3.4 CC(C)Oc1ccccc1N1CCN(Cc2cc(CO)cs2)CC1 10.1016/s0960-894x(02)00347-5
127035062 135915 0 None -11 19 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A receptor after 90 mins by scintillation counting methodDisplacement of [3H]Prazosin from human recombinant alpha 1A receptor after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 135915 0 None -11 19 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A receptor after 90 mins by scintillation counting methodDisplacement of [3H]Prazosin from human recombinant alpha 1A receptor after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
44582675 189099 0 None -467 16 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned alpha1A adrenergic receptor by competitive binding experimentInhibition of human cloned alpha1A adrenergic receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189099 0 None -467 16 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned alpha1A adrenergic receptor by competitive binding experimentInhibition of human cloned alpha1A adrenergic receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
12840734 100449 3 None -794 5 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 355 4 0 4 2.5 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2)CC1 10.1021/jm030944+
CHEMBL293968 100449 3 None -794 5 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 355 4 0 4 2.5 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2)CC1 10.1021/jm030944+
76318762 84377 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 435 9 1 6 4.0 COc1cccc(OC)c1OCCNC1COCC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
CHEMBL2234440 84377 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 435 9 1 6 4.0 COc1cccc(OC)c1OCCNC1COCC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
25131193 85749 0 None -239 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 449 10 1 6 4.0 COc1cccc(OC)c1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.02.056
CHEMBL2312225 85749 0 None -239 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 449 10 1 6 4.0 COc1cccc(OC)c1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.02.056
24894141 186816 0 None -30 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 449 10 1 6 4.0 COc1cccc(OC)c1OCCNC[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm800461k
CHEMBL493697 186816 0 None -30 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 449 10 1 6 4.0 COc1cccc(OC)c1OCCNC[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm800461k
25131193 85749 0 None -239 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 449 10 1 6 4.0 COc1cccc(OC)c1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm301525w
CHEMBL2312225 85749 0 None -239 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 449 10 1 6 4.0 COc1cccc(OC)c1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm301525w
53328872 63058 0 None -3 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 433 5 0 5 2.9 COc1ccccc1N1CCN(CCN2C(=O)CC3(CCc4ccccc43)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796048 63058 0 None -3 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 433 5 0 5 2.9 COc1ccccc1N1CCN(CCN2C(=O)CC3(CCc4ccccc43)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
9906978 42451 1 None -2 12 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 42451 1 None -2 12 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
16041451 97346 0 None -5 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 500 7 2 5 5.4 COc1ccc(Cl)cc1NC(=O)NC1CCC(N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL271913 97346 0 None -5 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 500 7 2 5 5.4 COc1ccc(Cl)cc1NC(=O)NC1CCC(N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.11.068
168270256 189464 0 None -8 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-prazosin from rat whole cortex membrane homogenate alpha 1 adrenergic receptorDisplacement of [3H]-prazosin from rat whole cortex membrane homogenate alpha 1 adrenergic receptor
ChEMBL 415 3 0 3 3.7 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4c3c(c(Br)n4C)CC2N(C)C1 10.1021/acs.jmedchem.2c00633
CHEMBL5172469 189464 0 None -8 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-prazosin from rat whole cortex membrane homogenate alpha 1 adrenergic receptorDisplacement of [3H]-prazosin from rat whole cortex membrane homogenate alpha 1 adrenergic receptor
ChEMBL 415 3 0 3 3.7 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4c3c(c(Br)n4C)CC2N(C)C1 10.1021/acs.jmedchem.2c00633
53328686 63055 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 469 7 0 5 4.0 COc1ccc(Cl)cc1N1CCN(CCCN2C(=O)CC(C)(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796045 63055 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 469 7 0 5 4.0 COc1ccc(Cl)cc1N1CCN(CCCN2C(=O)CC(C)(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
2337 3193 72 None -3 63 Rat 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3193 72 None -3 63 Rat 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3193 72 None -3 63 Rat 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3193 72 None -3 63 Rat 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3193 72 None -3 63 Rat 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
75201901 165861 14 None -251 24 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165861 14 None -251 24 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
16756752 142047 0 None -4168 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389129 142047 0 None -4168 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
44460449 204149 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 426 7 0 6 3.7 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3CCCCCC3=O)co2)CC1 10.1016/s0960-894x(02)00436-5
CHEMBL83791 204149 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 426 7 0 6 3.7 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3CCCCCC3=O)co2)CC1 10.1016/s0960-894x(02)00436-5
53328115 63038 0 None -2 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 407 6 0 5 2.8 COc1ccccc1N1CCN(CCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796028 63038 0 None -2 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 407 6 0 5 2.8 COc1ccccc1N1CCN(CCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
132060776 161840 0 None -11 16 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4165863 161840 0 None -11 16 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Prazosin from human adrenergic alpha1A receptor after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
44295193 101295 0 None 11 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 576 7 2 9 2.6 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc3c(c2)OCO3)CC1 10.1016/s0960-894x(99)00653-8
CHEMBL299984 101295 0 None 11 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 576 7 2 9 2.6 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc3c(c2)OCO3)CC1 10.1016/s0960-894x(99)00653-8
46881382 7228 0 None -275 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 437 9 1 5 5.4 COc1ccccc1OCCNCC1CSC(c2ccccc2)(c2ccccc2)S1 10.1016/j.bmcl.2010.01.030
CHEMBL1086156 7228 0 None -275 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 437 9 1 5 5.4 COc1ccccc1OCCNCC1CSC(c2ccccc2)(c2ccccc2)S1 10.1016/j.bmcl.2010.01.030
49832191 166967 0 None -407 3 Human 6.5 pKi = 6.5 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 382 6 2 5 2.9 CNc1ccc2c(c1)C(NCCOc1cc(F)ccc1F)CCS2(=O)=O 10.1016/j.ejmech.2017.07.071
CHEMBL4218307 166967 0 None -407 3 Human 6.5 pKi = 6.5 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 382 6 2 5 2.9 CNc1ccc2c(c1)C(NCCOc1cc(F)ccc1F)CCS2(=O)=O 10.1016/j.ejmech.2017.07.071
CHEMBL4300210 166967 0 None -407 3 Human 6.5 pKi = 6.5 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 382 6 2 5 2.9 CNc1ccc2c(c1)C(NCCOc1cc(F)ccc1F)CCS2(=O)=O 10.1016/j.ejmech.2017.07.071
1346 83 108 None -2884 9 Rat 5.5 pKi = 5.5 Binding
Binding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranesBinding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranes
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00110a014
280 83 108 None -2884 9 Rat 5.5 pKi = 5.5 Binding
Binding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranesBinding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranes
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00110a014
9899402 83 108 None -2884 9 Rat 5.5 pKi = 5.5 Binding
Binding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranesBinding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranes
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00110a014
CHEMBL9666 83 108 None -2884 9 Rat 5.5 pKi = 5.5 Binding
Binding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranesBinding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranes
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00110a014
155515301 169389 0 None -29 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(C[C@H]2OCCOC2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2019.02.056
CHEMBL4441888 169389 0 None -29 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(C[C@H]2OCCOC2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2019.02.056
10092819 16579 0 None -34 12 Rat 7.4 pKi = 7.4 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0211220
CHEMBL124444 16579 0 None -34 12 Rat 7.4 pKi = 7.4 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0211220
44431590 87537 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 555 8 1 6 4.9 COc1ccc(C(F)(F)F)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234231 87537 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 555 8 1 6 4.9 COc1ccc(C(F)(F)F)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
44431615 87596 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 521 8 1 5 4.7 O=S(=O)(N[C@H]1CC[C@@H](N2CCN(c3ccccc3OCC3CC3)CC2)CC1)c1cc(Cl)ccc1F 10.1016/j.bmcl.2007.04.008
CHEMBL234476 87596 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 521 8 1 5 4.7 O=S(=O)(N[C@H]1CC[C@@H](N2CCN(c3ccccc3OCC3CC3)CC2)CC1)c1cc(Cl)ccc1F 10.1016/j.bmcl.2007.04.008
13141187 130181 0 None 9 2 Bovine 7.4 pKi = 7.4 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 378 1 0 3 5.2 CN1CCC(=C2c3cc(SC(F)(F)F)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
CHEMBL368475 130181 0 None 9 2 Bovine 7.4 pKi = 7.4 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 378 1 0 3 5.2 CN1CCC(=C2c3cc(SC(F)(F)F)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
56649650 67501 0 None -41 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910141 67501 0 None -41 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
145946527 166998 0 None 5 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 382 10 0 4 3.6 Cc1cccc(OCCOCCN2CCN(CCc3ccccc3)CC2)c1C 10.1016/j.bmcl.2018.04.059
CHEMBL4217761 166998 0 None 5 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 382 10 0 4 3.6 Cc1cccc(OCCOCCN2CCN(CCc3ccccc3)CC2)c1C 10.1016/j.bmcl.2018.04.059
CHEMBL4300609 166998 0 None 5 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 382 10 0 4 3.6 Cc1cccc(OCCOCCN2CCN(CCc3ccccc3)CC2)c1C 10.1016/j.bmcl.2018.04.059
126225 94522 4 None -13 8 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Alpha-1A adrenergic receptor.In vitro binding affinity at human Alpha-1A adrenergic receptor.
ChEMBL 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm0307741
CHEMBL25467 94522 4 None -13 8 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Alpha-1A adrenergic receptor.In vitro binding affinity at human Alpha-1A adrenergic receptor.
ChEMBL 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm0307741
126225 94522 4 None -13 8 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
CHEMBL25467 94522 4 None -13 8 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
3038603 101382 6 None -48 3 Human 7.4 pKi = 7.4 Binding
The compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligandThe compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligand
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL300647 101382 6 None -48 3 Human 7.4 pKi = 7.4 Binding
The compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligandThe compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligand
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
10790988 115587 0 None -3 3 Rat 7.4 pKi = 7.4 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 483 8 1 10 2.0 COc1cc2nc(N3CCN(C(=O)COc4c(OC)cccc4OC)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL335731 115587 0 None -3 3 Rat 7.4 pKi = 7.4 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 483 8 1 10 2.0 COc1cc2nc(N3CCN(C(=O)COc4c(OC)cccc4OC)CC3)nc(N)c2cc1OC 10.1021/jm9805337
76307950 84382 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 5 0 5 4.1 COc1ccccc1N1CCN(CC2CO[C@@H](c3cccc4ccccc34)O2)CC1 10.1007/s00044-010-9379-1
CHEMBL2234445 84382 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 5 0 5 4.1 COc1ccccc1N1CCN(CC2CO[C@@H](c3cccc4ccccc34)O2)CC1 10.1007/s00044-010-9379-1
10508016 205417 0 None 3 6 Human 7.4 pKi = 7.4 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 613 9 2 5 7.7 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2ccccc2c1 10.1021/jm980077m
CHEMBL92322 205417 0 None 3 6 Human 7.4 pKi = 7.4 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 613 9 2 5 7.7 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2ccccc2c1 10.1021/jm980077m
10508016 84853 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 613 9 2 5 6.8 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2ccccc2c1 10.1007/s00044-004-0120-9
CHEMBL2260369 84853 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 613 9 2 5 6.8 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2ccccc2c1 10.1007/s00044-004-0120-9
76307950 84382 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 5 0 5 4.1 COc1ccccc1N1CCN(CC2CO[C@@H](c3cccc4ccccc34)O2)CC1 10.1007/s00044-010-9379-1
CHEMBL2234445 84382 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 5 0 5 4.1 COc1ccccc1N1CCN(CC2CO[C@@H](c3cccc4ccccc34)O2)CC1 10.1007/s00044-010-9379-1
9944409 7517 0 None 1 5 Rat 7.4 pKi = 7.4 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 307 3 3 4 2.0 CS(=O)(=O)Nc1c(O)ccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL108804 7517 0 None 1 5 Rat 7.4 pKi = 7.4 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 307 3 3 4 2.0 CS(=O)(=O)Nc1c(O)ccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
53328315 63045 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 469 8 0 5 4.2 COc1ccc(Cl)cc1N1CCN(CCCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796035 63045 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 469 8 0 5 4.2 COc1ccc(Cl)cc1N1CCN(CCCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
10617200 26214 0 None -6 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 341 5 2 5 2.4 O[C@@H]1[C@H](NC[C@H]2COc3ccccc3O2)CC[C@H]1Oc1ccccc1 10.1021/jm991065j
CHEMBL135973 26214 0 None -6 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 341 5 2 5 2.4 O[C@@H]1[C@H](NC[C@H]2COc3ccccc3O2)CC[C@H]1Oc1ccccc1 10.1021/jm991065j
9944409 7517 0 None 1 5 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 307 3 3 4 2.0 CS(=O)(=O)Nc1c(O)ccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL108804 7517 0 None 1 5 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 307 3 3 4 2.0 CS(=O)(=O)Nc1c(O)ccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
71719108 85610 1 None -141 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 895 16 6 11 3.5 N=C(N)NCCC[C@@H](NC(=O)CC1(CC(=O)N2CCN(C3c4ccccc4NC(=O)c4ccccc43)CC2)CCCC1)C(=O)NCCn1c(=O)n(-c2ccccc2)n(-c2ccccc2)c1=O 10.1016/j.bmcl.2013.11.061
CHEMBL2307889 85610 1 None -141 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 895 16 6 11 3.5 N=C(N)NCCC[C@@H](NC(=O)CC1(CC(=O)N2CCN(C3c4ccccc4NC(=O)c4ccccc43)CC2)CCCC1)C(=O)NCCn1c(=O)n(-c2ccccc2)n(-c2ccccc2)c1=O 10.1016/j.bmcl.2013.11.061
10619916 205001 0 None -12 2 Rat 6.4 pKi = 6.4 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 382 5 0 4 3.0 FC(F)(F)c1cccc(N2CCN(CCCN3CC4CCCN4C3)CC2)c1 10.1021/jm970216k
CHEMBL89950 205001 0 None -12 2 Rat 6.4 pKi = 6.4 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 382 5 0 4 3.0 FC(F)(F)c1cccc(N2CCN(CCCN3CC4CCCN4C3)CC2)c1 10.1021/jm970216k
9909389 164748 5 None -524 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 408 6 1 5 3.5 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
CHEMBL423361 164748 5 None -524 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 408 6 1 5 3.5 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
9809007 171986 6 None 134 6 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
CHEMBL448620 171986 6 None 134 6 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
9976756 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm021078o
CHEMBL1083181 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm021078o
CHEMBL37883 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm021078o
9976756 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL1083181 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL37883 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
9976756 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.bmcl.2010.01.030
CHEMBL1083181 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.bmcl.2010.01.030
CHEMBL37883 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.bmcl.2010.01.030
9976756 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1039/C4MD00484A
CHEMBL1083181 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1039/C4MD00484A
CHEMBL37883 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1039/C4MD00484A
9976756 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm200421e
CHEMBL1083181 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm200421e
CHEMBL37883 6514 0 None -10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 375 8 1 4 4.0 c1ccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm200421e
44431173 92356 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 519 5 0 5 4.8 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4c(F)c(F)c(F)c(F)c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
CHEMBL243690 92356 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 519 5 0 5 4.8 CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4c(F)c(F)c(F)c(F)c4C3=O)CC2)CC1 10.1016/j.bmcl.2006.12.111
12613159 186733 7 None -1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL493054 186733 7 None -1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
10084076 97454 0 None -20 9 Human 6.4 pKi = 6.4 Binding
Binding affinity towards alpha-1-adrenergic receptorBinding affinity towards alpha-1-adrenergic receptor
ChEMBL 262 0 1 2 2.8 CN1CCc2ccc3c4c2[C@H]1Cc1cccc(c1-4)[C@@H]3N 10.1021/jm030030n
CHEMBL27251 97454 0 None -20 9 Human 6.4 pKi = 6.4 Binding
Binding affinity towards alpha-1-adrenergic receptorBinding affinity towards alpha-1-adrenergic receptor
ChEMBL 262 0 1 2 2.8 CN1CCc2ccc3c4c2[C@H]1Cc1cccc(c1-4)[C@@H]3N 10.1021/jm030030n
3024499 174890 67 None -20 2 Bovine 6.4 pKi = 6.4 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cccc(N2CCNCC2)n1 10.1021/jm00366a007
CHEMBL45773 174890 67 None -20 2 Bovine 6.4 pKi = 6.4 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cccc(N2CCNCC2)n1 10.1021/jm00366a007
11384983 195616 0 None -295 4 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 433 4 0 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2Br)CC1 10.1021/jm030944+
CHEMBL56869 195616 0 None -295 4 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 433 4 0 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2Br)CC1 10.1021/jm030944+
10651027 120537 0 None 11 3 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 588 11 3 7 3.7 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(CN(C)C)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
CHEMBL356923 120537 0 None 11 3 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 588 11 3 7 3.7 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(CN(C)C)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
98358 118968 8 None 1 2 Bovine 7.4 pKi = 7.4 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 226 0 1 1 3.3 c1ccc2c3c([nH]c2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL345349 118968 8 None 1 2 Bovine 7.4 pKi = 7.4 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 226 0 1 1 3.3 c1ccc2c3c([nH]c2c1)C1CCCCN1CC3 10.1021/jm00398a025
44267884 15376 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 403 8 0 6 2.2 CC(C)Oc1ccccc1N1CCN(CCOC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL12202 15376 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 403 8 0 6 2.2 CC(C)Oc1ccccc1N1CCN(CCOC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
44426405 85228 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 562 9 1 5 5.7 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1ccc(OC(F)F)cc1 10.1016/j.bmcl.2007.04.098
CHEMBL228554 85228 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 562 9 1 5 5.7 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1ccc(OC(F)F)cc1 10.1016/j.bmcl.2007.04.098
60785 204167 42 None -630 8 Rat 7.4 pKi = 7.4 Binding
Binding affinity to rat cerebral cortex homogenate alpha 1 adrenergic receptor assessed as inhibition constantBinding affinity to rat cerebral cortex homogenate alpha 1 adrenergic receptor assessed as inhibition constant
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL83894 204167 42 None -630 8 Rat 7.4 pKi = 7.4 Binding
Binding affinity to rat cerebral cortex homogenate alpha 1 adrenergic receptor assessed as inhibition constantBinding affinity to rat cerebral cortex homogenate alpha 1 adrenergic receptor assessed as inhibition constant
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.2c00633
133 2450 48 None -70 43 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2450 48 None -70 43 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2450 48 None -70 43 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2450 48 None -70 43 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2450 48 None -70 43 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
16040907 97421 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 466 7 2 5 4.7 COc1ccccc1NC(=O)NC1CCC(N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL272340 97421 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 466 7 2 5 4.7 COc1ccccc1NC(=O)NC1CCC(N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.11.068
71508684 86608 0 None 169 2 Bovine 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 371 3 0 5 4.2 CN1CCC(c2cn(-c3ccncc3)c3ccc(-c4cnn(C)c4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL2325929 86608 0 None 169 2 Bovine 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysisDisplacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
ChEMBL 371 3 0 5 4.2 CN1CCC(c2cn(-c3ccncc3)c3ccc(-c4cnn(C)c4)cc23)CC1 10.1016/j.bmc.2012.10.049
2470 3583 46 None -398 60 Rat 7.4 pKi = 7.4 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm960510x
3300 3583 46 None -398 60 Rat 7.4 pKi = 7.4 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm960510x
5265 3583 46 None -398 60 Rat 7.4 pKi = 7.4 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm960510x
99 3583 46 None -398 60 Rat 7.4 pKi = 7.4 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm960510x
CHEMBL267930 3583 46 None -398 60 Rat 7.4 pKi = 7.4 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm960510x
98358 118968 8 None 1 2 Bovine 7.4 pKi = 7.4 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 226 0 1 1 3.3 c1ccc2c3c([nH]c2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL345349 118968 8 None 1 2 Bovine 7.4 pKi = 7.4 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 226 0 1 1 3.3 c1ccc2c3c([nH]c2c1)C1CCCCN1CC3 10.1021/jm00398a025
44288469 161129 0 None 1 3 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1ccc2c(c1)CCC1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC21 10.1021/jm990567u
CHEMBL41332 161129 0 None 1 3 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1ccc2c(c1)CCC1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC21 10.1021/jm990567u
127024959 137263 0 None -30 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2ccccc2F)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
CHEMBL3759607 137263 0 None -30 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2ccccc2F)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
155562125 175759 0 None -20 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 8 1 4 4.4 c1ccc(OCCNCC2CCOC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4582160 175759 0 None -20 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 8 1 4 4.4 c1ccc(OCCNCC2CCOC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4595563 175759 0 None -20 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 8 1 4 4.4 c1ccc(OCCNCC2CCOC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
56945165 71159 0 None -69 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 442 6 1 4 4.6 COc1ccccc1N1CCN(C[C@H]2CCC(c3ccccc3)(c3ccccc3)[C@H]2O)CC1 10.1021/jm200421e
CHEMBL1946787 71159 0 None -69 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 442 6 1 4 4.6 COc1ccccc1N1CCN(C[C@H]2CCC(c3ccccc3)(c3ccccc3)[C@H]2O)CC1 10.1021/jm200421e
CHEMBL1962770 71159 0 None -69 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 442 6 1 4 4.6 COc1ccccc1N1CCN(C[C@H]2CCC(c3ccccc3)(c3ccccc3)[C@H]2O)CC1 10.1021/jm200421e
44288492 162850 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 439 9 1 6 2.9 COC(=O)C1(c2ccccc2)CCN(CCNC(=O)CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL41959 162850 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 439 9 1 6 2.9 COC(=O)C1(c2ccccc2)CCN(CCNC(=O)CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(00)00307-3
2419 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2010.05.023
9 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2010.05.023
CHEMBL13647 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2010.05.023
2419 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2019.02.056
9 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2019.02.056
CHEMBL13647 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assayDisplacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2019.02.056
2419 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.bmcl.2010.01.030
9 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.bmcl.2010.01.030
CHEMBL13647 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.bmcl.2010.01.030
2419 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm991065j
9 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm991065j
CHEMBL13647 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm991065j
2419 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm800461k
9 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm800461k
CHEMBL13647 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm800461k
2419 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm301525w
9 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm301525w
CHEMBL13647 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm301525w
2419 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm200421e
9 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm200421e
CHEMBL13647 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm200421e
3778834 100837 70 None -144 2 Bovine 5.4 pKi = 5.4 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 208 2 1 5 0.4 O=[N+]([O-])c1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL296653 100837 70 None -144 2 Bovine 5.4 pKi = 5.4 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 208 2 1 5 0.4 O=[N+]([O-])c1cccnc1N1CCNCC1 10.1021/jm00366a007
11338314 170794 0 None -676 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 391 4 0 4 2.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccc(F)cc2F)CC1 10.1021/jm0491391
CHEMBL446180 170794 0 None -676 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 391 4 0 4 2.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccc(F)cc2F)CC1 10.1021/jm0491391
294234 102407 3 None -512 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 182 1 1 3 1.7 C1CCCC(NC2=NCCO2)CC1 10.1016/0960-894X(94)85032-1
CHEMBL305928 102407 3 None -512 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 182 1 1 3 1.7 C1CCCC(NC2=NCCO2)CC1 10.1016/0960-894X(94)85032-1
10640982 26215 0 None -467 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 341 5 2 5 2.4 O[C@H]1[C@@H](NC[C@H]2COc3ccccc3O2)CC[C@@H]1Oc1ccccc1 10.1021/jm991065j
CHEMBL135974 26215 0 None -467 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 341 5 2 5 2.4 O[C@H]1[C@@H](NC[C@H]2COc3ccccc3O2)CC[C@@H]1Oc1ccccc1 10.1021/jm991065j
2419 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2016.09.050
9 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2016.09.050
CHEMBL13647 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2016.09.050
9796526 109383 0 None 6 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 305 3 2 3 2.6 Cc1ccc(NS(C)(=O)=O)c2c1C(c1c[nH]cn1)CCC2 10.1021/jm030551a
CHEMBL323440 109383 0 None 6 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 305 3 2 3 2.6 Cc1ccc(NS(C)(=O)=O)c2c1C(c1c[nH]cn1)CCC2 10.1021/jm030551a
71455083 81404 0 None -64 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand binding assayBinding affinity to adrenergic alpha1A receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164354 81404 0 None -64 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand binding assayBinding affinity to adrenergic alpha1A receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
3033538 1287 36 None -7 9 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
7155 1287 36 None -7 9 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
781 1287 36 None -7 9 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
CHEMBL1201216 1287 36 None -7 9 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
DB00298 1287 36 None -7 9 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
13091268 77830 0 None -42 14 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL210578 77830 0 None -42 14 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-1A receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
52937830 60975 0 None -125 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 367 4 0 4 3.7 CN1CCC[C@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767154 60975 0 None -125 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 367 4 0 4 3.7 CN1CCC[C@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
17747460 60985 8 None -158 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767164 60985 8 None -158 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
3584 3706 60 None -2 14 Human 7.4 pKi = 7.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm960697s
5401 3706 60 None -2 14 Human 7.4 pKi = 7.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm960697s
7302 3706 60 None -2 14 Human 7.4 pKi = 7.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm960697s
CHEMBL611 3706 60 None -2 14 Human 7.4 pKi = 7.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm960697s
DB01162 3706 60 None -2 14 Human 7.4 pKi = 7.4 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm960697s
56946579 71154 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 440 6 0 4 4.8 COc1ccccc1N1CCN(CC2CCC(c3ccccc3)(c3ccccc3)C2=O)CC1 10.1021/jm200421e
CHEMBL1946783 71154 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 440 6 0 4 4.8 COc1ccccc1N1CCN(CC2CCC(c3ccccc3)(c3ccccc3)C2=O)CC1 10.1021/jm200421e
CHEMBL1962755 71154 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 440 6 0 4 4.8 COc1ccccc1N1CCN(CC2CCC(c3ccccc3)(c3ccccc3)C2=O)CC1 10.1021/jm200421e
52937729 60967 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2cccc(Cl)c2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767146 60967 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2cccc(Cl)c2)c2ccccc2c1=O 10.1021/jm1013874
11857791 168420 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 554 7 1 6 4.9 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2007.04.098
CHEMBL439197 168420 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 554 7 1 6 4.9 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2007.04.098
3584 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity radioligandIn vitro binding affinity radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990200p
5401 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity radioligandIn vitro binding affinity radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990200p
7302 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity radioligandIn vitro binding affinity radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990200p
CHEMBL611 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity radioligandIn vitro binding affinity radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990200p
DB01162 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity radioligandIn vitro binding affinity radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990200p
44289525 165431 0 None -4 9 Human 8.4 pKi = 8.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNCC1Oc2ccccc2OC1c1ccc(C)cc1 10.1016/j.bmcl.2004.11.032
CHEMBL42539 165431 0 None -4 9 Human 8.4 pKi = 8.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNCC1Oc2ccccc2OC1c1ccc(C)cc1 10.1016/j.bmcl.2004.11.032
57402787 68838 0 None -1 5 Pig 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1926700 68838 0 None -1 5 Pig 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
2142 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
4920903 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
502 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
5775 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
CHEMBL597 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
DB00692 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
10555134 40541 0 None 173 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 573 9 2 8 4.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc3c(c2)OCO3)CC1 10.1007/s00044-004-0120-9
CHEMBL148552 40541 0 None 173 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 573 9 2 8 4.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc3c(c2)OCO3)CC1 10.1007/s00044-004-0120-9
44428851 91872 0 None -8 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 447 4 1 7 3.5 COc1cc2nc(N3CCN(C(=O)c4ccccc4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
CHEMBL242934 91872 0 None -8 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 447 4 1 7 3.5 COc1cc2nc(N3CCN(C(=O)c4ccccc4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
491 191 4 None -50 12 Human 8.4 pKi = 8.4 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
9891167 191 4 None -50 12 Human 8.4 pKi = 8.4 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
CHEMBL13856 191 4 None -50 12 Human 8.4 pKi = 8.4 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
10555134 40541 0 None 173 3 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 573 9 2 8 4.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc3c(c2)OCO3)CC1 10.1021/jm980506g
CHEMBL148552 40541 0 None 173 3 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 573 9 2 8 4.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(C)=O)C2c2ccc3c(c2)OCO3)CC1 10.1021/jm980506g
3584 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
5401 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
7302 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
CHEMBL611 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
DB01162 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1016/s0960-894x(98)00446-6
10554745 36986 0 None 97 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 552 10 1 6 4.9 COC(=O)C1(c2ccccc2)CCN(CCCCCN2C(C)=NC(C)=C(C(N)=O)C2c2ccc(F)cc2F)CC1 10.1021/jm9902032
CHEMBL145353 36986 0 None 97 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 552 10 1 6 4.9 COC(=O)C1(c2ccccc2)CCN(CCCCCN2C(C)=NC(C)=C(C(N)=O)C2c2ccc(F)cc2F)CC1 10.1021/jm9902032
491 191 4 None -50 12 Human 8.4 pKi = 8.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/j.bmcl.2004.11.032
9891167 191 4 None -50 12 Human 8.4 pKi = 8.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/j.bmcl.2004.11.032
CHEMBL13856 191 4 None -50 12 Human 8.4 pKi = 8.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/j.bmcl.2004.11.032
3584 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980053f
5401 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980053f
7302 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980053f
CHEMBL611 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980053f
DB01162 3706 60 None -2 14 Human 8.4 pKi = 8.4 Binding
Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980053f
57390119 68946 0 None 9 5 Pig 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928127 68946 0 None 9 5 Pig 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
10603030 205720 0 None 47 3 Human 8.4 pKi = 8.4 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 565 7 3 4 4.5 N#Cc1cc(F)ccc1C1CCN(CCCNC(=O)C2=C(C(F)(F)F)NC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
CHEMBL94259 205720 0 None 47 3 Human 8.4 pKi = 8.4 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 565 7 3 4 4.5 N#Cc1cc(F)ccc1C1CCN(CCCNC(=O)C2=C(C(F)(F)F)NC(=O)N[C@@H]2c2ccc(F)c(F)c2)CC1 10.1021/jm990612y
44362633 121020 0 None 95 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 597 9 3 6 3.9 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCC(C)N2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL358590 121020 0 None 95 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 597 9 3 6 3.9 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCC(C)N2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
10674133 162856 0 None 32 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 546 9 2 7 2.9 CCOc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
CHEMBL419624 162856 0 None 32 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 546 9 2 7 2.9 CCOc1ccccc1N1CCN(CC(O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
44428848 91848 0 None -17 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 453 4 1 8 3.6 COc1cc2nc(N3CCN(C(=O)c4cccs4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
CHEMBL242724 91848 0 None -17 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 453 4 1 8 3.6 COc1cc2nc(N3CCN(C(=O)c4cccs4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
134551 355 25 None -3 21 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 355 25 None -3 21 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 355 25 None -3 21 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 355 25 None -3 21 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
44431594 166845 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 532 9 1 8 3.8 COc1ccc([N+](=O)[O-])cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL429623 166845 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 532 9 1 8 3.8 COc1ccc([N+](=O)[O-])cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
136806211 205939 0 None 61 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 650 14 4 7 5.0 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CCCCN)N1 10.1016/s0960-894x(99)00484-9
44328738 205939 0 None 61 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 650 14 4 7 5.0 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CCCCN)N1 10.1016/s0960-894x(99)00484-9
CHEMBL95434 205939 0 None 61 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 650 14 4 7 5.0 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CCCCN)N1 10.1016/s0960-894x(99)00484-9
9817640 98858 0 None 9 3 Human 8.4 pKi = 8.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 295 6 1 2 3.6 COc1ccc(CCNCC2CCc3ccccc3C2)cc1 10.1016/j.bmcl.2004.11.032
CHEMBL282214 98858 0 None 9 3 Human 8.4 pKi = 8.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 295 6 1 2 3.6 COc1ccc(CCNCC2CCc3ccccc3C2)cc1 10.1016/j.bmcl.2004.11.032
489 145 22 None -4 13 Bovine 8.4 pKi = 8.4 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
5640 145 22 None -4 13 Bovine 8.4 pKi = 8.4 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
CHEMBL420060 145 22 None -4 13 Bovine 8.4 pKi = 8.4 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
10841387 99144 0 None 91 6 Human 8.4 pKi = 8.4 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL284103 99144 0 None 91 6 Human 8.4 pKi = 8.4 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
10841387 99144 0 None 91 6 Human 8.4 pKi = 8.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL284103 99144 0 None 91 6 Human 8.4 pKi = 8.4 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
73453 29388 22 None -6 17 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29388 22 None -6 17 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
136680384 205911 0 None 104 6 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 694 16 4 8 4.9 CCNC(=O)C1=C(CC)NC(COCCN)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
44328799 205911 0 None 104 6 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 694 16 4 8 4.9 CCNC(=O)C1=C(CC)NC(COCCN)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
CHEMBL95290 205911 0 None 104 6 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 694 16 4 8 4.9 CCNC(=O)C1=C(CC)NC(COCCN)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
44431602 144396 0 None -6 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 525 7 1 5 5.2 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL391035 144396 0 None -6 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 525 7 1 5 5.2 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2007.04.008
11857710 85179 0 None 10 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 518 8 1 5 5.4 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1 10.1016/j.bmcl.2007.04.098
CHEMBL228279 85179 0 None 10 4 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 518 8 1 5 5.4 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@H](N2CCC(c3ccccc3OC3CC3)CC2)CC1 10.1016/j.bmcl.2007.04.098
10674791 37922 0 None 10 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 582 8 2 7 4.2 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(Cl)cc1 10.1021/jm990200p
CHEMBL146163 37922 0 None 10 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 582 8 2 7 4.2 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(Cl)cc1 10.1021/jm990200p
10674544 118273 0 None 331 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 568 6 2 7 3.5 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CC2)C(=O)Oc2ccccc23)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL342111 118273 0 None 331 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 568 6 2 7 3.5 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CC2)C(=O)Oc2ccccc23)C1c1ccc(F)c(F)c1 10.1021/jm990201h
44417713 12301 0 None 2 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1185884 12301 0 None 2 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL439346 12301 0 None 2 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
118716714 114497 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 501 6 0 7 2.7 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4ccc(C)cc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342867 114497 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 501 6 0 7 2.7 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4ccc(C)cc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
56837634 68949 0 None -10 5 Pig 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928130 68949 0 None -10 5 Pig 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
44362867 37399 0 None 165 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 658 8 2 5 6.9 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3cc(C)cc(C)c3)(c3cc(C)cc(C)c3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL145719 37399 0 None 165 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 658 8 2 5 6.9 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3cc(C)cc(C)c3)(c3cc(C)cc(C)c3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
2142 3035 54 None -2 37 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
4920903 3035 54 None -2 37 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
502 3035 54 None -2 37 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
5775 3035 54 None -2 37 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
CHEMBL597 3035 54 None -2 37 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
DB00692 3035 54 None -2 37 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
44312563 203202 2 None -3 7 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampus (+ 10 uM) CES membrane using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampus (+ 10 uM) CES membrane using [3H]prazosin as radioligand
ChEMBL 401 7 1 8 1.0 COc1ccc(C)cc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1021/jm960069a
CHEMBL76168 203202 2 None -3 7 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampus (+ 10 uM) CES membrane using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampus (+ 10 uM) CES membrane using [3H]prazosin as radioligand
ChEMBL 401 7 1 8 1.0 COc1ccc(C)cc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1021/jm960069a
463 1373 17 None 5 13 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
6918097 1373 17 None 5 13 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
837 1373 17 None 5 13 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
CHEMBL2051956 1373 17 None 5 13 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
DB14068 1373 17 None 5 13 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
44299835 196715 0 None 61 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 583 7 2 7 4.0 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccn4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL57691 196715 0 None 61 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 583 7 2 7 4.0 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccn4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
56961507 120915 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 678 6 4 11 5.0 COc1cc2nc(N3CCN(C(=S)Nc4ccc(-c5c6ccc(=O)cc-6oc6cc(O)ccc56)c(C(=O)O)c4)CC3)nc(N)c2cc1OC 10.1021/ml5004298
CHEMBL3582271 120915 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
ChEMBL 678 6 4 11 5.0 COc1cc2nc(N3CCN(C(=S)Nc4ccc(-c5c6ccc(=O)cc-6oc6cc(O)ccc56)c(C(=O)O)c4)CC3)nc(N)c2cc1OC 10.1021/ml5004298
10554492 167991 0 None -1 3 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 505 5 1 8 3.4 COC(=O)c1ccc2sc3c(=O)n(CCN4C[C@@H]5CCc6c(OC)cccc6[C@@H]5C4)c(=O)[nH]c3c2c1 10.1021/jm990567u
CHEMBL43573 167991 0 None -1 3 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 505 5 1 8 3.4 COC(=O)c1ccc2sc3c(=O)n(CCN4C[C@@H]5CCc6c(OC)cccc6[C@@H]5C4)c(=O)[nH]c3c2c1 10.1021/jm990567u
44294569 101536 0 None -5 4 Human 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 447 7 1 8 2.5 COc1ccccc1N1CCN(CCn2nc(-c3ccccc3)c(C(C)=O)c(N)c2=O)CC1 10.1021/jm981006q
CHEMBL301726 101536 0 None -5 4 Human 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 447 7 1 8 2.5 COc1ccccc1N1CCN(CCn2nc(-c3ccccc3)c(C(C)=O)c(N)c2=O)CC1 10.1021/jm981006q
10532044 84845 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 629 12 2 10 4.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)OCCC#N)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
136901434 84845 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 629 12 2 10 4.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)OCCC#N)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
CHEMBL2260361 84845 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 629 12 2 10 4.0 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)OCCC#N)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
10603688 120620 0 None 645 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 603 11 3 8 3.7 CCNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL357681 120620 0 None 645 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 603 11 3 8 3.7 CCNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL151825 44109 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 629 12 2 10 4.8 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)N=C(C)/C(=C(/O)OCCC#N)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
136680386 205959 0 None 60 6 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 680 16 4 8 4.6 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCCN)N1 10.1016/s0960-894x(99)00484-9
44328801 205959 0 None 60 6 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 680 16 4 8 4.6 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCCN)N1 10.1016/s0960-894x(99)00484-9
CHEMBL95578 205959 0 None 60 6 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 680 16 4 8 4.6 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCCN)N1 10.1016/s0960-894x(99)00484-9
44431555 88718 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 535 8 1 7 3.3 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL236617 88718 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 535 8 1 7 3.3 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
11857793 85217 0 None 7 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 548 7 1 4 5.9 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1cc(Cl)ccc1F 10.1016/j.bmcl.2007.04.098
CHEMBL228494 85217 0 None 7 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 548 7 1 4 5.9 O=S(=O)(N[C@H]1CC[C@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1cc(Cl)ccc1F 10.1016/j.bmcl.2007.04.098
44273916 98360 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 608 7 2 8 3.4 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL278716 98360 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 608 7 2 8 3.4 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4C#N)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
10603688 120620 0 None 645 3 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 603 11 3 8 3.7 CCNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
CHEMBL357681 120620 0 None 645 3 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 603 11 3 8 3.7 CCNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
10154 141585 54 None 58 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membraneDisplacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membrane
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL388342 141585 54 None 58 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membraneDisplacement of [3H]prazosin from adrenergic alpha1A receptor in rat brain membrane
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/np990433j
44431618 86624 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 488 8 1 7 3.3 COc1ccncc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL232607 86624 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 488 8 1 7 3.3 COc1ccncc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
10627329 37195 0 None 8 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 595 7 2 6 4.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145525 37195 0 None 8 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 595 7 2 6 4.4 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
10091187 78399 0 None -23 6 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 380 5 0 4 4.6 COc1cccc(C2CCC(N3CCN(c4ccccc4OC)CC3)CC2)c1 10.1021/jm010866v
CHEMBL2112779 78399 0 None -23 6 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined on human cloned Alpha-1A adrenoceptorBinding affinity was determined on human cloned Alpha-1A adrenoceptor
ChEMBL 380 5 0 4 4.6 COc1cccc(C2CCC(N3CCN(c4ccccc4OC)CC3)CC2)c1 10.1021/jm010866v
10430183 203906 0 None -398 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to human alpha 1A adrenergic receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human alpha 1A adrenergic receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL81728 203906 0 None -398 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to human alpha 1A adrenergic receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human alpha 1A adrenergic receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
2801 161313 56 None -4 29 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161313 56 None -4 29 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161313 56 None -4 29 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
12134996 202379 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 385 6 0 5 3.2 COc1ccccc1N1CCN(Cc2ccc(CN3CCCC3=O)s2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL70178 202379 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 385 6 0 5 3.2 COc1ccccc1N1CCN(Cc2ccc(CN3CCCC3=O)s2)CC1 10.1016/s0960-894x(02)00347-5
11520239 3562 4 None -144 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
1313 3562 4 None -144 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
CHEMBL185271 3562 4 None -144 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
49865641 15844 0 None -3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 338 7 1 4 3.7 Cc1cccc(N2CCN(CCCCNc3ccccn3)CC2)c1C 10.1016/j.bmcl.2010.07.096
CHEMBL1223682 15844 0 None -3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 338 7 1 4 3.7 Cc1cccc(N2CCN(CCCCNc3ccccn3)CC2)c1C 10.1016/j.bmcl.2010.07.096
10320782 99502 0 None -4 7 Rat 7.4 pKi = 7.4 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNC[C@H]1Oc2ccccc2O[C@@H]1c1ccc(C)cc1 10.1021/jm960069a
CHEMBL286565 99502 0 None -4 7 Rat 7.4 pKi = 7.4 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNC[C@H]1Oc2ccccc2O[C@@H]1c1ccc(C)cc1 10.1021/jm960069a
46934645 16493 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 465 7 0 7 2.2 COc1ccccc1N1CCN(C[C@@H]2CO[C@@](CN3C(=O)CCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242725 16493 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 465 7 0 7 2.2 COc1ccccc1N1CCN(C[C@@H]2CO[C@@](CN3C(=O)CCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
15166842 98391 19 None - 1 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 160 1 1 2 1.5 C1=C(c2ccccn2)CCNC1 10.1021/jm00375a017
CHEMBL278934 98391 19 None - 1 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 160 1 1 2 1.5 C1=C(c2ccccn2)CCNC1 10.1021/jm00375a017
9823115 196916 0 None -2041 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 414 4 0 5 3.0 N#Cc1ccc(Cl)cc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
CHEMBL57868 196916 0 None -2041 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 414 4 0 5 3.0 N#Cc1ccc(Cl)cc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
76311538 84390 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 299 6 1 4 2.8 c1ccc(OCCN[C@H]2COC[C@H](c3ccccc3)O2)cc1 10.1007/s00044-010-9379-1
CHEMBL2234453 84390 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 299 6 1 4 2.8 c1ccc(OCCN[C@H]2COC[C@H](c3ccccc3)O2)cc1 10.1007/s00044-010-9379-1
9823115 196916 0 None -2041 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 414 4 0 5 3.0 N#Cc1ccc(Cl)cc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
CHEMBL57868 196916 0 None -2041 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 414 4 0 5 3.0 N#Cc1ccc(Cl)cc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1007/s00044-010-9379-1
25132565 186678 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 313 7 1 4 2.8 c1ccc(OCCNC[C@@H]2COC[C@@H](c3ccccc3)O2)cc1 10.1021/jm800461k
CHEMBL492785 186678 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 313 7 1 4 2.8 c1ccc(OCCNC[C@@H]2COC[C@@H](c3ccccc3)O2)cc1 10.1021/jm800461k
22629308 63961 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 425 3 2 5 3.6 N=C(Nc1ccccc1)N1CCN(/C=C2/N=C(c3cccc4ccccc34)OC2=O)CC1 10.1016/j.bmcl.2004.11.032
CHEMBL181071 63961 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 425 3 2 5 3.6 N=C(Nc1ccccc1)N1CCN(/C=C2/N=C(c3cccc4ccccc34)OC2=O)CC1 10.1016/j.bmcl.2004.11.032
9865254 68318 0 None -512 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 391 4 0 4 2.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccc(F)c(F)c2)CC1 10.1021/jm0491391
CHEMBL192099 68318 0 None -512 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 391 4 0 4 2.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccc(F)c(F)c2)CC1 10.1021/jm0491391
11948707 165603 0 None -128 13 Human 6.4 pKi = 6.4 Binding
Binding affinity to alpha 1A adrenergic receptor by radioligand binding assayBinding affinity to alpha 1A adrenergic receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
CHEMBL426317 165603 0 None -128 13 Human 6.4 pKi = 6.4 Binding
Binding affinity to alpha 1A adrenergic receptor by radioligand binding assayBinding affinity to alpha 1A adrenergic receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
11395842 100211 0 None -21 3 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 412 7 0 4 4.0 CN(CCOc1cc(Cl)ccc1Cl)CCN1C(=O)CC2(CCCC2)CC1=O 10.1021/jm030944+
CHEMBL292399 100211 0 None -21 3 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 412 7 0 4 4.0 CN(CCOc1cc(Cl)ccc1Cl)CCN1C(=O)CC2(CCCC2)CC1=O 10.1021/jm030944+
11058166 202989 0 None -1 5 Human 6.4 pKi = 6.4 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74114 202989 0 None -1 5 Human 6.4 pKi = 6.4 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
52942591 17415 0 None 4 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 542 9 1 7 2.6 COC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL1258228 17415 0 None 4 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 542 9 1 7 2.6 COC(=O)CN1C(=O)N(CC(O)CN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
12039032 97797 0 None 14 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 415 9 0 6 2.1 CC(C)Oc1ccccc1N1CCN(CC(=O)CC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL274529 97797 0 None 14 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 415 9 0 6 2.1 CC(C)Oc1ccccc1N1CCN(CC(=O)CC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
127025279 137117 0 None -3 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 347 9 1 4 2.8 COc1ccccc1N1CCN(CCCCNC(=O)CC(C)C)CC1 10.1016/j.bmcl.2015.12.068
CHEMBL3758403 137117 0 None -3 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 347 9 1 4 2.8 COc1ccccc1N1CCN(CCCCNC(=O)CC(C)C)CC1 10.1016/j.bmcl.2015.12.068
44308654 201881 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 401 6 1 6 3.4 COc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3O)s2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL66823 201881 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 401 6 1 6 3.4 COc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3O)s2)CC1 10.1016/s0960-894x(02)00347-5
9822814 101466 0 None -346 5 Human 7.4 pKi = 7.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 409 4 0 3 4.3 O=C1CC2(CCCC2)CCN1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1016/j.bmcl.2004.11.032
CHEMBL301224 101466 0 None -346 5 Human 7.4 pKi = 7.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 409 4 0 3 4.3 O=C1CC2(CCCC2)CCN1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1016/j.bmcl.2004.11.032
11589069 95787 0 None -25 8 Human 7.4 pKi = 7.4 Binding
Inhibition of adrenergic alpha-1 receptorInhibition of adrenergic alpha-1 receptor
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
CHEMBL260994 95787 0 None -25 8 Human 7.4 pKi = 7.4 Binding
Inhibition of adrenergic alpha-1 receptorInhibition of adrenergic alpha-1 receptor
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
9822814 101466 0 None -389 5 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 409 4 0 3 4.3 O=C1CC2(CCCC2)CCN1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL301224 101466 0 None -389 5 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 409 4 0 3 4.3 O=C1CC2(CCCC2)CCN1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
2419 687 22 None -275 12 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2011.03.054
9 687 22 None -275 12 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2011.03.054
CHEMBL13647 687 22 None -275 12 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/j.ejmech.2011.03.054
506 2212 32 None -81 6 Human 6.4 pKi = 6.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1016/j.bmcl.2004.11.032
6603904 2212 32 None -81 6 Human 6.4 pKi = 6.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1016/j.bmcl.2004.11.032
CHEMBL19476 2212 32 None -81 6 Human 6.4 pKi = 6.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1016/j.bmcl.2004.11.032
506 2212 32 None -81 6 Human 6.4 pKi = 6.4 Binding
Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
6603904 2212 32 None -81 6 Human 6.4 pKi = 6.4 Binding
Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
CHEMBL19476 2212 32 None -81 6 Human 6.4 pKi = 6.4 Binding
Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
11315660 167414 0 None -144 4 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 403 4 0 4 3.6 O=C1CC2(CCCCC2)CC(=O)N1CCN1CCN(c2ccccc2Cl)CC1 10.1021/jm030944+
CHEMBL431943 167414 0 None -144 4 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 403 4 0 4 3.6 O=C1CC2(CCCCC2)CC(=O)N1CCN1CCN(c2ccccc2Cl)CC1 10.1021/jm030944+
155529118 175980 0 None -37 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 9 1 4 4.2 c1ccc(OCCNC[C@@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4462768 175980 0 None -37 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 9 1 4 4.2 c1ccc(OCCNC[C@@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4597358 175980 0 None -37 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 9 1 4 4.2 c1ccc(OCCNC[C@@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
44420418 83003 0 None -13 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 474 4 1 6 4.0 O=c1[nH]c2c(sc3ccccc32)c(=O)n1CCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2006.09.034
CHEMBL219718 83003 0 None -13 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 474 4 1 6 4.0 O=c1[nH]c2c(sc3ccccc32)c(=O)n1CCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2006.09.034
135 2486 38 None -9 58 Bovine 7.4 pKi = 7.4 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00366a007
1796 2486 38 None -9 58 Bovine 7.4 pKi = 7.4 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00366a007
4184 2486 38 None -9 58 Bovine 7.4 pKi = 7.4 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00366a007
CHEMBL6437 2486 38 None -9 58 Bovine 7.4 pKi = 7.4 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00366a007
DB06148 2486 38 None -9 58 Bovine 7.4 pKi = 7.4 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00366a007
11857864 143705 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 534 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4cc(F)ccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL390473 143705 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 534 9 1 6 5.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4cc(F)ccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
2419 687 22 None -52 12 Bovine 7.4 pKi = 7.4 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
9 687 22 None -52 12 Bovine 7.4 pKi = 7.4 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
CHEMBL13647 687 22 None -52 12 Bovine 7.4 pKi = 7.4 Binding
Binding affinity towards bovine Alpha-1A adrenergic receptorBinding affinity towards bovine Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1016/s0960-894x(01)00159-7
3158 55959 21 None -295 20 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55959 21 None -295 20 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
135 2486 38 None -9 58 Bovine 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00375a017
1796 2486 38 None -9 58 Bovine 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00375a017
4184 2486 38 None -9 58 Bovine 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00375a017
CHEMBL6437 2486 38 None -9 58 Bovine 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00375a017
DB06148 2486 38 None -9 58 Bovine 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00375a017
11372228 101184 0 None -51 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 373 4 0 3 3.8 O=C1CC2(C=CN1CCN1CCN(c3ccccc3Cl)CC1)CCCC2 10.1007/s00044-010-9379-1
CHEMBL299253 101184 0 None -51 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 373 4 0 3 3.8 O=C1CC2(C=CN1CCN1CCN(c3ccccc3Cl)CC1)CCCC2 10.1007/s00044-010-9379-1
11108001 10756 2 None -3 6 Human 7.4 pKi = 7.4 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117248 10756 2 None -3 6 Human 7.4 pKi = 7.4 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540542 10756 2 None -3 6 Human 7.4 pKi = 7.4 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
11000184 12926 0 None 1 6 Human 7.4 pKi = 7.4 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1190038 12926 0 None 1 6 Human 7.4 pKi = 7.4 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540035 12926 0 None 1 6 Human 7.4 pKi = 7.4 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
11372228 101184 0 None -51 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 373 4 0 3 3.8 O=C1CC2(C=CN1CCN1CCN(c3ccccc3Cl)CC1)CCCC2 10.1007/s00044-010-9379-1
CHEMBL299253 101184 0 None -51 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 373 4 0 3 3.8 O=C1CC2(C=CN1CCN1CCN(c3ccccc3Cl)CC1)CCCC2 10.1007/s00044-010-9379-1
9802999 193991 0 None -2 3 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 434 5 0 6 3.1 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc([N+](=O)[O-])ccc2Cl)CC1 10.1021/jm030944+
CHEMBL55655 193991 0 None -2 3 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 434 5 0 6 3.1 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc([N+](=O)[O-])ccc2Cl)CC1 10.1021/jm030944+
197001 63002 14 None - 1 Human 6.4 pKi = 6.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1C[C@@H]3N(C)CC2)OCO4 10.1016/j.bmcl.2004.11.032
CHEMBL179440 63002 14 None - 1 Human 6.4 pKi = 6.4 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1C[C@@H]3N(C)CC2)OCO4 10.1016/j.bmcl.2004.11.032
10840781 36687 0 None 3 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 569 8 2 7 3.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccc(C(C)=O)cc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
CHEMBL145122 36687 0 None 3 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 569 8 2 7 3.6 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCN(c3ccc(C(C)=O)cc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990202+
44292470 101151 4 None -57 2 Bovine 5.4 pKi = 5.4 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 211 1 1 3 1.5 Cc1ccnc(N2CCNCC2)c1Cl 10.1021/jm00366a007
CHEMBL299007 101151 4 None -57 2 Bovine 5.4 pKi = 5.4 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 211 1 1 3 1.5 Cc1ccnc(N2CCNCC2)c1Cl 10.1021/jm00366a007
10646816 43120 0 None 7 3 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 441 8 3 6 2.3 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCCCC2)=C(C)N1 10.1021/jm980506g
CHEMBL150743 43120 0 None 7 3 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 441 8 3 6 2.3 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCCCC2)=C(C)N1 10.1021/jm980506g
2419 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm9810654
9 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm9810654
CHEMBL13647 687 22 None -275 12 Human 6.4 pKi = 6.4 Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm9810654
71817857 91679 0 None 3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 354 7 2 5 3.0 COc1ccc2cc[nH]c2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL2419766 91679 0 None 3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 354 7 2 5 3.0 COc1ccc2cc[nH]c2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm400867d
25130876 192015 0 None -125 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 343 8 1 5 2.8 COc1ccccc1OCCNC[C@@H]1CO[C@H](c2ccccc2)CO1 10.1021/jm800461k
CHEMBL521665 192015 0 None -125 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 343 8 1 5 2.8 COc1ccccc1OCCNC[C@@H]1CO[C@H](c2ccccc2)CO1 10.1021/jm800461k
10236758 115259 3 None -446 13 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354065 115259 3 None -446 13 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
71521480 85820 0 None -1096 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNC[C@H]2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm301525w
CHEMBL2312538 85820 0 None -1096 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins
ChEMBL 389 8 1 4 4.0 c1ccc(OCCNC[C@H]2COCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm301525w
44462130 203611 0 None 45 3 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 490 7 0 6 3.5 COC(=O)C1(c2ccccc2)CCN(CCCCN2C(=O)c3cc(Cl)ccc3S2(=O)=O)CC1 10.1016/s0960-894x(98)00451-x
CHEMBL79532 203611 0 None 45 3 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 490 7 0 6 3.5 COC(=O)C1(c2ccccc2)CCN(CCCCN2C(=O)c3cc(Cl)ccc3S2(=O)=O)CC1 10.1016/s0960-894x(98)00451-x
13141185 60150 0 None 9 2 Bovine 7.4 pKi = 7.4 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 356 0 0 2 4.3 CN1CCC(=C2c3cc(Br)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
CHEMBL175508 60150 0 None 9 2 Bovine 7.4 pKi = 7.4 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 356 0 0 2 4.3 CN1CCC(=C2c3cc(Br)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
155533100 175760 0 None -6 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 377 11 1 4 4.5 COc1ccccc1OCCNCCOC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.05.024
CHEMBL4468507 175760 0 None -6 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 377 11 1 4 4.5 COc1ccccc1OCCNCCOC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.05.024
CHEMBL4595564 175760 0 None -6 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 377 11 1 4 4.5 COc1ccccc1OCCNCCOC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.05.024
56945167 71156 0 None -56 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 442 6 1 4 4.6 COc1ccccc1N1CCN(C[C@H]2CCC(c3ccccc3)(c3ccccc3)[C@@H]2O)CC1 10.1021/jm200421e
CHEMBL1946788 71156 0 None -56 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 442 6 1 4 4.6 COc1ccccc1N1CCN(C[C@H]2CCC(c3ccccc3)(c3ccccc3)[C@@H]2O)CC1 10.1021/jm200421e
CHEMBL1962757 71156 0 None -56 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 442 6 1 4 4.6 COc1ccccc1N1CCN(C[C@H]2CCC(c3ccccc3)(c3ccccc3)[C@@H]2O)CC1 10.1021/jm200421e
12488 1619 51 None -77 23 Rat 6.4 pKi = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1619 51 None -77 23 Rat 6.4 pKi = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1619 51 None -77 23 Rat 6.4 pKi = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1619 51 None -77 23 Rat 6.4 pKi = 6.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
9931327 69452 1 None -2290 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 409 4 0 4 2.9 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)c(F)cc2F)CC1 10.1021/jm0491391
CHEMBL193620 69452 1 None -2290 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 409 4 0 4 2.9 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)c(F)cc2F)CC1 10.1021/jm0491391
136 3228 28 None -9332 16 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00019a001
223 3228 28 None -9332 16 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00019a001
643606 3228 28 None -9332 16 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00019a001
CHEMBL10347 3228 28 None -9332 16 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00019a001
1960 2805 64 None -10 26 Bovine 6.4 pKi = 6.4 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
439260 2805 64 None -10 26 Bovine 6.4 pKi = 6.4 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
505 2805 64 None -10 26 Bovine 6.4 pKi = 6.4 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
CHEMBL1437 2805 64 None -10 26 Bovine 6.4 pKi = 6.4 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
DB00368 2805 64 None -10 26 Bovine 6.4 pKi = 6.4 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
9905391 108985 0 None 6 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1ccc(Cl)c2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL322082 108985 0 None 6 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1ccc(Cl)c2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
123981 16267 20 None -245 8 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 10.1021/jm00019a001
CHEMBL123349 16267 20 None -245 8 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 10.1021/jm00019a001
CHEMBL536803 16267 20 None -245 8 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 10.1021/jm00019a001
11740041 204823 0 None -8 2 Rat 7.4 pKi = 7.4 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 372 7 0 5 2.7 COc1ccccc1N1CCN(CCCCN2CC3CCCCN3C2)CC1 10.1021/jm970216k
CHEMBL88715 204823 0 None -8 2 Rat 7.4 pKi = 7.4 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 372 7 0 5 2.7 COc1ccccc1N1CCN(CCCCN2CC3CCCCN3C2)CC1 10.1021/jm970216k
44431612 148320 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 509 7 1 5 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cc(Cl)ccc3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL394139 148320 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 509 7 1 5 4.7 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cc(Cl)ccc3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
36811 1421 34 None -2 7 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
535 1421 34 None -2 7 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
937 1421 34 None -2 7 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
CHEMBL926 1421 34 None -2 7 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
DB00841 1421 34 None -2 7 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
44330880 206400 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 371 3 0 3 4.6 O=C1OC2(CCN(CCc3cccc4ccccc34)CC2)Cc2ccccc21 10.1016/s0960-894x(98)00732-x
CHEMBL98168 206400 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 371 3 0 3 4.6 O=C1OC2(CCN(CCc3cccc4ccccc34)CC2)Cc2ccccc21 10.1016/s0960-894x(98)00732-x
10132012 109244 0 None 7 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 339 4 2 3 3.3 CCS(=O)(=O)Nc1cc(Cl)cc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL323004 109244 0 None 7 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 339 4 2 3 3.3 CCS(=O)(=O)Nc1cc(Cl)cc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
136806214 206378 0 None 60 3 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 633 15 4 9 2.4 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(CN(C)C)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
44329028 206378 0 None 60 3 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 633 15 4 9 2.4 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(CN(C)C)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
CHEMBL98038 206378 0 None 60 3 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 633 15 4 9 2.4 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(CN(C)C)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
10916464 202443 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1cc(Cl)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70563 202443 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1cc(Cl)ccc1NCC1=NCCN1 10.1021/jm000542r
11312410 8799 0 None 9 3 Rat 6.3 pKi = 6.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 293 3 2 4 1.5 CS(=O)(=O)Nc1cccc2c1CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
CHEMBL109755 8799 0 None 9 3 Rat 6.3 pKi = 6.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 293 3 2 4 1.5 CS(=O)(=O)Nc1cccc2c1CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
11312410 8799 0 None 9 3 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 293 3 2 4 1.5 CS(=O)(=O)Nc1cccc2c1CCCC2C1=NCCN1 10.1021/jm030551a
CHEMBL109755 8799 0 None 9 3 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 293 3 2 4 1.5 CS(=O)(=O)Nc1cccc2c1CCCC2C1=NCCN1 10.1021/jm030551a
11511026 15845 0 None -75 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3ccc4ccccc4n3)CC2)c1Cl 10.1016/j.bmcl.2010.07.096
CHEMBL1223683 15845 0 None -75 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3ccc4ccccc4n3)CC2)c1Cl 10.1016/j.bmcl.2010.07.096
127024958 137107 0 None -3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 403 7 2 4 3.9 O=C(NCCCCN1CCN(c2ccccc2O)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
CHEMBL3758330 137107 0 None -3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 403 7 2 4 3.9 O=C(NCCCCN1CCN(c2ccccc2O)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
76326541 84903 0 None 28 4 Rat 7.3 pKi = 7.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCC[C@H]2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL2261355 84903 0 None 28 4 Rat 7.3 pKi = 7.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCC[C@H]2c1c[nH]cn1 10.1007/s00044-004-0020-z
53328311 63040 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 421 7 0 5 3.1 COc1ccccc1N1CCN(CCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796030 63040 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 421 7 0 5 3.1 COc1ccccc1N1CCN(CCCN2C(=O)CC(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
9926529 9284 2 None 1 5 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL111496 9284 2 None 1 5 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
10698608 43066 0 None 40 3 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 588 10 3 7 2.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(C(=O)N(C)C)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
CHEMBL150696 43066 0 None 40 3 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 588 10 3 7 2.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(C(=O)N(C)C)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
76318764 84391 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 359 8 1 6 2.8 COc1cccc(OC)c1OCCN[C@H]1COC[C@H](c2ccccc2)O1 10.1007/s00044-010-9379-1
CHEMBL2234454 84391 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 359 8 1 6 2.8 COc1cccc(OC)c1OCCN[C@H]1COC[C@H](c2ccccc2)O1 10.1007/s00044-010-9379-1
25131192 186732 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 373 9 1 6 2.8 COc1cccc(OC)c1OCCNC[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm800461k
CHEMBL493043 186732 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 373 9 1 6 2.8 COc1cccc(OC)c1OCCNC[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm800461k
213 3780 50 None -4 44 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3780 50 None -4 44 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3780 50 None -4 44 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3780 50 None -4 44 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3780 50 None -4 44 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
44288754 169938 0 None 36 3 Human 7.3 pKi = 7.3 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 453 9 1 6 3.4 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C(C)c2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL44496 169938 0 None 36 3 Human 7.3 pKi = 7.3 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 453 9 1 6 3.4 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C(C)c2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(00)00307-3
53328312 63041 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 425 6 0 4 3.8 O=C1CC(c2ccccc2)CC(=O)N1CCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796031 63041 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 425 6 0 4 3.8 O=C1CC(c2ccccc2)CC(=O)N1CCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.ejmech.2011.03.054
118567543 170792 0 None -4 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-prazosin from human alpha1A adrenoreceptor expressed in enriched membranes incubated for 90 mins by liquid scintillation counting methodDisplacement of [3H]-prazosin from human alpha1A adrenoreceptor expressed in enriched membranes incubated for 90 mins by liquid scintillation counting method
ChEMBL 463 4 0 4 4.2 O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2 10.1021/acs.jmedchem.9b01256
CHEMBL4461774 170792 0 None -4 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-prazosin from human alpha1A adrenoreceptor expressed in enriched membranes incubated for 90 mins by liquid scintillation counting methodDisplacement of [3H]-prazosin from human alpha1A adrenoreceptor expressed in enriched membranes incubated for 90 mins by liquid scintillation counting method
ChEMBL 463 4 0 4 4.2 O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2 10.1021/acs.jmedchem.9b01256
71450550 83379 0 None 1 16 Human 6.3 pKi = 6.3 Binding
Binding affinity to alpha1A adrenergicBinding affinity to alpha1A adrenergic
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 83379 0 None 1 16 Human 6.3 pKi = 6.3 Binding
Binding affinity to alpha1A adrenergicBinding affinity to alpha1A adrenergic
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
72457 101791 11 None -4 2 Human 5.3 pKi = 5.3 Binding
Compound was tested for its binding affinity towards Rat-1 cells stably expressing hamster alpha-1b adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards Rat-1 cells stably expressing hamster alpha-1b adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 342 3 4 3 4.0 O=C(c1nc(-c2c[nH]c3ccccc23)c[nH]1)c1c[nH]c2cc(O)ccc12 10.1016/0960-894X(96)00376-9
CHEMBL303282 101791 11 None -4 2 Human 5.3 pKi = 5.3 Binding
Compound was tested for its binding affinity towards Rat-1 cells stably expressing hamster alpha-1b adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards Rat-1 cells stably expressing hamster alpha-1b adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 342 3 4 3 4.0 O=C(c1nc(-c2c[nH]c3ccccc23)c[nH]1)c1c[nH]c2cc(O)ccc12 10.1016/0960-894X(96)00376-9
9814617 9229 0 None 2 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 293 3 2 4 1.7 CS(=O)(=O)Nc1cccc2c1OCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL111151 9229 0 None 2 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 293 3 2 4 1.7 CS(=O)(=O)Nc1cccc2c1OCCC2c1c[nH]cn1 10.1021/jm030551a
9958160 197166 0 None -31 4 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 515 4 0 4 3.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(I)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL58384 197166 0 None -31 4 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 515 4 0 4 3.8 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(I)ccc2Cl)CC1 10.1021/jm030944+
16041263 94990 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 470 6 2 4 5.4 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL257098 94990 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 470 6 2 4 5.4 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
53328506 63050 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 459 6 0 4 4.4 O=C1CC(c2ccc(Cl)cc2)CC(=O)N1CCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796040 63050 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 459 6 0 4 4.4 O=C1CC(c2ccc(Cl)cc2)CC(=O)N1CCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.ejmech.2011.03.054
44428850 91849 0 None -8 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 448 4 1 8 2.9 COc1cc2nc(N3CCN(C(=O)c4ccccn4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
CHEMBL242725 91849 0 None -8 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
ChEMBL 448 4 1 8 2.9 COc1cc2nc(N3CCN(C(=O)c4ccccn4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2007.01.028
46881444 7519 0 None -6 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 403 9 1 4 4.5 COc1ccccc1CCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
CHEMBL1088072 7519 0 None -6 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 403 9 1 4 4.5 COc1ccccc1CCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
118716703 114485 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 347 4 1 6 1.3 COc1ccccc1N1CCN(CC2COC3(CCNCC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342856 114485 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 347 4 1 6 1.3 COc1ccccc1N1CCN(CC2COC3(CCNCC3)O2)CC1 10.1016/j.ejmech.2014.09.070
44414173 12765 0 None -7 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 339 5 0 3 4.2 Cn1cc(C2CCN(CCCN3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2006.05.002
CHEMBL1188901 12765 0 None -7 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 339 5 0 3 4.2 Cn1cc(C2CCN(CCCN3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2006.05.002
CHEMBL537650 12765 0 None -7 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 339 5 0 3 4.2 Cn1cc(C2CCN(CCCN3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2006.05.002
21670271 64893 3 None - 1 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 174 1 0 2 1.8 CN1CC=C(c2cccnc2)CC1 10.1021/jm00375a017
CHEMBL18270 64893 3 None - 1 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 174 1 0 2 1.8 CN1CC=C(c2cccnc2)CC1 10.1021/jm00375a017
46846073 5708 0 None -223 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 451 9 1 4 5.6 c1ccc(-c2ccccc2OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.bmcl.2010.01.030
CHEMBL1078772 5708 0 None -223 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 451 9 1 4 5.6 c1ccc(-c2ccccc2OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.bmcl.2010.01.030
240 929 39 None -4 25 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 929 39 None -4 25 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 929 39 None -4 25 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 929 39 None -4 25 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 929 39 None -4 25 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 929 39 None -4 25 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 929 39 None -4 25 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
13298530 98602 18 None -97 2 Bovine 6.3 pKi = 6.3 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 195 1 0 3 1.0 CN1CCN(c2ncccc2F)CC1 10.1021/jm00366a007
CHEMBL280514 98602 18 None -97 2 Bovine 6.3 pKi = 6.3 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 195 1 0 3 1.0 CN1CCN(c2ncccc2F)CC1 10.1021/jm00366a007
6603710 123416 9 None - 1 Human 6.3 pKi = 6.3 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 345 5 2 3 3.9 CCS(=O)(=O)Nc1cccc(C(=C2CCCCC2)c2c[nH]cn2)c1 10.1016/j.bmcl.2004.11.032
CHEMBL362863 123416 9 None - 1 Human 6.3 pKi = 6.3 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 345 5 2 3 3.9 CCS(=O)(=O)Nc1cccc(C(=C2CCCCC2)c2c[nH]cn2)c1 10.1016/j.bmcl.2004.11.032
13298530 98602 18 None -97 2 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 195 1 0 3 1.0 CN1CCN(c2ncccc2F)CC1 10.1021/jm00375a017
CHEMBL280514 98602 18 None -97 2 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 195 1 0 3 1.0 CN1CCN(c2ncccc2F)CC1 10.1021/jm00375a017
4735 193435 92 None -77 10 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL361506 193435 92 None -77 10 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL55 193435 92 None -77 10 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
2419 687 22 None -288 12 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm030944+
9 687 22 None -288 12 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm030944+
CHEMBL13647 687 22 None -288 12 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm030944+
19085827 104371 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 485 7 0 8 2.9 COc1ccc2c(c1)oc(=O)n2C1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL311014 104371 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 485 7 0 8 2.9 COc1ccc2c(c1)oc(=O)n2C1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/s0960-894x(98)00446-6
44571938 179483 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 300 3 1 3 3.0 Fc1ccn(Cc2c(F)ccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
CHEMBL474796 179483 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 300 3 1 3 3.0 Fc1ccn(Cc2c(F)ccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
44431617 87900 0 None 3 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 458 7 1 6 3.3 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cccnc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234854 87900 0 None 3 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 458 7 1 6 3.3 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3cccnc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
44390740 122410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 478 7 3 7 0.9 C[C@@]1(O)C(=O)N(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)C(=O)N[C@@H]1O 10.1016/j.bmcl.2004.11.032
CHEMBL360688 122410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 478 7 3 7 0.9 C[C@@]1(O)C(=O)N(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)C(=O)N[C@@H]1O 10.1016/j.bmcl.2004.11.032
3033677 201246 33 None -25 9 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]-WB4101 from rat forebrain alpha 1 adrenergic receptorsDisplacement of [3H]-WB4101 from rat forebrain alpha 1 adrenergic receptors
ChEMBL 411 5 1 5 3.8 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=S)[nH]c3ccccc3c2=O)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL2355519 201246 33 None -25 9 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]-WB4101 from rat forebrain alpha 1 adrenergic receptorsDisplacement of [3H]-WB4101 from rat forebrain alpha 1 adrenergic receptors
ChEMBL 411 5 1 5 3.8 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=S)[nH]c3ccccc3c2=O)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL62919 201246 33 None -25 9 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]-WB4101 from rat forebrain alpha 1 adrenergic receptorsDisplacement of [3H]-WB4101 from rat forebrain alpha 1 adrenergic receptors
ChEMBL 411 5 1 5 3.8 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=S)[nH]c3ccccc3c2=O)CC1 10.1021/acs.jmedchem.2c00633
127025276 137189 0 None -3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 416 8 2 4 4.1 COc1ccccc1N1CCN(CCCCNC(=O)Nc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2015.12.068
CHEMBL3758991 137189 0 None -3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 416 8 2 4 4.1 COc1ccccc1N1CCN(CCCCNC(=O)Nc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2015.12.068
10579632 35342 0 None 5 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 611 9 2 7 5.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
CHEMBL143940 35342 0 None 5 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 611 9 2 7 5.3 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm990200p
52944674 16926 0 None 2 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 395 11 3 6 3.7 Oc1cccc(O)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1255085 16926 0 None 2 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 395 11 3 6 3.7 Oc1cccc(O)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
134150497 151548 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 324 6 0 3 3.8 CC(C)Oc1ccccc1N1CCN(CCc2ccccc2)CC1 10.1016/j.ejmech.2016.06.052
CHEMBL3967641 151548 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 minsDisplacement of [3H]prazosin from human alpha1A-adrenoceptor expressed in CHO cell membranes measured after 30 mins
ChEMBL 324 6 0 3 3.8 CC(C)Oc1ccccc1N1CCN(CCc2ccccc2)CC1 10.1016/j.ejmech.2016.06.052
44298780 194863 0 None 25 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 478 7 3 7 0.9 C[C@]1(O)C(=O)N(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)C(=O)N[C@H]1O 10.1016/s0960-894x(03)00305-6
CHEMBL56375 194863 0 None 25 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 478 7 3 7 0.9 C[C@]1(O)C(=O)N(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)C(=O)N[C@H]1O 10.1016/s0960-894x(03)00305-6
44329026 206673 0 None 19 6 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 679 16 3 7 6.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CCCCOC)N1 10.1016/s0960-894x(99)00484-9
CHEMBL99864 206673 0 None 19 6 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 679 16 3 7 6.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CCCCOC)N1 10.1016/s0960-894x(99)00484-9
16041264 94986 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 470 6 2 4 5.4 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL257077 94986 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 470 6 2 4 5.4 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
2894 206321 4 None -12 6 Bovine 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)C4CCCCC43)nc(N)c2cc1OC 10.1021/jm020938y
CHEMBL97698 206321 4 None -12 6 Bovine 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)C4CCCCC43)nc(N)c2cc1OC 10.1021/jm020938y
44288485 161958 0 None 29 3 Human 8.3 pKi = 8.3 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 498 9 1 4 5.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C(c2ccc(C)cc2)c2ccc(C)cc2)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL41677 161958 0 None 29 3 Human 8.3 pKi = 8.3 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 498 9 1 4 5.1 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C(c2ccc(C)cc2)c2ccc(C)cc2)CC1 10.1016/s0960-894x(00)00307-3
10746137 36708 0 None 138 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 599 9 2 7 3.9 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C#N)(c3ccccc3F)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL145134 36708 0 None 138 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 599 9 2 7 3.9 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(C#N)(c3ccccc3F)CC2)C(=O)N1 10.1021/jm990201h
90645595 111982 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 611 11 2 8 5.1 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298748 111982 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 611 11 2 8 5.1 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
118716717 114500 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 532 7 0 9 2.3 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4ccc([N+](=O)[O-])cc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342870 114500 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 532 7 0 9 2.3 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4ccc([N+](=O)[O-])cc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
44404321 69934 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 297 4 1 5 3.0 COc1cccc(N(NC2=NCCO2)c2ccc(C)cc2)c1 10.1016/j.bmcl.2005.07.083
CHEMBL194323 69934 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 297 4 1 5 3.0 COc1cccc(N(NC2=NCCO2)c2ccc(C)cc2)c1 10.1016/j.bmcl.2005.07.083
44404326 132988 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 283 3 2 5 2.7 Cc1ccc(N(NC2=NCCO2)c2cccc(O)c2)cc1 10.1016/j.bmcl.2005.07.083
CHEMBL370818 132988 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
ChEMBL 283 3 2 5 2.7 Cc1ccc(N(NC2=NCCO2)c2cccc(O)c2)cc1 10.1016/j.bmcl.2005.07.083
44447018 94410 0 None -131 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 496 7 1 5 5.0 O=C(Cc1ccccc1)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
CHEMBL253878 94410 0 None -131 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 496 7 1 5 5.0 O=C(Cc1ccccc1)NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21 10.1016/j.bmcl.2007.11.106
44288468 167806 0 None 1 3 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1cccc2c1C1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC1CC2 10.1021/jm990567u
CHEMBL434591 167806 0 None 1 3 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1cccc2c1C1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC1CC2 10.1021/jm990567u
16041630 97085 0 None -2 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(F)cccc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL270589 97085 0 None -2 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(F)cccc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
44289525 165431 0 None -5 9 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampus (+ 10 uM) CES membrane using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampus (+ 10 uM) CES membrane using [3H]prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNCC1Oc2ccccc2OC1c1ccc(C)cc1 10.1021/jm960069a
CHEMBL42539 165431 0 None -5 9 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampus (+ 10 uM) CES membrane using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampus (+ 10 uM) CES membrane using [3H]prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNCC1Oc2ccccc2OC1c1ccc(C)cc1 10.1021/jm960069a
44426405 141509 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 562 9 1 5 5.7 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1ccc(OC(F)F)cc1 10.1016/j.bmcl.2007.04.098
CHEMBL387832 141509 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 562 9 1 5 5.7 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1ccc(OC(F)F)cc1 10.1016/j.bmcl.2007.04.098
10746433 120557 0 None 295 3 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 619 13 3 9 3.0 COCCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
CHEMBL357061 120557 0 None 295 3 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 619 13 3 9 3.0 COCCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
69781970 160792 0 None -14 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 477 5 1 8 4.0 COc1cc2nc(N3CCN(C(=O)OCc4ccccc4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4125981 160792 0 None -14 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 477 5 1 8 4.0 COc1cc2nc(N3CCN(C(=O)OCc4ccccc4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
132266 1247 9 None -48 9 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm8016046
486 1247 9 None -48 9 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm8016046
CHEMBL423294 1247 9 None -48 9 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm8016046
180 397 50 None -10 39 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -10 39 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -10 39 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -10 39 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -10 39 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
44431554 87901 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234874 87901 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
44431547 154055 0 None -2 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccccc3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL399195 154055 0 None -2 4 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 475 7 1 5 4.0 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccccc3F)CC2)CC1 10.1016/j.bmcl.2007.04.008
11994667 11711 0 None 1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1ccc(-c2ccccc2)cc1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182143 11711 0 None 1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1ccc(-c2ccccc2)cc1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL214694 11711 0 None 1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1ccc(-c2ccccc2)cc1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
71458492 84132 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153556 84132 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220896 84132 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
44447012 94345 0 None -56 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 516 6 1 5 5.7 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1ccc(Cl)cc1 10.1016/j.bmcl.2007.11.106
CHEMBL253439 94345 0 None -56 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
ChEMBL 516 6 1 5 5.7 O=C(NC1CCc2ccc(CCN3CCN(c4nsc5ccccc45)CC3)cc21)c1ccc(Cl)cc1 10.1016/j.bmcl.2007.11.106
10575494 165183 0 None -1 3 Rat 8.3 pKi = 8.3 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 449 7 1 8 2.5 COc1cc2nc(N3CCN(C(=O)CCC(=O)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL424658 165183 0 None -1 3 Rat 8.3 pKi = 8.3 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 449 7 1 8 2.5 COc1cc2nc(N3CCN(C(=O)CCC(=O)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
44301681 200997 0 None 309 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 481 8 2 4 4.6 Cc1ccc(C(O)(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(01)00320-1
CHEMBL61643 200997 0 None 309 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 481 8 2 4 4.6 Cc1ccc(C(O)(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(01)00320-1
145953314 160870 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 441 7 1 7 3.8 CCCCCC(=O)N1CCN(c2nc(N)c3cc(OC)c(OC)cc3n2)[C@@H]2CCCC[C@@H]21 10.1016/j.bmc.2018.05.023
CHEMBL4127078 160870 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 441 7 1 7 3.8 CCCCCC(=O)N1CCN(c2nc(N)c3cc(OC)c(OC)cc3n2)[C@@H]2CCCC[C@@H]21 10.1016/j.bmc.2018.05.023
10895039 18319 0 None -11 8 Rat 8.2 pKi = 8.2 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
CHEMBL127400 18319 0 None -11 8 Rat 8.2 pKi = 8.2 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
CHEMBL129022 18319 0 None -11 8 Rat 8.2 pKi = 8.2 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
44431617 144356 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 458 7 1 6 3.3 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3cccnc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL391016 144356 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 458 7 1 6 3.3 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3cccnc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
44295044 101096 0 None 169 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 535 6 2 6 3.5 N#CC1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
CHEMBL298579 101096 0 None 169 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 535 6 2 6 3.5 N#CC1(c2ccccc2)CCN(CCCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
4418 33985 80 None -1 7 Human 8.2 pKi = 8.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1007/s00044-010-9379-1
CHEMBL142635 33985 80 None -1 7 Human 8.2 pKi = 8.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1007/s00044-010-9379-1
4418 33985 80 None -1 7 Human 8.2 pKi = 8.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1007/s00044-010-9379-1
CHEMBL142635 33985 80 None -1 7 Human 8.2 pKi = 8.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1007/s00044-010-9379-1
10793963 99198 0 None 9 6 Human 8.2 pKi = 8.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 622 11 2 7 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm960697s
CHEMBL284470 99198 0 None 9 6 Human 8.2 pKi = 8.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 622 11 2 7 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm960697s
10032383 109608 0 None 194 6 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
136680387 109608 0 None 194 6 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
CHEMBL323579 109608 0 None 194 6 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
11857793 85209 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 548 7 1 4 5.9 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1cc(Cl)ccc1F 10.1016/j.bmcl.2007.04.098
CHEMBL228445 85209 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 548 7 1 4 5.9 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1cc(Cl)ccc1F 10.1016/j.bmcl.2007.04.098
10743042 187559 0 None 2 4 Human 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 471 5 1 8 3.1 Cn1nc(Cl)c2cn3nc(NCCN4CCN(c5ccccc5Cl)CC4)ccc3c2c1=O 10.1021/jm981006q
CHEMBL49851 187559 0 None 2 4 Human 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cellsThe compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 471 5 1 8 3.1 Cn1nc(Cl)c2cn3nc(NCCN4CCN(c5ccccc5Cl)CC4)ccc3c2c1=O 10.1021/jm981006q
10651706 120987 0 None 25 3 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 637 11 3 8 4.5 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(C(=O)Oc3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
CHEMBL358406 120987 0 None 25 3 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 637 11 3 8 4.5 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(C(=O)Oc3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
144096985 163531 0 None -5 3 Human 7.3 pKi = 7.3 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 385 9 1 4 3.5 CS(=O)(=O)c1ccccc1CCCNCCOc1cc(F)ccc1Cl 10.1016/j.ejmech.2017.07.071
CHEMBL4209590 163531 0 None -5 3 Human 7.3 pKi = 7.3 Binding
Displacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting methodDisplacement of 7-methoxy-[3H]-prazosin from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes after 60 mins by TopCount liquid scintillation counting method
ChEMBL 385 9 1 4 3.5 CS(=O)(=O)c1ccccc1CCCNCCOc1cc(F)ccc1Cl 10.1016/j.ejmech.2017.07.071
9841781 122531 0 None -13 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 359 5 1 2 4.8 c1ccc2c(c1)CN(CCCN1CCC(c3c[nH]c4ccccc34)CC1)C2 10.1016/j.bmcl.2015.07.046
CHEMBL3609357 122531 0 None -13 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 359 5 1 2 4.8 c1ccc2c(c1)CN(CCCN1CCC(c3c[nH]c4ccccc34)CC1)C2 10.1016/j.bmcl.2015.07.046
44288794 161515 0 None 39 3 Human 7.3 pKi = 7.3 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 429 8 1 3 5.0 N#CC1(c2ccccc2)CCN(CCCNC(=O)C(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL416073 161515 0 None 39 3 Human 7.3 pKi = 7.3 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 429 8 1 3 5.0 N#CC1(c2ccccc2)CCN(CCCNC(=O)C(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(00)00307-3
10026936 162894 0 None 114 3 Human 7.3 pKi = 7.3 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 453 8 1 3 5.1 Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2ccc(F)c(F)c2)C(C)C)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL41994 162894 0 None 114 3 Human 7.3 pKi = 7.3 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 453 8 1 3 5.1 Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2ccc(F)c(F)c2)C(C)C)CC1 10.1016/s0960-894x(00)00307-3
2267 553 64 None -15 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
271 553 64 None -15 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
7121 553 64 None -15 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
CHEMBL639 553 64 None -15 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
DB00972 553 64 None -15 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
52937728 60966 0 None -100 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 351 4 0 4 3.2 CN1CCC[C@@H]1Cn1nc(Cc2cccc(F)c2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767145 60966 0 None -100 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 351 4 0 4 3.2 CN1CCC[C@@H]1Cn1nc(Cc2cccc(F)c2)c2ccccc2c1=O 10.1021/jm1013874
155565449 175747 0 None -3 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 433 11 1 5 4.6 COc1ccccc1OCCNCC[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4579802 175747 0 None -3 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 433 11 1 5 4.6 COc1ccccc1OCCNCC[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4595447 175747 0 None -3 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 433 11 1 5 4.6 COc1ccccc1OCCNCC[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
2267 553 64 None -15 7 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
271 553 64 None -15 7 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
7121 553 64 None -15 7 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
CHEMBL639 553 64 None -15 7 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
DB00972 553 64 None -15 7 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
19608536 137244 0 None -10 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
CHEMBL3759513 137244 0 None -10 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2015.12.068
12575 1949 28 None -331 17 Bovine 6.3 pKi = 6.3 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm00366a007
54459 1949 28 None -331 17 Bovine 6.3 pKi = 6.3 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm00366a007
CHEMBL10316 1949 28 None -331 17 Bovine 6.3 pKi = 6.3 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm00366a007
506 2212 32 None -97 6 Rat 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
6603904 2212 32 None -97 6 Rat 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
CHEMBL19476 2212 32 None -97 6 Rat 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1 10.1021/jm980053f
102 4051 44 None -1258 50 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
3659 4051 44 None -1258 50 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969 4051 44 None -1258 50 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
CHEMBL15245 4051 44 None -1258 50 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
DB01392 4051 44 None -1258 50 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
10792152 205213 0 None - 1 Human 6.3 pKi = 6.3 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 523 7 3 4 3.9 O=C1NC(C(F)(F)F)=C(C(=O)NCCCN2CCC(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1021/jm990612y
CHEMBL91179 205213 0 None - 1 Human 6.3 pKi = 6.3 Binding
Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.
ChEMBL 523 7 3 4 3.9 O=C1NC(C(F)(F)F)=C(C(=O)NCCCN2CCC(c3ccccn3)CC2)[C@@H](c2ccc(F)c(F)c2)N1 10.1021/jm990612y
75306277 108754 0 None -251 23 Human 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 108754 0 None -251 23 Human 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
52937731 60969 0 None -630 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 347 4 0 4 3.4 Cc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1 10.1021/jm1013874
CHEMBL1767148 60969 0 None -630 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 347 4 0 4 3.4 Cc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1 10.1021/jm1013874
52937829 60974 0 None -316 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 313 6 0 4 3.2 CCCCCc1nn(C[C@H]2CCCN2C)c(=O)c2ccccc12 10.1021/jm1013874
CHEMBL1767153 60974 0 None -316 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 313 6 0 4 3.2 CCCCCc1nn(C[C@H]2CCCN2C)c(=O)c2ccccc12 10.1021/jm1013874
11736917 9172 2 None 1 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 254 4 2 3 1.5 CCS(=O)(=O)Nc1cccc(C2CCNC2)c1 10.1021/jm030551a
CHEMBL110859 9172 2 None 1 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 254 4 2 3 1.5 CCS(=O)(=O)Nc1cccc(C2CCNC2)c1 10.1021/jm030551a
9880162 9197 0 None -1 3 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 321 4 2 4 2.3 COc1ccc2c(c1NS(C)(=O)=O)CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL110976 9197 0 None -1 3 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 321 4 2 4 2.3 COc1ccc2c(c1NS(C)(=O)=O)CCCC2c1c[nH]cn1 10.1021/jm030551a
9823115 196916 0 None -2511 5 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 414 4 0 5 3.0 N#Cc1ccc(Cl)cc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
CHEMBL57868 196916 0 None -2511 5 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 414 4 0 5 3.0 N#Cc1ccc(Cl)cc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
16041449 94763 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 538 6 2 4 6.7 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(Cl)cc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL256040 94763 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 538 6 2 4 6.7 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(Cl)cc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
16041092 94923 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccc(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL256804 94923 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3ccc(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
9820229 122530 0 None -6 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 359 5 1 2 4.8 c1ccc2c(c1)CCN2CCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2015.07.046
CHEMBL3609356 122530 0 None -6 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 359 5 1 2 4.8 c1ccc2c(c1)CCN2CCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2015.07.046
10739024 69475 0 None -20 6 Rat 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 388 4 3 8 0.9 COc1cc2nc(N3CCN[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
CHEMBL19376 69475 0 None -20 6 Rat 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 388 4 3 8 0.9 COc1cc2nc(N3CCN[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
10961938 119021 0 None -8511 8 Rat 5.3 pKi = 5.3 Binding
Binding affinity for rat Alpha-1A adrenergic receptor using [11C] radiotracerBinding affinity for rat Alpha-1A adrenergic receptor using [11C] radiotracer
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm050171k
CHEMBL345820 119021 0 None -8511 8 Rat 5.3 pKi = 5.3 Binding
Binding affinity for rat Alpha-1A adrenergic receptor using [11C] radiotracerBinding affinity for rat Alpha-1A adrenergic receptor using [11C] radiotracer
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm050171k
76322413 84389 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 359 8 1 6 2.8 COc1cccc(OC)c1OCCN[C@H]1CO[C@H](c2ccccc2)CO1 10.1007/s00044-010-9379-1
CHEMBL2234452 84389 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 359 8 1 6 2.8 COc1cccc(OC)c1OCCN[C@H]1CO[C@H](c2ccccc2)CO1 10.1007/s00044-010-9379-1
2803 939 53 None -8 19 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
516 939 53 None -8 19 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
704 939 53 None -8 19 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
CHEMBL134 939 53 None -8 19 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
DB00575 939 53 None -8 19 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
25132564 186809 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 373 9 1 6 2.8 COc1cccc(OC)c1OCCNC[C@@H]1CO[C@@H](c2ccccc2)CO1 10.1021/jm800461k
CHEMBL493661 186809 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 373 9 1 6 2.8 COc1cccc(OC)c1OCCNC[C@@H]1CO[C@@H](c2ccccc2)CO1 10.1021/jm800461k
3086326 202816 17 None -138 6 Human 5.3 pKi = 5.3 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 247 1 2 5 1.7 Clc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL72753 202816 17 None -138 6 Human 5.3 pKi = 5.3 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 247 1 2 5 1.7 Clc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
16041630 97085 0 None -2 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(F)cccc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL270589 97085 0 None -2 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 472 6 2 4 5.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(F)cccc3F)CC2)CC1 10.1016/j.bmcl.2007.11.068
49783209 17412 0 None -912 27 Human 6.3 pKi = 6.3 Binding
Binding affinity to human adrenergic alpha1A receptorBinding affinity to human adrenergic alpha1A receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17412 0 None -912 27 Human 6.3 pKi = 6.3 Binding
Binding affinity to human adrenergic alpha1A receptorBinding affinity to human adrenergic alpha1A receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
127036932 136811 0 None -17 22 Human 6.3 pKi = 6.3 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 136811 0 None -17 22 Human 6.3 pKi = 6.3 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
9813756 8913 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 255 2 2 2 2.8 CC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL109848 8913 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 255 2 2 2 2.8 CC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
9813756 8913 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 255 2 2 2 2.8 CC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL109848 8913 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 255 2 2 2 2.8 CC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
15546405 96697 0 None 12 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 416 8 0 5 2.1 CC(C)Oc1ccccc1N1CCN(CCN(C)C(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL268030 96697 0 None 12 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 416 8 0 5 2.1 CC(C)Oc1ccccc1N1CCN(CCN(C)C(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
44331277 4394 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 371 3 0 3 4.9 O=C1CC2(CCN(CCc3cccc4ccccc34)CC2)Oc2ccccc21 10.1016/s0960-894x(98)00732-x
CHEMBL101869 4394 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 371 3 0 3 4.9 O=C1CC2(CCN(CCc3cccc4ccccc34)CC2)Oc2ccccc21 10.1016/s0960-894x(98)00732-x
9800400 122528 1 None -7 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 387 5 1 3 4.0 O=C1c2ccccc2C(=O)N1CCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2015.07.046
CHEMBL3609354 122528 1 None -7 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 387 5 1 3 4.0 O=C1c2ccccc2C(=O)N1CCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2015.07.046
10818003 105927 0 None 3 6 Human 7.3 pKi = 7.3 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 649 12 3 6 6.2 CC(C)C1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C(C)C)N1 10.1021/jm980077m
CHEMBL313953 105927 0 None 3 6 Human 7.3 pKi = 7.3 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 649 12 3 6 6.2 CC(C)C1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C(C)C)N1 10.1021/jm980077m
10818003 105927 0 None 3 6 Human 7.3 pKi = 7.3 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 649 12 3 6 6.2 CC(C)C1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C(C)C)N1 10.1007/s00044-004-0120-9
CHEMBL313953 105927 0 None 3 6 Human 7.3 pKi = 7.3 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 649 12 3 6 6.2 CC(C)C1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C(C)C)N1 10.1007/s00044-004-0120-9
44420412 84358 0 None -3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 470 5 1 7 3.4 COc1ccc(Cl)cc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
CHEMBL223289 84358 0 None -3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 470 5 1 7 3.4 COc1ccc(Cl)cc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
14925759 157482 6 None -18 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 157482 6 None -18 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
56946472 71152 0 None -26 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 373 8 1 3 4.8 c1ccc(OCCNCC2CCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm200421e
CHEMBL1946778 71152 0 None -26 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 373 8 1 3 4.8 c1ccc(OCCNCC2CCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm200421e
CHEMBL1962753 71152 0 None -26 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 373 8 1 3 4.8 c1ccc(OCCNCC2CCC(c3ccccc3)(c3ccccc3)O2)cc1 10.1021/jm200421e
11372228 101184 0 None -64 5 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 373 4 0 3 3.8 O=C1CC2(C=CN1CCN1CCN(c3ccccc3Cl)CC1)CCCC2 10.1021/jm030944+
CHEMBL299253 101184 0 None -64 5 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 373 4 0 3 3.8 O=C1CC2(C=CN1CCN1CCN(c3ccccc3Cl)CC1)CCCC2 10.1021/jm030944+
11771731 107747 2 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL319706 107747 2 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)Displacement of [3H]prazosin from alpha-1A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
9947861 202452 0 None 4 4 Human 6.3 pKi = 6.3 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70634 202452 0 None 4 4 Human 6.3 pKi = 6.3 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
76311539 84394 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 299 6 1 4 2.8 c1ccc(OCCN[C@H]2CO[C@H](c3ccccc3)CO2)cc1 10.1007/s00044-010-9379-1
CHEMBL2234457 84394 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 299 6 1 4 2.8 c1ccc(OCCN[C@H]2CO[C@H](c3ccccc3)CO2)cc1 10.1007/s00044-010-9379-1
10267873 110158 0 None 5 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 317 4 2 3 2.8 O=S(=O)(Nc1cccc2c1CCCC2c1c[nH]cn1)C1CC1 10.1007/s00044-004-0020-z
CHEMBL325897 110158 0 None 5 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 317 4 2 3 2.8 O=S(=O)(Nc1cccc2c1CCCC2c1c[nH]cn1)C1CC1 10.1007/s00044-004-0020-z
14004035 119001 0 None 1 2 Bovine 6.3 pKi = 6.3 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 227 0 1 2 2.6 c1cnc2[nH]c3c(c2c1)CCN1CCCCC31 10.1021/jm00398a025
CHEMBL345621 119001 0 None 1 2 Bovine 6.3 pKi = 6.3 Binding
Compound was evaluated for log 1/Ki at alpha-1 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-1 adrenergic receptor
ChEMBL 227 0 1 2 2.6 c1cnc2[nH]c3c(c2c1)CCN1CCCCC31 10.1021/jm00398a025
25131196 192021 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 313 7 1 4 2.8 c1ccc(OCCNC[C@@H]2CO[C@@H](c3ccccc3)CO2)cc1 10.1021/jm800461k
CHEMBL521694 192021 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 313 7 1 4 2.8 c1ccc(OCCNC[C@@H]2CO[C@@H](c3ccccc3)CO2)cc1 10.1021/jm800461k
10267873 110158 0 None 5 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 317 4 2 3 2.8 O=S(=O)(Nc1cccc2c1CCCC2c1c[nH]cn1)C1CC1 10.1021/jm030551a
CHEMBL325897 110158 0 None 5 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 317 4 2 3 2.8 O=S(=O)(Nc1cccc2c1CCCC2c1c[nH]cn1)C1CC1 10.1021/jm030551a
441383 20118 54 None -257 17 Rat 5.3 pKi = 5.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 20118 54 None -257 17 Rat 5.3 pKi = 5.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
11505007 89819 0 None -6 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 557 9 1 7 4.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL238402 89819 0 None -6 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 557 9 1 7 4.1 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCN(c4ccccc4OCC(F)(F)F)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
11303253 196910 0 None -147 4 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 371 5 0 4 3.0 COc1ccccc1N1CCN(CCN2CCC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
CHEMBL57859 196910 0 None -147 4 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 371 5 0 4 3.0 COc1ccccc1N1CCN(CCN2CCC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
9909471 195221 0 None -17 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 409 4 0 4 3.4 O=C1CC2(CCCC2)C(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL56620 195221 0 None -17 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 409 4 0 4 3.4 O=C1CC2(CCCC2)C(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
9909471 195221 0 None -17 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 409 4 0 4 3.4 O=C1CC2(CCCC2)C(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL56620 195221 0 None -17 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 409 4 0 4 3.4 O=C1CC2(CCCC2)C(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1007/s00044-010-9379-1
14004035 119001 0 None 1 2 Bovine 6.3 pKi = 6.3 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 227 0 1 2 2.6 c1cnc2[nH]c3c(c2c1)CCN1CCCCC31 10.1021/jm00398a025
CHEMBL345621 119001 0 None 1 2 Bovine 6.3 pKi = 6.3 Binding
Affinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranesAffinity to alpha-1 adrenergic receptor by the displacement of [3H]-prazosin from calf cerebral cortex membranes
ChEMBL 227 0 1 2 2.6 c1cnc2[nH]c3c(c2c1)CCN1CCCCC31 10.1021/jm00398a025
1343 1850 55 None -87 9 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
3519 1850 55 None -87 9 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
522 1850 55 None -87 9 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL862 1850 55 None -87 9 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
DB01018 1850 55 None -87 9 Rat 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
10411237 116966 0 None -3019 4 Rat 6.3 pKi = 6.3 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0211220
CHEMBL339960 116966 0 None -3019 4 Rat 6.3 pKi = 6.3 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0211220
CHEMBL4287055 116966 0 None -3019 4 Rat 6.3 pKi = 6.3 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0211220
11090351 162827 0 None -2 4 Human 6.3 pKi = 6.3 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL419448 162827 0 None -2 4 Human 6.3 pKi = 6.3 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
76330200 84902 0 None 2 3 Rat 5.3 pKi = 5.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 323 3 2 5 1.2 CN(c1c(O)ccc2c1CCCC2C1=NCCN1)S(C)(=O)=O 10.1007/s00044-004-0020-z
CHEMBL2261354 84902 0 None 2 3 Rat 5.3 pKi = 5.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 323 3 2 5 1.2 CN(c1c(O)ccc2c1CCCC2C1=NCCN1)S(C)(=O)=O 10.1007/s00044-004-0020-z
135423051 77464 0 None 2 3 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(C[C@@H]2CN=C3c4ccccc4NC(=O)N32)CC1 10.1021/jm970159v
CHEMBL2092926 77464 0 None 2 3 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranesDisplacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(C[C@@H]2CN=C3c4ccccc4NC(=O)N32)CC1 10.1021/jm970159v
456386 201305 5 None -3 2 Human 6.3 pKi = 6.3 Binding
Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 376 2 3 1 5.5 Brc1ccc2c(-c3c[nH]c(-c4c[nH]c5ccccc45)n3)c[nH]c2c1 10.1016/0960-894X(96)00376-9
CHEMBL63208 201305 5 None -3 2 Human 6.3 pKi = 6.3 Binding
Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 376 2 3 1 5.5 Brc1ccc2c(-c3c[nH]c(-c4c[nH]c5ccccc45)n3)c[nH]c2c1 10.1016/0960-894X(96)00376-9
44300018 196606 0 None -660 4 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 389 4 0 4 3.2 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2Cl)CC1 10.1021/jm030944+
CHEMBL57593 196606 0 None -660 4 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 389 4 0 4 3.2 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2Cl)CC1 10.1021/jm030944+
44331198 4378 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 357 3 0 2 5.2 c1ccc2c(c1)CCC1(CCN(CCc3cccc4ccccc34)CC1)O2 10.1016/s0960-894x(98)00732-x
CHEMBL101739 4378 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 357 3 0 2 5.2 c1ccc2c(c1)CCC1(CCN(CCc3cccc4ccccc34)CC1)O2 10.1016/s0960-894x(98)00732-x
9797995 13819 0 None -51 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 339 6 1 2 4.6 c1ccc2c(C3CCN(CCCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
CHEMBL1196601 13819 0 None -51 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 339 6 1 2 4.6 c1ccc2c(C3CCN(CCCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
CHEMBL557584 13819 0 None -51 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 339 6 1 2 4.6 c1ccc2c(C3CCN(CCCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
10626982 110994 0 None 2 6 Human 7.3 pKi = 7.3 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 575 9 2 6 5.9 CC1=C(C#N)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL327775 110994 0 None 2 6 Human 7.3 pKi = 7.3 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 575 9 2 6 5.9 CC1=C(C#N)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
10626982 110994 0 None 2 6 Human 7.3 pKi = 7.3 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 575 9 2 6 5.9 CC1=C(C#N)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
CHEMBL327775 110994 0 None 2 6 Human 7.3 pKi = 7.3 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 575 9 2 6 5.9 CC1=C(C#N)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
52941981 17319 0 None -2 3 Rat 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 502 7 1 5 3.1 CN1C(=O)N(CC(O)CN2CCN(c3ccccc3F)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
CHEMBL1257883 17319 0 None -2 3 Rat 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 502 7 1 5 3.1 CN1C(=O)N(CC(O)CN2CCN(c3ccccc3F)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.bmcl.2010.07.101
44314198 103920 0 None -95 4 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCCC1NC1=NCCO1 10.1016/0960-894X(94)85032-1
CHEMBL310335 103920 0 None -95 4 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCCC1NC1=NCCO1 10.1016/0960-894X(94)85032-1
1201549 590 22 None -51 20 Rat 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 590 22 None -51 20 Rat 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 590 22 None -51 20 Rat 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 590 22 None -51 20 Rat 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 590 22 None -51 20 Rat 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 590 22 None -51 20 Rat 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
18001206 12662 0 None -4 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 327 5 0 4 3.9 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)noc2c1 10.1016/j.bmcl.2006.05.002
CHEMBL1188049 12662 0 None -4 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 327 5 0 4 3.9 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)noc2c1 10.1016/j.bmcl.2006.05.002
CHEMBL534943 12662 0 None -4 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 327 5 0 4 3.9 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)noc2c1 10.1016/j.bmcl.2006.05.002
9798656 12766 0 None -38 3 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 353 7 1 2 5.0 c1ccc2c(C3CCN(CCCCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
CHEMBL1188902 12766 0 None -38 3 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 353 7 1 2 5.0 c1ccc2c(C3CCN(CCCCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
CHEMBL537651 12766 0 None -38 3 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 353 7 1 2 5.0 c1ccc2c(C3CCN(CCCCCN4CCCCC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.05.002
10859076 13555 0 None 1 6 Human 7.2 pKi = 7.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1194763 13555 0 None 1 6 Human 7.2 pKi = 7.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL553276 13555 0 None 1 6 Human 7.2 pKi = 7.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
134137025 142194 0 None -11 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 362 4 0 5 3.6 COc1ccccc1N1CCN(CC2CSC3(CCCCC3)O2)CC1 10.1016/j.ejmech.2016.09.050
CHEMBL3892434 142194 0 None -11 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 362 4 0 5 3.6 COc1ccccc1N1CCN(CC2CSC3(CCCCC3)O2)CC1 10.1016/j.ejmech.2016.09.050
44288810 168884 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 483 9 2 3 4.5 Cc1ccc(C(C(=O)NCCCN2CCC(C(N)=O)(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
CHEMBL44288 168884 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 483 9 2 3 4.5 Cc1ccc(C(C(=O)NCCCN2CCC(C(N)=O)(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
12134994 162744 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 316 5 0 5 2.9 COc1ccccc1N1CCN(Cc2ccc(C=O)s2)CC1 10.1016/s0960-894x(02)00347-5
CHEMBL418882 162744 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
ChEMBL 316 5 0 5 2.9 COc1ccccc1N1CCN(Cc2ccc(C=O)s2)CC1 10.1016/s0960-894x(02)00347-5
6075 149563 36 None -11 16 Rat 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 149563 36 None -11 16 Rat 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
11568725 15907 0 None -104 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 454 8 1 4 6.1 Clc1cccc(N2CCN(CCCCNc3cc(-c4ccccc4)ccn3)CC2)c1Cl 10.1016/j.bmcl.2010.07.096
CHEMBL1223856 15907 0 None -104 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 454 8 1 4 6.1 Clc1cccc(N2CCN(CCCCNc3cc(-c4ccccc4)ccn3)CC2)c1Cl 10.1016/j.bmcl.2010.07.096
44362633 121020 0 None 95 3 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 597 9 3 6 3.9 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCC(C)N2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL358590 121020 0 None 95 3 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 597 9 3 6 3.9 CCC1=C(C(N)=O)C(c2ccc(F)c(F)c2)N(C(=O)NCCC(C)N2CCC(C(=O)OC)(c3ccccc3)CC2)C(=O)N1 10.1021/jm990201h
10946567 16277 0 None -47 6 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 265 1 0 2 4.1 CCc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
CHEMBL123448 16277 0 None -47 6 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cellsInhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
ChEMBL 265 1 0 2 4.1 CCc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
10508132 106521 0 None 13 6 Human 7.2 pKi = 7.2 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 621 10 2 6 5.5 CC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)N(C)C)=C(C)N1 10.1021/jm980077m
CHEMBL315392 106521 0 None 13 6 Human 7.2 pKi = 7.2 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 621 10 2 6 5.5 CC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)N(C)C)=C(C)N1 10.1021/jm980077m
10769499 43950 0 None 489 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 576 10 3 8 3.6 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
CHEMBL151668 43950 0 None 489 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 576 10 3 8 3.6 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
10508132 106521 0 None 13 6 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 621 10 2 6 5.5 CC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)N(C)C)=C(C)N1 10.1007/s00044-004-0120-9
CHEMBL315392 106521 0 None 13 6 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 621 10 2 6 5.5 CC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)N(C)C)=C(C)N1 10.1007/s00044-004-0120-9
155542075 176035 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 9 1 4 4.4 c1ccc(OCCNCCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4520390 176035 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 9 1 4 4.4 c1ccc(OCCNCCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4597826 176035 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 389 9 1 4 4.4 c1ccc(OCCNCCC2COC(c3ccccc3)(c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
9934955 71917 0 None -165 6 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 482 5 2 9 2.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
CHEMBL19826 71917 0 None -165 6 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 482 5 2 9 2.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
23290944 81400 0 None -389 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand binding assayBinding affinity to adrenergic alpha1A receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164350 81400 0 None -389 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand binding assayBinding affinity to adrenergic alpha1A receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
11474152 100141 0 None -275 4 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 369 4 0 4 2.8 Cc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
CHEMBL291908 100141 0 None -275 4 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 369 4 0 4 2.8 Cc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1 10.1021/jm030944+
9816461 10604 6 None 2 4 Human 6.2 pKi = 6.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117094 10604 6 None 2 4 Human 6.2 pKi = 6.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL544290 10604 6 None 2 4 Human 6.2 pKi = 6.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
11034737 202813 0 None -2 6 Human 6.2 pKi = 6.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72724 202813 0 None -2 6 Human 6.2 pKi = 6.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
10769499 43950 0 None 489 3 Human 7.2 pKi = 7.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 576 10 3 8 3.6 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
CHEMBL151668 43950 0 None 489 3 Human 7.2 pKi = 7.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 576 10 3 8 3.6 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)O)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
44390756 63511 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 445 10 0 7 2.1 CCOC(=O)C1CCC(=O)N1CC(=O)CCN1CCN(c2ccccc2OC(C)C)CC1 10.1016/j.bmcl.2004.11.032
CHEMBL180312 63511 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 445 10 0 7 2.1 CCOC(=O)C1CCC(=O)N1CC(=O)CCN1CCN(c2ccccc2OC(C)C)CC1 10.1016/j.bmcl.2004.11.032
9822942 196250 0 None -48 4 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 411 5 0 4 3.7 CCC1(C)CC(=O)N(CCN2CCN(c3cc(Cl)ccc3Cl)CC2)C(=O)C1 10.1021/jm030944+
CHEMBL57317 196250 0 None -48 4 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 411 5 0 4 3.7 CCC1(C)CC(=O)N(CCN2CCN(c3cc(Cl)ccc3Cl)CC2)C(=O)C1 10.1021/jm030944+
9845181 206410 1 None -4168 15 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
CHEMBL98241 206410 1 None -4168 15 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
49865601 15831 0 None -34 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 378 7 1 4 4.1 FC(F)(F)c1cccc(N2CCN(CCCCNc3ccccn3)CC2)c1 10.1016/j.bmcl.2010.07.096
CHEMBL1223617 15831 0 None -34 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 378 7 1 4 4.1 FC(F)(F)c1cccc(N2CCN(CCCCNc3ccccn3)CC2)c1 10.1016/j.bmcl.2010.07.096
2865 4064 67 None -14 54 Human 8.2 pKi = 8.2 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 nan
59 4064 67 None -14 54 Human 8.2 pKi = 8.2 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 nan
60854 4064 67 None -14 54 Human 8.2 pKi = 8.2 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 nan
CHEMBL708 4064 67 None -14 54 Human 8.2 pKi = 8.2 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 nan
DB00246 4064 67 None -14 54 Human 8.2 pKi = 8.2 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 nan
44431574 87360 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 505 8 1 6 4.0 COc1ccc(F)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL233814 87360 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 505 8 1 6 4.0 COc1ccc(F)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCN(c3ccccc3OC(C)C)CC2)CC1 10.1016/j.bmcl.2007.04.008
49865668 15860 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 390 8 1 5 4.3 COc1ccccc1N1CCN(CCCCNc2nccc3ccccc23)CC1 10.1016/j.bmcl.2010.07.096
CHEMBL1223748 15860 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 390 8 1 5 4.3 COc1ccccc1N1CCN(CCCCNc2nccc3ccccc23)CC1 10.1016/j.bmcl.2010.07.096
24805674 97356 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 390 8 1 5 4.3 COc1ccccc1N1CCN(CCCCNc2ccc3ccccc3n2)CC1 10.1016/j.bmcl.2010.07.096
CHEMBL271989 97356 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 390 8 1 5 4.3 COc1ccccc1N1CCN(CCCCNc2ccc3ccccc3n2)CC1 10.1016/j.bmcl.2010.07.096
10698880 120342 0 None 630 3 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 603 11 3 8 3.7 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)NC)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
CHEMBL355910 120342 0 None 630 3 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 603 11 3 8 3.7 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)NC)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1021/jm980506g
10698880 120342 0 None 630 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 603 11 3 8 3.7 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)NC)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
CHEMBL355910 120342 0 None 630 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 603 11 3 8 3.7 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(=O)NC)C2c2ccc([N+](=O)[O-])cc2)CC1 10.1007/s00044-004-0120-9
9893246 120965 0 None 34 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 531 9 3 6 4.0 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL358253 120965 0 None 34 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 531 9 3 6 4.0 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
9893246 120965 0 None 34 3 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 531 9 3 6 4.0 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
CHEMBL358253 120965 0 None 34 3 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 531 9 3 6 4.0 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
11857792 168792 0 None -3 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 560 8 1 5 5.8 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1 10.1016/j.bmcl.2007.04.098
CHEMBL442059 168792 0 None -3 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 560 8 1 5 5.8 COc1ccc(Cl)cc1S(=O)(=O)N[C@H]1CC[C@@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1 10.1016/j.bmcl.2007.04.098
16041265 94880 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 504 6 2 4 6.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(Cl)cccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL256597 94880 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 504 6 2 4 6.0 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(Cl)cccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
44431548 86604 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 502 8 1 7 3.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL232592 86604 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 502 8 1 7 3.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2007.04.008
136806218 112168 0 None 75 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 682 15 4 9 3.9 COc1ccc(C2(c3ccccc3)CCN(CCCNC(=O)C3=C(COCCN)NC(C)=C(C(N)=O)C3c3ccc([N+](=O)[O-])cc3)CC2)cc1 10.1016/s0960-894x(99)00484-9
44328754 112168 0 None 75 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 682 15 4 9 3.9 COc1ccc(C2(c3ccccc3)CCN(CCCNC(=O)C3=C(COCCN)NC(C)=C(C(N)=O)C3c3ccc([N+](=O)[O-])cc3)CC2)cc1 10.1016/s0960-894x(99)00484-9
CHEMBL330401 112168 0 None 75 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
ChEMBL 682 15 4 9 3.9 COc1ccc(C2(c3ccccc3)CCN(CCCNC(=O)C3=C(COCCN)NC(C)=C(C(N)=O)C3c3ccc([N+](=O)[O-])cc3)CC2)cc1 10.1016/s0960-894x(99)00484-9
52944615 16913 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 431 11 1 4 5.6 Clc1cccc(Cl)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1255002 16913 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 431 11 1 4 5.6 Clc1cccc(Cl)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
44298762 100149 0 None 15 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 473 8 1 7 1.9 CN(C)c1c[nH]c(=O)n(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
CHEMBL291951 100149 0 None 15 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 473 8 1 7 1.9 CN(C)c1c[nH]c(=O)n(CCCN2CCN(c3ccc(F)cc3OCC(F)(F)F)CC2)c1=O 10.1016/s0960-894x(03)00305-6
10839389 99877 0 None -3 3 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 472 4 1 7 3.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5c(C#N)cccc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL289627 99877 0 None -3 3 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 472 4 1 7 3.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5c(C#N)cccc54)c3=O)C[C@@H]21 10.1021/jm990567u
487 3564 17 None -4 12 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960069a
60602 3564 17 None -4 12 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960069a
CHEMBL405355 3564 17 None -4 12 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960069a
DB09239 3564 17 None -4 12 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm960069a
44288792 99839 0 None 134 3 Human 8.2 pKi = 8.2 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 451 8 1 3 5.5 Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2ccc(Cl)cc2)C(C)C)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL289339 99839 0 None 134 3 Human 8.2 pKi = 8.2 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 451 8 1 3 5.5 Cc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2ccc(Cl)cc2)C(C)C)CC1 10.1016/s0960-894x(00)00307-3
124 2921 44 None -13 33 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
2032 2921 44 None -13 33 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
4636 2921 44 None -13 33 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
CHEMBL762 2921 44 None -13 33 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
DB00935 2921 44 None -13 33 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
118716704 114486 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 423 5 0 6 3.2 COc1ccccc1N1CCN(CC2COC3(CCN(c4ccccc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342857 114486 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 423 5 0 6 3.2 COc1ccccc1N1CCN(CC2COC3(CCN(c4ccccc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
118716715 114498 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 521 6 0 7 3.1 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4ccc(Cl)cc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342868 114498 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 521 6 0 7 3.1 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4ccc(Cl)cc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
44331169 167373 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 444 6 1 6 3.1 COc1ccccc1CCN1CCC2(CC1)CC(=O)c1ccc(NS(C)(=O)=O)cc1O2 10.1016/s0960-894x(98)00732-x
CHEMBL431631 167373 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 444 6 1 6 3.1 COc1ccccc1CCN1CCC2(CC1)CC(=O)c1ccc(NS(C)(=O)=O)cc1O2 10.1016/s0960-894x(98)00732-x
16041449 94763 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 538 6 2 4 6.7 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(Cl)cc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL256040 94763 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 538 6 2 4 6.7 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)Nc3c(Cl)cc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2007.11.068
57391896 68948 0 None 1 5 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928129 68948 0 None 1 5 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
2894 206321 4 None -12 6 Bovine 8.2 pKi = 8.2 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)C4CCCCC43)nc(N)c2cc1OC 10.1021/jm960510x
CHEMBL97698 206321 4 None -12 6 Bovine 8.2 pKi = 8.2 Binding
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)C4CCCCC43)nc(N)c2cc1OC 10.1021/jm960510x
46934791 16496 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 479 7 0 7 2.6 COc1ccccc1N1CCN(C[C@H]2CO[C@@](CN3C(=O)CCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
CHEMBL1242818 16496 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration techniqueDisplacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique
ChEMBL 479 7 0 7 2.6 COc1ccccc1N1CCN(C[C@H]2CO[C@@](CN3C(=O)CCCC3=O)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2010.05.023
145960918 160969 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 427 3 1 7 3.2 COc1cc2nc(N3CCN(C(=O)C(C)(C)C)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4128460 160969 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 427 3 1 7 3.2 COc1cc2nc(N3CCN(C(=O)C(C)(C)C)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
46882085 5723 0 None -7 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 419 10 1 5 4.4 CCOc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
CHEMBL1078953 5723 0 None -7 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 419 10 1 5 4.4 CCOc1ccccc1OCCNCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmcl.2010.01.030
21830793 91389 5 None -44 46 Human 8.2 pKi = 8.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 91389 5 None -44 46 Human 8.2 pKi = 8.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
11948707 165603 0 None -128 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1021/acs.jmedchem.2c00633
CHEMBL426317 165603 0 None -128 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constantBinding affinity to alpha 1A adrenergic receptor (unknown origin) assessed as inhibition constant
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1021/acs.jmedchem.2c00633
118716700 114482 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 437 6 0 6 3.2 COc1ccccc1N1CCN(CC2COC3(CCN(Cc4ccccc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342853 114482 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 437 6 0 6 3.2 COc1ccccc1N1CCN(CC2COC3(CCN(Cc4ccccc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
10841296 36211 0 None 46 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 601 8 0 7 6.1 COC(=O)C1=C(C)N=C(C)N(Cc2cccc(CN3CCC(C(=O)OC)(c4ccccc4)CC3)c2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
CHEMBL144731 36211 0 None 46 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.
ChEMBL 601 8 0 7 6.1 COC(=O)C1=C(C)N=C(C)N(Cc2cccc(CN3CCC(C(=O)OC)(c4ccccc4)CC3)c2)C1c1ccc(F)c(F)c1 10.1021/jm9902032
10810527 100094 0 None -2 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 392 4 1 6 1.8 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4ccncc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL291588 100094 0 None -2 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 392 4 1 6 1.8 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4ccncc4c3=O)C[C@@H]21 10.1021/jm000541z
2142 3035 54 None -1 37 Bovine 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm020938y
4920903 3035 54 None -1 37 Bovine 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm020938y
502 3035 54 None -1 37 Bovine 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm020938y
5775 3035 54 None -1 37 Bovine 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm020938y
CHEMBL597 3035 54 None -1 37 Bovine 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm020938y
DB00692 3035 54 None -1 37 Bovine 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm020938y
3584 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
5401 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
7302 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
CHEMBL611 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
DB01162 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptorAbility to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
10507357 202229 0 None 58 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 574 10 1 7 4.0 COC(CNC(=O)c1ccc2c(c1)C(=O)N(c1cccc(F)c1)C2=O)CN1CCN(c2ccccc2OC(C)C)CC1 10.1021/jm9905918
CHEMBL69245 202229 0 None 58 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 574 10 1 7 4.0 COC(CNC(=O)c1ccc2c(c1)C(=O)N(c1cccc(F)c1)C2=O)CN1CCN(c2ccccc2OC(C)C)CC1 10.1021/jm9905918
3584 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990200p
3584 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990202+
5401 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990200p
5401 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990202+
7302 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990200p
7302 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990202+
CHEMBL611 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990200p
CHEMBL611 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990202+
DB01162 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990200p
DB01162 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990202+
3584 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990201h
5401 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990201h
7302 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990201h
CHEMBL611 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990201h
DB01162 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm990201h
10747021 120494 0 None 12 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 670 8 2 5 7.0 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccc(Cl)cc3)(c3ccc(Cl)cc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL356571 120494 0 None 12 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 670 8 2 5 7.0 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(c3ccc(Cl)cc3)(c3ccc(Cl)cc3)CC2)C1c1ccc(F)c(F)c1 10.1021/jm990201h
3584 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
5401 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
7302 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
CHEMBL611 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
DB01162 3706 60 None -2 14 Human 8.2 pKi = 8.2 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
90645600 111928 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 640 12 2 9 4.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCN(C)Cc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298018 111928 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 640 12 2 9 4.6 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCN(C)Cc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
135398745 2858 108 None -39 66 Human 7.2 pKi = 7.2 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2858 108 None -39 66 Human 7.2 pKi = 7.2 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2858 108 None -39 66 Human 7.2 pKi = 7.2 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2858 108 None -39 66 Human 7.2 pKi = 7.2 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
3038495 699 30 None -40 19 Rat 7.2 pKi = 7.2 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
7625 699 30 None -40 19 Rat 7.2 pKi = 7.2 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
CHEMBL25236 699 30 None -40 19 Rat 7.2 pKi = 7.2 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
44414264 12664 0 None -7 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 326 5 0 3 4.5 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)coc2c1 10.1016/j.bmcl.2006.05.002
CHEMBL1188050 12664 0 None -7 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 326 5 0 3 4.5 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)coc2c1 10.1016/j.bmcl.2006.05.002
CHEMBL534944 12664 0 None -7 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 326 5 0 3 4.5 c1ccc2c(C3CCN(CCCN4CCCCC4)CC3)coc2c1 10.1016/j.bmcl.2006.05.002
11705395 15861 0 None -19 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2010.07.096
CHEMBL1223749 15861 0 None -19 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2010.07.096
135398745 2858 108 None -39 66 Human 7.2 pKi = 7.2 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
47 2858 108 None -39 66 Human 7.2 pKi = 7.2 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
CHEMBL715 2858 108 None -39 66 Human 7.2 pKi = 7.2 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
DB00334 2858 108 None -39 66 Human 7.2 pKi = 7.2 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
197033 197463 58 None -7 8 Human 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589390 197463 58 None -7 8 Human 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
76315668 84897 0 None 36 3 Rat 7.2 pKi = 7.2 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 323 4 3 5 1.6 CCS(=O)(=O)Nc1c(O)ccc2c1CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
CHEMBL2261347 84897 0 None 36 3 Rat 7.2 pKi = 7.2 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 323 4 3 5 1.6 CCS(=O)(=O)Nc1c(O)ccc2c1CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
155555859 175643 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 433 11 1 5 4.6 COc1ccccc1OCCNCC[C@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4551941 175643 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 433 11 1 5 4.6 COc1ccccc1OCCNCC[C@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4594653 175643 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 433 11 1 5 4.6 COc1ccccc1OCCNCC[C@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
118716711 114494 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 389 4 0 6 1.6 COc1ccccc1N1CCN(CC2COC3(CCN(C(C)=O)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342864 114494 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 389 4 0 6 1.6 COc1ccccc1N1CCN(CC2COC3(CCN(C(C)=O)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
68712 99861 57 None -8 5 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1016/0960-894X(94)85032-1
CHEMBL289480 99861 57 None -8 5 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1016/0960-894X(94)85032-1
10326069 39044 1 None 23 9 Human 6.2 pKi = 6.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
CHEMBL147077 39044 1 None 23 9 Human 6.2 pKi = 6.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
73346334 92095 0 None -6 7 Human 5.2 pKi = 5.2 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 265 4 1 1 3.0 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
CHEMBL2432048 92095 0 None -6 7 Human 5.2 pKi = 5.2 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha1A receptor (unknown origin) by PDSP assay
ChEMBL 265 4 1 1 3.0 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
44431560 145033 0 None -2 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.008
CHEMBL391530 145033 0 None -2 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.008
44288816 154760 0 None 17 3 Human 7.2 pKi = 7.2 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 443 8 1 3 5.4 N#CC1(c2ccccc2)CCN(CCCNC(=O)C(c2ccccc2)C2CCCCC2)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL40303 154760 0 None 17 3 Human 7.2 pKi = 7.2 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 443 8 1 3 5.4 N#CC1(c2ccccc2)CCN(CCCNC(=O)C(c2ccccc2)C2CCCCC2)CC1 10.1016/s0960-894x(00)00307-3
3038603 101382 6 None -48 3 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligandThe compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligand
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL300647 101382 6 None -48 3 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligandThe compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligand
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
14378574 108087 0 None -24 5 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity at human Alpha-1A adrenergic receptor.In vitro binding affinity at human Alpha-1A adrenergic receptor.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(O)c3OC)C[C@@H]21 10.1021/jm0307741
CHEMBL320397 108087 0 None -24 5 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity at human Alpha-1A adrenergic receptor.In vitro binding affinity at human Alpha-1A adrenergic receptor.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(O)c3OC)C[C@@H]21 10.1021/jm0307741
10923927 202468 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 279 3 2 5 0.8 O=S1(=O)CCCc2cccc(NCC3=NCCN3)c21 10.1021/jm000542r
CHEMBL70740 202468 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 279 3 2 5 0.8 O=S1(=O)CCCc2cccc(NCC3=NCCN3)c21 10.1021/jm000542r
19968568 84901 0 None 2 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 323 4 2 5 1.5 COc1ccc2c(c1NS(C)(=O)=O)CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
CHEMBL2261353 84901 0 None 2 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 323 4 2 5 1.5 COc1ccc2c(c1NS(C)(=O)=O)CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
118717458 114629 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 412 10 2 4 6.9 Cc1ccc2nccc(NCCCCCCCNc3ccnc4ccc(C)cc34)c2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343980 114629 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 412 10 2 4 6.9 Cc1ccc2nccc(NCCCCCCCNc3ccnc4ccc(C)cc34)c2c1 10.1016/j.bmc.2014.09.017
118717458 114629 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 412 10 2 4 6.9 Cc1ccc2nccc(NCCCCCCCNc3ccnc4ccc(C)cc34)c2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343980 114629 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 412 10 2 4 6.9 Cc1ccc2nccc(NCCCCCCCNc3ccnc4ccc(C)cc34)c2c1 10.1016/j.bmc.2014.09.017
44295170 101339 0 None 19 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 554 6 2 7 2.8 COC(=O)C1(c2ccccc2)CCN(CCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
CHEMBL300272 101339 0 None 19 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 554 6 2 7 2.8 COC(=O)C1(c2ccccc2)CCN(CCNC(=O)N2C(=O)NC3=C(C(=O)OC3)C2c2ccc(F)c(F)c2)CC1 10.1016/s0960-894x(99)00653-8
10622206 101609 0 None 1 3 Rat 7.2 pKi = 7.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 423 6 1 6 3.6 COc1cc2c(cc1OC)NCN(CCN1C[C@@H]3CCc4c(OC)cccc4[C@@H]3C1)C2 10.1021/jm000541z
CHEMBL302192 101609 0 None 1 3 Rat 7.2 pKi = 7.2 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 423 6 1 6 3.6 COc1cc2c(cc1OC)NCN(CCN1C[C@@H]3CCc4c(OC)cccc4[C@@H]3C1)C2 10.1021/jm000541z
11211017 196547 0 None -43 7 Human 6.2 pKi = 6.2 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 373 4 0 4 2.7 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm0491391
CHEMBL57546 196547 0 None -43 7 Human 6.2 pKi = 6.2 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 373 4 0 4 2.7 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm0491391
2419 687 22 None -288 12 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm980053f
9 687 22 None -288 12 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm980053f
CHEMBL13647 687 22 None -288 12 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptorCompound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
ChEMBL 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 10.1021/jm980053f
16785637 180985 77 None -11 2 Bovine 4.2 pKi = 4.2 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 206 2 2 4 -0.4 NC(=O)c1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL47688 180985 77 None -11 2 Bovine 4.2 pKi = 4.2 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 206 2 2 4 -0.4 NC(=O)c1cccnc1N1CCNCC1 10.1021/jm00366a007
5282322 77844 16 None - 1 Rat 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 785 11 4 15 2.4 CO[C@@H]1[C@@H](O[C@@H]2O[C@H](C)[C@@H](O[C@H]3C[C@@](C)(O)[C@@H](OC(=O)CC(C)C)[C@H](C)O3)[C@H](N(C)C)[C@H]2O)[C@@H](CC=O)C[C@@H](C)[C@@H](O)/C=C/C=C/C[C@@H](C)OC(=O)C[C@H]1O nan
CHEMBL2106399 77844 16 None - 1 Rat 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 785 11 4 15 2.4 CO[C@@H]1[C@@H](O[C@@H]2O[C@H](C)[C@@H](O[C@H]3C[C@@](C)(O)[C@@H](OC(=O)CC(C)C)[C@H](C)O3)[C@H](N(C)C)[C@H]2O)[C@@H](CC=O)C[C@@H](C)[C@@H](O)/C=C/C=C/C[C@@H](C)OC(=O)C[C@H]1O nan
11091738 117576 0 None -954 6 Rat 6.2 pKi = 6.2 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm0211220
CHEMBL340641 117576 0 None -954 6 Rat 6.2 pKi = 6.2 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm0211220
10792347 121479 0 None 8 3 Human 7.2 pKi = 7.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 531 9 3 6 3.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(C)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
CHEMBL359375 121479 0 None 8 3 Human 7.2 pKi = 7.2 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 531 9 3 6 3.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(C)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
52937630 60962 0 None -199 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 351 4 0 4 3.2 CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767140 60962 0 None -199 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 351 4 0 4 3.2 CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)cc2)c2ccccc2c1=O 10.1021/jm1013874
24803638 60986 0 None -199 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 636 15 0 7 7.1 COc1ccc(Cc2nn(C[C@H]3CCCN3CCCCc3ccc(OCCCN4CCCCCC4)cc3)c(=O)c3ccccc23)cc1 10.1021/jm1013874
CHEMBL1767165 60986 0 None -199 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 636 15 0 7 7.1 COc1ccc(Cc2nn(C[C@H]3CCCN3CCCCc3ccc(OCCCN4CCCCCC4)cc3)c(=O)c3ccccc23)cc1 10.1021/jm1013874
53328873 63059 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 447 6 0 5 3.2 COc1ccccc1N1CCN(CCCN2C(=O)CC3(CCc4ccccc43)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796049 63059 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 447 6 0 5 3.2 COc1ccccc1N1CCN(CCCN2C(=O)CC3(CCc4ccccc43)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
9864325 101255 0 None -758 7 Human 6.2 pKi = 6.2 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 373 4 0 4 2.7 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2F)CC1 10.1021/jm0491391
CHEMBL299691 101255 0 None -758 7 Human 6.2 pKi = 6.2 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 373 4 0 4 2.7 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2ccccc2F)CC1 10.1021/jm0491391
14378574 108087 0 None -24 5 Human 6.2 pKi = 6.2 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(O)c3OC)C[C@@H]21 10.1016/j.bmcl.2004.11.032
CHEMBL320397 108087 0 None -24 5 Human 6.2 pKi = 6.2 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactiveBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(O)c3OC)C[C@@H]21 10.1016/j.bmcl.2004.11.032
11440979 195973 0 None -8 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 400 5 1 6 1.3 COc1ccccc1N1CCN(CCN2C(=O)CC3(CCNCC3)CC2=O)CC1 10.1021/jm030944+
CHEMBL57098 195973 0 None -8 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 400 5 1 6 1.3 COc1ccccc1N1CCN(CCN2C(=O)CC3(CCNCC3)CC2=O)CC1 10.1021/jm030944+
127036953 136977 0 None -63 22 Human 6.2 pKi = 6.2 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 136977 0 None -63 22 Human 6.2 pKi = 6.2 Binding
Binding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-1A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
10571609 204960 0 None -2 2 Rat 7.2 pKi = 7.2 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 376 6 0 4 3.4 Clc1cccc(N2CCN(CCCCN3CC4CCCCN4C3)CC2)c1 10.1021/jm970216k
CHEMBL89677 204960 0 None -2 2 Rat 7.2 pKi = 7.2 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 376 6 0 4 3.4 Clc1cccc(N2CCN(CCCCN3CC4CCCCN4C3)CC2)c1 10.1021/jm970216k
10594858 165092 0 None -2 2 Rat 7.2 pKi = 7.2 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 362 6 0 4 3.0 Clc1cccc(N2CCN(CCCCN3CC4CCCN4C3)CC2)c1 10.1021/jm970216k
CHEMBL424432 165092 0 None -2 2 Rat 7.2 pKi = 7.2 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 362 6 0 4 3.0 Clc1cccc(N2CCN(CCCCN3CC4CCCN4C3)CC2)c1 10.1021/jm970216k
3565378 178229 8 None -26 2 Rat 7.2 pKi = 7.2 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 424 6 0 4 3.0 O=C1C2CCCN2C(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm970216k
CHEMBL46918 178229 8 None -26 2 Rat 7.2 pKi = 7.2 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 424 6 0 4 3.0 O=C1C2CCCN2C(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm970216k
44361064 31385 0 None -23 6 Rat 6.2 pKi = 6.2 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 338 7 2 4 4.5 N=CCC(O)CC1CCN(c2ccccc2Oc2ccccc2)CC1 10.1021/jm960510x
CHEMBL140450 31385 0 None -23 6 Rat 6.2 pKi = 6.2 Binding
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assayBinding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
ChEMBL 338 7 2 4 4.5 N=CCC(O)CC1CCN(c2ccccc2Oc2ccccc2)CC1 10.1021/jm960510x
127025278 137176 0 None -33 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 387 9 1 4 3.7 COc1ccccc1N1CCN(CCCCNC(=O)CC2CCCCC2)CC1 10.1016/j.bmcl.2015.12.068
CHEMBL3758913 137176 0 None -33 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 387 9 1 4 3.7 COc1ccccc1N1CCN(CCCCNC(=O)CC2CCCCC2)CC1 10.1016/j.bmcl.2015.12.068
11994673 12195 0 None -3 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL1185036 12195 0 None -3 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL385371 12195 0 None -3 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
71449516 84167 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153552 84167 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2221146 84167 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 361 8 2 7 2.2 COc1cccc(OC)c1OCCNC[C@@H]1COc2cccc(O)c2O1 10.1016/j.ejmech.2012.09.049
11079593 202406 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70326 202406 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
10454026 17710 0 None -2041 9 Rat 6.2 pKi = 6.2 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0211220
CHEMBL125916 17710 0 None -2041 9 Rat 6.2 pKi = 6.2 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0211220
49800167 17484 0 None -1 3 Rat 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 514 9 2 6 3.1 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)NC(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL1258457 17484 0 None -1 3 Rat 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 514 9 2 6 3.1 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)NC(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
53328507 63051 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 469 8 0 5 4.2 COc1ccccc1N1CCN(CCCCN2C(=O)CC(c3ccc(Cl)cc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796041 63051 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 469 8 0 5 4.2 COc1ccccc1N1CCN(CCCCN2C(=O)CC(c3ccc(Cl)cc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
11554490 15862 0 None -67 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 428 7 1 4 5.3 FC(F)(F)c1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1 10.1016/j.bmcl.2010.07.096
CHEMBL1223750 15862 0 None -67 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 428 7 1 4 5.3 FC(F)(F)c1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1 10.1016/j.bmcl.2010.07.096
9909471 195221 0 None -21 4 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 409 4 0 4 3.4 O=C1CC2(CCCC2)C(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL56620 195221 0 None -21 4 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 409 4 0 4 3.4 O=C1CC2(CCCC2)C(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
3039881 173675 6 None -19 3 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligandThe compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligand
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL45491 173675 6 None -19 3 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligandThe compound was tested for binding affinity against Alpha-1 adrenergic receptor using WB-4101 as radioligand
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
11651319 181036 24 None -17 2 Bovine 5.2 pKi = 5.2 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cnccc1N1CCNCC1 10.1021/jm00366a007
CHEMBL47740 181036 24 None -17 2 Bovine 5.2 pKi = 5.2 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cnccc1N1CCNCC1 10.1021/jm00366a007
118717457 114626 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 374 7 2 6 4.3 COc1ccc2c(NCCNc3ccnc4cc(OC)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343978 114626 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 374 7 2 6 4.3 COc1ccc2c(NCCNc3ccnc4cc(OC)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
11857861 85235 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 520 10 1 6 4.5 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCCF)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
CHEMBL228606 85235 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to human cloned adrenergic Alpha-1A receptorBinding affinity to human cloned adrenergic Alpha-1A receptor
ChEMBL 520 10 1 6 4.5 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCCF)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.09.051
11857861 85235 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 520 10 1 6 4.5 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCCF)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL228606 85235 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 520 10 1 6 4.5 COc1ccc(S(=O)(=O)N[C@H]2CC[C@H](N3CCC(c4ccccc4OCCF)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
44275526 98397 0 None 2 3 Human 7.2 pKi = 7.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 621 11 2 6 7.3 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(OC(C)C)cc1 10.1021/jm960697s
CHEMBL27899 98397 0 None 2 3 Human 7.2 pKi = 7.2 Binding
Binding affinity was tested on human Alpha-1A adrenergic receptorBinding affinity was tested on human Alpha-1A adrenergic receptor
ChEMBL 621 11 2 6 7.3 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(OC(C)C)cc1 10.1021/jm960697s
118717457 114626 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 374 7 2 6 4.3 COc1ccc2c(NCCNc3ccnc4cc(OC)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
CHEMBL3343978 114626 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 374 7 2 6 4.3 COc1ccc2c(NCCNc3ccnc4cc(OC)ccc34)ccnc2c1 10.1016/j.bmc.2014.09.017
9884513 12902 0 None -43 2 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 343 5 1 2 4.4 Fc1ccc2[nH]cc(C3CCN(CCCN4CCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.05.002
CHEMBL1189871 12902 0 None -43 2 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 343 5 1 2 4.4 Fc1ccc2[nH]cc(C3CCN(CCCN4CCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.05.002
CHEMBL539601 12902 0 None -43 2 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 343 5 1 2 4.4 Fc1ccc2[nH]cc(C3CCN(CCCN4CCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.05.002
11338630 9551 0 None -6 3 Bovine 6.2 pKi = 6.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 403 4 2 3 4.8 O=S(=O)(Nc1cccc2c1CCCC2c1c[nH]cn1)c1ccc2ccccc2c1 10.1021/jm030551a
CHEMBL112814 9551 0 None -6 3 Bovine 6.2 pKi = 6.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 403 4 2 3 4.8 O=S(=O)(Nc1cccc2c1CCCC2c1c[nH]cn1)c1ccc2ccccc2c1 10.1021/jm030551a
53328504 63048 0 None -4 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 445 5 0 4 4.0 O=C1CC(c2ccc(Cl)cc2)CC(=O)N1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796038 63048 0 None -4 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 445 5 0 4 4.0 O=C1CC(c2ccc(Cl)cc2)CC(=O)N1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.ejmech.2011.03.054
101876962 114627 0 None 5 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 342 5 2 4 4.9 Cc1cccc2c(NCCNc3ccnc4c(C)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
CHEMBL3343979 114627 0 None 5 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 342 5 2 4 4.9 Cc1cccc2c(NCCNc3ccnc4c(C)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
11857794 85218 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 562 9 1 5 5.7 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1cccc(OC(F)F)c1 10.1016/j.bmcl.2007.04.098
CHEMBL228496 85218 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 562 9 1 5 5.7 O=S(=O)(N[C@H]1CC[C@@H](N2CCC(c3ccccc3OCC(F)(F)F)CC2)CC1)c1cccc(OC(F)F)c1 10.1016/j.bmcl.2007.04.098
57390115 68939 0 None -1 5 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928120 68939 0 None -1 5 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
10841190 106546 0 None 28 6 Human 8.2 pKi = 8.2 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 593 10 2 6 6.5 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(OC)cc1 10.1021/jm980077m
CHEMBL315538 106546 0 None 28 6 Human 8.2 pKi = 8.2 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 593 10 2 6 6.5 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(OC)cc1 10.1021/jm980077m
10841190 84835 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 593 10 2 6 5.7 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(OC)cc1 10.1007/s00044-004-0120-9
CHEMBL2260150 84835 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 593 10 2 6 5.7 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(OC)cc1 10.1007/s00044-004-0120-9
44126269 199789 4 None -18 6 Human 8.2 pKi = 8.2 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL605081 199789 4 None -18 6 Human 8.2 pKi = 8.2 Binding
Binding affinity to adrenergic alpha1A receptor by radioligand displacement assayBinding affinity to adrenergic alpha1A receptor by radioligand displacement assay
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
90645594 111981 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 597 10 2 8 4.7 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
CHEMBL3298747 111981 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
ChEMBL 597 10 2 8 4.7 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3c(sc4ccc(NC(=O)CCCc5ccccc5)cc43)c2=O)CC1 10.1016/j.ejmech.2014.06.057
145962478 161687 0 None -13 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 459 5 2 9 2.8 COc1cc2nc(N3CCC[C@H](NC4=CC(=O)c5ccccc5C4=O)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
CHEMBL4163587 161687 0 None -13 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 minsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
ChEMBL 459 5 2 9 2.8 COc1cc2nc(N3CCC[C@H](NC4=CC(=O)c5ccccc5C4=O)C3)nc(N)c2cc1OC 10.1016/j.ejmech.2017.05.003
2470 3583 46 None -398 60 Rat 8.1 pKi = 8.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00018a001
3300 3583 46 None -398 60 Rat 8.1 pKi = 8.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00018a001
5265 3583 46 None -398 60 Rat 8.1 pKi = 8.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00018a001
99 3583 46 None -398 60 Rat 8.1 pKi = 8.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00018a001
CHEMBL267930 3583 46 None -398 60 Rat 8.1 pKi = 8.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00018a001
155526629 175814 0 None -14 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 10 1 5 4.4 COc1ccccc1OCCNCCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4458714 175814 0 None -14 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 10 1 5 4.4 COc1ccccc1OCCNCCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4595984 175814 0 None -14 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 10 1 5 4.4 COc1ccccc1OCCNCCC1COC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
3584 3706 60 None -2 14 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
5401 3706 60 None -2 14 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
7302 3706 60 None -2 14 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
CHEMBL611 3706 60 None -2 14 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
DB01162 3706 60 None -2 14 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
21712258 168686 0 None 194 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 465 8 1 3 5.5 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(01)00320-1
CHEMBL44124 168686 0 None 194 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 465 8 1 3 5.5 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(01)00320-1
21712258 168686 0 None 194 2 Human 8.1 pKi = 8.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 465 8 1 3 5.5 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
CHEMBL44124 168686 0 None 194 2 Human 8.1 pKi = 8.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 465 8 1 3 5.5 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
44288815 100971 0 None 87 3 Human 8.1 pKi = 8.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 431 8 1 3 5.1 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3C)CC2)C(C)C)cc1 10.1016/s0960-894x(00)00307-3
CHEMBL297667 100971 0 None 87 3 Human 8.1 pKi = 8.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 431 8 1 3 5.1 Cc1ccc(C(C(=O)NCCCN2CCC(C#N)(c3ccccc3C)CC2)C(C)C)cc1 10.1016/s0960-894x(00)00307-3
101876962 114627 0 None 5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 342 5 2 4 4.9 Cc1cccc2c(NCCNc3ccnc4c(C)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
CHEMBL3343979 114627 0 None 5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 342 5 2 4 4.9 Cc1cccc2c(NCCNc3ccnc4c(C)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
44288392 99891 0 None -1 3 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 475 6 1 6 4.4 COc1cccc2c1CCC1CN(CCCCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC21 10.1021/jm990567u
CHEMBL289758 99891 0 None -1 3 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 475 6 1 6 4.4 COc1cccc2c1CCC1CN(CCCCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)CC21 10.1021/jm990567u
44431555 88719 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 535 8 1 7 3.3 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL236618 88719 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 535 8 1 7 3.3 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@H](NS(=O)(=O)c3ccc(S(C)(=O)=O)cc3)CC2)CC1 10.1016/j.bmcl.2007.04.008
10841819 118236 0 None 346 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 640 7 1 8 3.9 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)N2CCC(N3CCC(C(=O)OC)(c4ccccc4)CC3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL341838 118236 0 None 346 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 640 7 1 8 3.9 COCC1=C(C(=O)OC)C(c2ccc(F)c(F)c2)N(C(=O)N2CCC(N3CCC(C(=O)OC)(c4ccccc4)CC3)CC2)C(=O)N1 10.1021/jm990201h
44289112 164334 0 None 75 3 Human 8.1 pKi = 8.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 495 9 1 4 5.5 COc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2ccc(C)cc2)c2ccc(C)cc2)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL42220 164334 0 None 75 3 Human 8.1 pKi = 8.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 495 9 1 4 5.5 COc1ccccc1C1(C#N)CCN(CCCNC(=O)C(c2ccc(C)cc2)c2ccc(C)cc2)CC1 10.1016/s0960-894x(00)00307-3
8459 3234 3 None -20 3 Rat 8.1 pKi = 8.1 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 495 8 1 9 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)COc1c(OC)cccc1C(C)C 10.1021/jm9805337
9891980 3234 3 None -20 3 Rat 8.1 pKi = 8.1 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 495 8 1 9 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)COc1c(OC)cccc1C(C)C 10.1021/jm9805337
CHEMBL430717 3234 3 None -20 3 Rat 8.1 pKi = 8.1 Binding
The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1A adrenergic receptor in the COS cell line.
ChEMBL 495 8 1 9 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)COc1c(OC)cccc1C(C)C 10.1021/jm9805337
10793504 41482 0 None 436 3 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 588 10 3 8 3.2 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc3c(c2)OCO3)CC1 10.1021/jm980506g
CHEMBL149263 41482 0 None 436 3 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 588 10 3 8 3.2 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc3c(c2)OCO3)CC1 10.1021/jm980506g
10721049 43460 0 None 245 3 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 533 9 4 7 2.8 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(O)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
CHEMBL151045 43460 0 None 245 3 Human 8.1 pKi = 8.1 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 533 9 4 7 2.8 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(O)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
10743111 197008 0 None -1 3 Rat 8.1 pKi = 8.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 473 5 1 6 4.1 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(-c5ccccc5)sc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL58105 197008 0 None -1 3 Rat 8.1 pKi = 8.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 473 5 1 6 4.1 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(-c5ccccc5)sc4c3=O)C[C@@H]21 10.1021/jm000541z
10793504 41482 0 None 436 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 588 10 3 8 3.2 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc3c(c2)OCO3)CC1 10.1007/s00044-004-0120-9
CHEMBL149263 41482 0 None 436 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 588 10 3 8 3.2 CCOC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc3c(c2)OCO3)CC1 10.1007/s00044-004-0120-9
10606659 100055 0 None 7 3 Rat 8.1 pKi = 8.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 436 6 0 5 3.4 COc1cc2c(cc1OC)C(=O)N(CCN1C[C@@H]3CCc4c(OC)cccc4[C@@H]3C1)CC2 10.1021/jm000541z
CHEMBL291305 100055 0 None 7 3 Rat 8.1 pKi = 8.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 436 6 0 5 3.4 COc1cc2c(cc1OC)C(=O)N(CCN1C[C@@H]3CCc4c(OC)cccc4[C@@H]3C1)CC2 10.1021/jm000541z
2470 3583 46 None -208 60 Human 8.1 pKi = 8.1 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2004.11.032
3300 3583 46 None -208 60 Human 8.1 pKi = 8.1 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2004.11.032
5265 3583 46 None -208 60 Human 8.1 pKi = 8.1 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2004.11.032
99 3583 46 None -208 60 Human 8.1 pKi = 8.1 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2004.11.032
CHEMBL267930 3583 46 None -208 60 Human 8.1 pKi = 8.1 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2004.11.032
10721730 37245 0 None 245 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 568 6 2 7 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CC2)OC(=O)c2ccccc23)C1c1ccc(F)c(F)c1 10.1021/jm990201h
CHEMBL145571 37245 0 None 245 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 568 6 2 7 3.7 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CC2)OC(=O)c2ccccc23)C1c1ccc(F)c(F)c1 10.1021/jm990201h
76326030 84383 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 5 0 5 4.1 COc1ccccc1N1CCN(CC2CO[C@H](c3cccc4ccccc34)O2)CC1 10.1007/s00044-010-9379-1
CHEMBL2234446 84383 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 5 0 5 4.1 COc1ccccc1N1CCN(CC2CO[C@H](c3cccc4ccccc34)O2)CC1 10.1007/s00044-010-9379-1
76326030 84383 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 5 0 5 4.1 COc1ccccc1N1CCN(CC2CO[C@H](c3cccc4ccccc34)O2)CC1 10.1007/s00044-010-9379-1
CHEMBL2234446 84383 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 404 5 0 5 4.1 COc1ccccc1N1CCN(CC2CO[C@H](c3cccc4ccccc34)O2)CC1 10.1007/s00044-010-9379-1
11619713 72457 0 None -8 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 468 14 1 8 4.2 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccccc1[N+](=O)[O-] 10.1021/jm0580398
CHEMBL200136 72457 0 None -8 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cellsDisplacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells
ChEMBL 468 14 1 8 4.2 COc1cccc(OC)c1OCCNCCOc1ccccc1OCc1ccccc1[N+](=O)[O-] 10.1021/jm0580398
52947088 16914 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 391 11 1 4 4.9 Cc1cccc(C)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1255003 16914 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 391 11 1 4 4.9 Cc1cccc(C)c1OCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
118716713 114496 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 487 6 0 7 2.4 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4ccccc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342866 114496 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 487 6 0 7 2.4 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4ccccc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
118716719 114502 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 493 6 0 8 2.5 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4cccs4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342872 114502 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 493 6 0 8 2.5 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4cccs4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
10572794 205375 0 None - 1 Bovine 8.1 pKi = 8.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 395 7 1 5 3.0 Cc1cccc(C)c1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL92109 205375 0 None - 1 Bovine 8.1 pKi = 8.1 Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptorIn vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL 395 7 1 5 3.0 Cc1cccc(C)c1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
44213730 193973 0 None 7 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 460 8 2 7 1.3 O=c1[nH]cc(CO)c(=O)n1CCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
CHEMBL55645 193973 0 None 7 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptorInhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
ChEMBL 460 8 2 7 1.3 O=c1[nH]cc(CO)c(=O)n1CCCN1CCN(c2ccc(F)cc2OCC(F)(F)F)CC1 10.1016/s0960-894x(03)00305-6
11234230 101218 0 None -128 5 Human 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 375 4 0 3 3.6 O=C1CC2(CCCC2)CCN1CCN1CCN(c2ccccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL299454 101218 0 None -128 5 Human 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 375 4 0 3 3.6 O=C1CC2(CCCC2)CCN1CCN1CCN(c2ccccc2Cl)CC1 10.1007/s00044-010-9379-1
11234230 101218 0 None -128 5 Human 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 375 4 0 3 3.6 O=C1CC2(CCCC2)CCN1CCN1CCN(c2ccccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL299454 101218 0 None -128 5 Human 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 375 4 0 3 3.6 O=C1CC2(CCCC2)CCN1CCN1CCN(c2ccccc2Cl)CC1 10.1007/s00044-010-9379-1
44292196 179416 0 None -5 2 Bovine 6.2 pKi = 6.2 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 287 3 0 3 3.1 Clc1cccnc1N1CCN(Cc2ccccc2)CC1 10.1021/jm00366a007
CHEMBL47471 179416 0 None -5 2 Bovine 6.2 pKi = 6.2 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 287 3 0 3 3.1 Clc1cccnc1N1CCN(Cc2ccccc2)CC1 10.1021/jm00366a007
541604 164776 10 None 72 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm00118a019
CHEMBL42359 164776 10 None 72 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm00118a019
130442572 171332 0 None -147 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171332 0 None -147 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
9796594 9268 0 None - 1 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 307 3 3 4 2.0 CS(=O)(=O)Nc1ccc(O)c2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL111372 9268 0 None - 1 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 307 3 3 4 2.0 CS(=O)(=O)Nc1ccc(O)c2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
11196451 167491 0 None -1 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 268 5 2 3 1.7 CCS(=O)(=O)Nc1cccc(CC2CCCN2)c1 10.1021/jm030551a
CHEMBL432451 167491 0 None -1 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 268 5 2 3 1.7 CCS(=O)(=O)Nc1cccc(CC2CCCN2)c1 10.1021/jm030551a
76326540 84900 0 None -1 3 Rat 5.2 pKi = 5.2 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 274 2 4 4 1.3 NC(=O)Nc1c(O)ccc2c1CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
CHEMBL2261352 84900 0 None -1 3 Rat 5.2 pKi = 5.2 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 274 2 4 4 1.3 NC(=O)Nc1c(O)ccc2c1CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
44331079 4238 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 355 3 0 2 5.3 C1=CC2(CCN(CCc3cccc4ccccc34)CC2)Oc2ccccc21 10.1016/s0960-894x(98)00732-x
CHEMBL100878 4238 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 355 3 0 2 5.3 C1=CC2(CCN(CCc3cccc4ccccc34)CC2)Oc2ccccc21 10.1016/s0960-894x(98)00732-x
24829343 158463 0 None -89 9 Human 7.2 pKi = 7.2 Binding
Inhibition of adrenergic alpha-1 receptorInhibition of adrenergic alpha-1 receptor
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
CHEMBL409662 158463 0 None -89 9 Human 7.2 pKi = 7.2 Binding
Inhibition of adrenergic alpha-1 receptorInhibition of adrenergic alpha-1 receptor
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
415628 206441 89 None -60 5 Rat 6.2 pKi = 6.2 Binding
Binding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranesBinding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranes
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00110a014
CHEMBL9841 206441 89 None -60 5 Rat 6.2 pKi = 6.2 Binding
Binding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranesBinding affinity measured for alpha-1 adrenergic receptor by displacement of [3H]prazosin from rat cortical membranes
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00110a014
2771 193337 67 None -8 27 Rat 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL1200781 193337 67 None -8 27 Rat 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL549 193337 67 None -8 27 Rat 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
11633992 15910 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 460 8 1 5 5.8 FC(F)(F)c1cccc(N2CCN(CCCCNc3nc(-c4ccccc4)cs3)CC2)c1 10.1016/j.bmcl.2010.07.096
CHEMBL1223859 15910 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 460 8 1 5 5.8 FC(F)(F)c1cccc(N2CCN(CCCCNc3nc(-c4ccccc4)cs3)CC2)c1 10.1016/j.bmcl.2010.07.096
44289058 164782 0 None 16 3 Human 7.1 pKi = 7.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 403 8 1 3 4.5 CC(C)C(C(=O)NCCCN1CCC(C#N)(c2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(00)00307-3
CHEMBL42361 164782 0 None 16 3 Human 7.1 pKi = 7.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 403 8 1 3 4.5 CC(C)C(C(=O)NCCCN1CCC(C#N)(c2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(00)00307-3
4384568 162541 8 None -7 3 Rat 7.1 pKi = 7.1 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 438 6 0 4 3.4 O=C1C2CCCCN2C(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm970216k
CHEMBL417709 162541 8 None -7 3 Rat 7.1 pKi = 7.1 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 438 6 0 4 3.4 O=C1C2CCCCN2C(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm970216k
10713438 106535 0 None -4 2 Rat 7.1 pKi = 7.1 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 358 7 0 5 2.3 COc1ccccc1N1CCN(CCCCN2CC3CCCN3C2)CC1 10.1021/jm970216k
CHEMBL315472 106535 0 None -4 2 Rat 7.1 pKi = 7.1 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 358 7 0 5 2.3 COc1ccccc1N1CCN(CCCCN2CC3CCCN3C2)CC1 10.1021/jm970216k
21302490 112295 26 None -10 9 Human 7.1 pKi = 7.1 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3233142 112295 26 None -10 9 Human 7.1 pKi = 7.1 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3306803 112295 26 None -10 9 Human 7.1 pKi = 7.1 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
44309199 202344 0 None - 1 Human 5.1 pKi = 5.1 Binding
In vitro binding affinity towards Alpha-1 adrenergic receptor by displacing [3H]prazosin radioligandIn vitro binding affinity towards Alpha-1 adrenergic receptor by displacing [3H]prazosin radioligand
ChEMBL 355 6 3 4 2.7 Cc1ccc(CC2(O)CCN(C[C@@H](O)Cc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(01)00392-4
CHEMBL69967 202344 0 None - 1 Human 5.1 pKi = 5.1 Binding
In vitro binding affinity towards Alpha-1 adrenergic receptor by displacing [3H]prazosin radioligandIn vitro binding affinity towards Alpha-1 adrenergic receptor by displacing [3H]prazosin radioligand
ChEMBL 355 6 3 4 2.7 Cc1ccc(CC2(O)CCN(C[C@@H](O)Cc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(01)00392-4
10473406 202510 0 None - 1 Human 5.1 pKi = 5.1 Binding
In vitro binding affinity towards Alpha-1 adrenergic receptor by displacing [3H]prazosin radioligandIn vitro binding affinity towards Alpha-1 adrenergic receptor by displacing [3H]prazosin radioligand
ChEMBL 355 6 3 4 2.7 Cc1ccc(CC2(O)CCN(C[C@H](O)Cc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(01)00392-4
CHEMBL70918 202510 0 None - 1 Human 5.1 pKi = 5.1 Binding
In vitro binding affinity towards Alpha-1 adrenergic receptor by displacing [3H]prazosin radioligandIn vitro binding affinity towards Alpha-1 adrenergic receptor by displacing [3H]prazosin radioligand
ChEMBL 355 6 3 4 2.7 Cc1ccc(CC2(O)CCN(C[C@H](O)Cc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(01)00392-4
118717462 114633 0 None 2 4 Human 7.1 pKi = 7.1 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 444 12 2 6 6.3 COc1cccc2c(NCCCCCCCNc3ccnc4c(OC)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
CHEMBL3343984 114633 0 None 2 4 Human 7.1 pKi = 7.1 Binding
Binding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptorBinding affinity to human alpha1A adrenergic receptor transfected in COS1 cells assessed as compound required to occupy 50% of receptor
ChEMBL 444 12 2 6 6.3 COc1cccc2c(NCCCCCCCNc3ccnc4c(OC)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
9913449 105958 0 None 13 3 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparations
ChEMBL 489 6 0 7 3.5 O=C1c2cc(Cl)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL313990 105958 0 None 13 3 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparations
ChEMBL 489 6 0 7 3.5 O=C1c2cc(Cl)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
16041090 94936 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 496 8 2 6 4.7 COc1ccc(NC(=O)NC2CCC(N3CCN(c4ccccc4OC(C)C)CC3)CC2)c(OC)c1 10.1016/j.bmcl.2007.11.068
CHEMBL256853 94936 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 496 8 2 6 4.7 COc1ccc(NC(=O)NC2CCC(N3CCN(c4ccccc4OC(C)C)CC3)CC2)c(OC)c1 10.1016/j.bmcl.2007.11.068
56649649 67500 0 None -87 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910140 67500 0 None -87 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]prazosin from alpha1A receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
44288741 168270 0 None 45 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 408 8 1 4 3.3 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(01)00320-1
CHEMBL43799 168270 0 None 45 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 408 8 1 4 3.3 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(01)00320-1
44288741 168270 0 None 45 2 Human 7.1 pKi = 7.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 408 8 1 4 3.3 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL43799 168270 0 None 45 2 Human 7.1 pKi = 7.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 408 8 1 4 3.3 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(00)00307-3
76333282 84393 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 405 8 1 5 4.0 COc1ccccc1OCCNC1COC(c2ccccc2)(c2ccccc2)CO1 10.1007/s00044-010-9379-1
CHEMBL2234456 84393 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 405 8 1 5 4.0 COc1ccccc1OCCNC1COC(c2ccccc2)(c2ccccc2)CO1 10.1007/s00044-010-9379-1
118717462 114633 0 None 2 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 444 12 2 6 6.3 COc1cccc2c(NCCCCCCCNc3ccnc4c(OC)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
CHEMBL3343984 114633 0 None 2 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cellsDisplacement of [3H]-prazosin from human alpha1A adrenergic receptor transfected in COS1 cells
ChEMBL 444 12 2 6 6.3 COc1cccc2c(NCCCCCCCNc3ccnc4c(OC)cccc34)ccnc12 10.1016/j.bmc.2014.09.017
44568917 186762 0 None -9 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNC[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/jm800461k
CHEMBL493283 186762 0 None -9 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNC[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/jm800461k
52945071 17446 0 None -1 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 470 7 2 5 2.7 O=C1NC(=O)C(c2ccccc2)(c2ccccc2)N1CC(O)CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
CHEMBL1258344 17446 0 None -1 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity to adrenergic alpha1A receptor in rat brainBinding affinity to adrenergic alpha1A receptor in rat brain
ChEMBL 470 7 2 5 2.7 O=C1NC(=O)C(c2ccccc2)(c2ccccc2)N1CC(O)CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2010.07.101
44288857 168207 0 None 43 3 Human 7.1 pKi = 7.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 439 9 1 6 2.9 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(00)00307-3
CHEMBL43749 168207 0 None 43 3 Human 7.1 pKi = 7.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 439 9 1 6 2.9 COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(00)00307-3
49862238 14824 13 None 1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic Alpha-1A receptorBinding affinity to adrenergic Alpha-1A receptor
ChEMBL 367 6 0 5 3.6 COc1cccc(F)c1OC1CN(Cc2cnn(-c3ccccc3)c2C)C1 10.1016/j.bmcl.2010.06.033
CHEMBL1209158 14824 13 None 1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic Alpha-1A receptorBinding affinity to adrenergic Alpha-1A receptor
ChEMBL 367 6 0 5 3.6 COc1cccc(F)c1OC1CN(Cc2cnn(-c3ccccc3)c2C)C1 10.1016/j.bmcl.2010.06.033
44301680 101487 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 521 7 0 5 5.8 Cc1ccc(C2(c3ccc(C)cc3)OC(=O)N(CCCN3CCC(C#N)(c4ccccc4C)CC3)C2=O)cc1 10.1016/s0960-894x(01)00320-1
CHEMBL301416 101487 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 521 7 0 5 5.8 Cc1ccc(C2(c3ccc(C)cc3)OC(=O)N(CCCN3CCC(C#N)(c4ccccc4C)CC3)C2=O)cc1 10.1016/s0960-894x(01)00320-1
10688604 24533 0 None -4 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 341 5 2 5 2.4 O[C@@H]1[C@H](NC[C@@H]2COc3ccccc3O2)CC[C@H]1Oc1ccccc1 10.1021/jm991065j
CHEMBL134428 24533 0 None -4 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 341 5 2 5 2.4 O[C@@H]1[C@H](NC[C@@H]2COc3ccccc3O2)CC[C@H]1Oc1ccccc1 10.1021/jm991065j
9929277 100496 0 None -23 4 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 369 4 0 4 2.7 O=C1CCCC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL294235 100496 0 None -23 4 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 369 4 0 4 2.7 O=C1CCCC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
456387 100276 5 None -6 2 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 376 2 3 1 5.5 Brc1ccc2c(-c3nc(-c4c[nH]c5ccccc45)c[nH]3)c[nH]c2c1 10.1016/0960-894X(96)00376-9
CHEMBL292801 100276 5 None -6 2 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
ChEMBL 376 2 3 1 5.5 Brc1ccc2c(-c3nc(-c4c[nH]c5ccccc45)c[nH]3)c[nH]c2c1 10.1016/0960-894X(96)00376-9
44271701 65167 0 None - 1 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 192 1 0 2 1.9 CN1CC=C(c2ccncc2F)CC1 10.1021/jm00375a017
CHEMBL18306 65167 0 None - 1 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 192 1 0 2 1.9 CN1CC=C(c2ccncc2F)CC1 10.1021/jm00375a017
145946265 166942 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
CHEMBL4203310 166942 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
CHEMBL4299892 166942 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
10221005 202609 0 None 4 4 Human 6.1 pKi = 6.1 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71479 202609 0 None 4 4 Human 6.1 pKi = 6.1 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
76330198 84898 0 None 2 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 337 5 3 5 2.0 CCCS(=O)(=O)Nc1c(O)ccc2c1CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
CHEMBL2261348 84898 0 None 2 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 337 5 3 5 2.0 CCCS(=O)(=O)Nc1c(O)ccc2c1CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
1547484 925 70 None -125 20 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 925 70 None -125 20 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 925 70 None -125 20 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 925 70 None -125 20 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 925 70 None -125 20 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
10873978 167910 0 None -1905 6 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0211220
CHEMBL435218 167910 0 None -1905 6 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0211220
11698643 3560 8 None -15 4 Human 7.1 pKi = 7.1 Binding
Binding affinity to human adrenergic alpha-1A receptorBinding affinity to human adrenergic alpha-1A receptor
ChEMBL 479 6 0 4 6.0 O=C1C(=Nc2cccc(c2)C(F)(F)F)c2c(N1c1cccc(c1)OCCN1CCCC1)cccc2 10.1016/j.bmcl.2006.05.025
6125 3560 8 None -15 4 Human 7.1 pKi = 7.1 Binding
Binding affinity to human adrenergic alpha-1A receptorBinding affinity to human adrenergic alpha-1A receptor
ChEMBL 479 6 0 4 6.0 O=C1C(=Nc2cccc(c2)C(F)(F)F)c2c(N1c1cccc(c1)OCCN1CCCC1)cccc2 10.1016/j.bmcl.2006.05.025
CHEMBL209497 3560 8 None -15 4 Human 7.1 pKi = 7.1 Binding
Binding affinity to human adrenergic alpha-1A receptorBinding affinity to human adrenergic alpha-1A receptor
ChEMBL 479 6 0 4 6.0 O=C1C(=Nc2cccc(c2)C(F)(F)F)c2c(N1c1cccc(c1)OCCN1CCCC1)cccc2 10.1016/j.bmcl.2006.05.025
53248361 61738 0 None -50 7 Human 7.1 pKi = 7.1 Binding
Inhibition of adrenergic alpha1A receptorInhibition of adrenergic alpha1A receptor
ChEMBL 568 7 0 5 3.2 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52I)c2ccccn2)CC1 10.1021/jm1009956
CHEMBL1774991 61738 0 None -50 7 Human 7.1 pKi = 7.1 Binding
Inhibition of adrenergic alpha1A receptorInhibition of adrenergic alpha1A receptor
ChEMBL 568 7 0 5 3.2 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52I)c2ccccn2)CC1 10.1021/jm1009956
2105 2993 34 None -1258 33 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 2993 34 None -1258 33 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 2993 34 None -1258 33 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 2993 34 None -1258 33 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 2993 34 None -1258 33 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
9867138 194109 0 None -48 4 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 425 7 0 4 4.1 CN(CCN1C(=O)CC2(CCCC2)CC1=O)CCN(C)c1cc(Cl)ccc1Cl 10.1021/jm030944+
CHEMBL55790 194109 0 None -48 4 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 425 7 0 4 4.1 CN(CCN1C(=O)CC2(CCCC2)CC1=O)CCN(C)c1cc(Cl)ccc1Cl 10.1021/jm030944+
448537 159691 86 None -1584 25 Rat 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159691 86 None -1584 25 Rat 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
12134985 203160 0 None - 1 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 438 7 1 7 2.7 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)nc(N)n2)CC1 10.1016/s0960-894x(00)00472-8
CHEMBL75808 203160 0 None - 1 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 438 7 1 7 2.7 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)nc(N)n2)CC1 10.1016/s0960-894x(00)00472-8
10314056 206399 1 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 322 3 0 4 3.1 O=C1CC2(CCN(CCc3ccccn3)CC2)Oc2ccccc21 10.1016/s0960-894x(98)00732-x
CHEMBL98167 206399 1 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 322 3 0 4 3.1 O=C1CC2(CCN(CCc3ccccn3)CC2)Oc2ccccc21 10.1016/s0960-894x(98)00732-x
9923051 108169 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 319 4 2 3 2.9 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]c(C)n1 10.1007/s00044-004-0020-z
CHEMBL320765 108169 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 319 4 2 3 2.9 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]c(C)n1 10.1007/s00044-004-0020-z
52937629 60960 0 None -158 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 377 6 0 5 3.5 CCOc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
CHEMBL1767139 60960 0 None -158 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
ChEMBL 377 6 0 5 3.5 CCOc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
11288646 8571 0 None - 1 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 268 4 2 3 1.8 CCS(=O)(=O)Nc1cccc2c1CCCC2CN 10.1021/jm030551a
CHEMBL109553 8571 0 None - 1 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 268 4 2 3 1.8 CCS(=O)(=O)Nc1cccc2c1CCCC2CN 10.1021/jm030551a
9923051 108169 0 None - 1 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 319 4 2 3 2.9 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]c(C)n1 10.1021/jm030551a
CHEMBL320765 108169 0 None - 1 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 319 4 2 3 2.9 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]c(C)n1 10.1021/jm030551a
10626686 202606 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 560 9 2 7 3.3 CC(C)Oc1ccccc1N1CCN(C[C@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
CHEMBL71473 202606 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligandBinding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
ChEMBL 560 9 2 7 3.3 CC(C)Oc1ccccc1N1CCN(C[C@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2cccc(F)c2)C3=O)CC1 10.1021/jm9905918
44331150 4349 0 None 3 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 530 6 1 7 4.4 Cn1cnc(S(=O)(=O)Nc2ccc3c(c2)C(=O)CC2(CCN(CCc4cccc5ccccc45)CC2)O3)c1 10.1016/s0960-894x(98)00732-x
CHEMBL101579 4349 0 None 3 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 530 6 1 7 4.4 Cn1cnc(S(=O)(=O)Nc2ccc3c(c2)C(=O)CC2(CCN(CCc4cccc5ccccc45)CC2)O3)c1 10.1016/s0960-894x(98)00732-x
9847419 206443 0 None 14 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 467 5 2 5 3.9 Cc1[nH]c2ccccc2c1CCN1CCC2(CC1)CC(=O)c1ccc(NS(C)(=O)=O)cc1O2 10.1016/s0960-894x(98)00732-x
CHEMBL98430 206443 0 None 14 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1C adrenergic receptor expressed in CHO cells
ChEMBL 467 5 2 5 3.9 Cc1[nH]c2ccccc2c1CCN1CCC2(CC1)CC(=O)c1ccc(NS(C)(=O)=O)cc1O2 10.1016/s0960-894x(98)00732-x
10507129 121446 0 None 9 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 562 8 2 7 3.8 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(C)cc1 10.1021/jm990200p
CHEMBL359173 121446 0 None 9 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.
ChEMBL 562 8 2 7 3.8 COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc(C)cc1 10.1021/jm990200p
9867616 167752 0 None -1 3 Human 8.1 pKi = 8.1 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 435 6 1 8 2.2 COc1cc2nc(N3CCN(C(=O)CC(=O)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
CHEMBL434228 167752 0 None -1 3 Human 8.1 pKi = 8.1 Binding
The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.The binding affinity towards Alpha-1C adrenergic receptor in the COS cell line.
ChEMBL 435 6 1 8 2.2 COc1cc2nc(N3CCN(C(=O)CC(=O)c4ccccc4)CC3)nc(N)c2cc1OC 10.1021/jm9805337
115 340 66 None -3 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm00018a001
2092 340 66 None -3 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm00018a001
7109 340 66 None -3 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm00018a001
CHEMBL709 340 66 None -3 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm00018a001
DB00346 340 66 None -3 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1021/jm00018a001
4149971 166068 8 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 386 7 0 5 2.0 COc1ccccc1N1CCN(CCCCN2C(=O)C3CCCN3C2=O)CC1 10.1021/jm970216k
CHEMBL42810 166068 8 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 386 7 0 5 2.0 COc1ccccc1N1CCN(CCCCN2C(=O)C3CCCN3C2=O)CC1 10.1021/jm970216k
44300166 194669 0 None 15 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 583 7 2 7 4.0 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@H](N3CCC(c4ccccn4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
CHEMBL56248 194669 0 None 15 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cellsDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor stably expressed in CHO cells
ChEMBL 583 7 2 7 4.0 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)N[C@H]2CC[C@H](N3CCC(c4ccccn4)CC3)C2)C(=O)N1 10.1016/s0960-894x(00)00374-7
44420408 141214 0 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 453 5 2 6 2.7 COc1ccc(Cl)cc1N1CCN(CCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
CHEMBL386005 141214 0 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cellsDisplacement of [125I]BE2254 from human cloned adrenergic alpha 1A receptor expressed in HEK293 cells
ChEMBL 453 5 2 6 2.7 COc1ccc(Cl)cc1N1CCN(CCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1016/j.bmcl.2006.09.034
10320782 99502 0 None 4 7 Bovine 8.1 pKi = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNC[C@H]1Oc2ccccc2O[C@@H]1c1ccc(C)cc1 10.1021/jm960069a
CHEMBL286565 99502 0 None 4 7 Bovine 8.1 pKi = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
ChEMBL 435 9 1 6 4.6 COc1cccc(OC)c1OCCNC[C@H]1Oc2ccccc2O[C@@H]1c1ccc(C)cc1 10.1021/jm960069a
10811627 203829 0 None 11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 412 7 0 6 3.3 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)no2)CC1 10.1016/s0960-894x(02)00436-5
CHEMBL538529 203829 0 None 11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 412 7 0 6 3.3 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)no2)CC1 10.1016/s0960-894x(02)00436-5
CHEMBL81093 203829 0 None 11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 412 7 0 6 3.3 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)no2)CC1 10.1016/s0960-894x(02)00436-5
44268966 33203 0 None -6 6 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 476 7 1 7 3.6 COc1ccccc1N1CCN(CCCn2c(=O)[nH]c3scc(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL14199 33203 0 None -6 6 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-1A adrenergic receptorBinding affinity for human Alpha-1A adrenergic receptor
ChEMBL 476 7 1 7 3.6 COc1ccccc1N1CCN(CCCn2c(=O)[nH]c3scc(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
11857861 193102 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 520 10 1 6 4.5 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCCF)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
CHEMBL538397 193102 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned adrenergic alpha-1a receptorBinding affinity to human cloned adrenergic alpha-1a receptor
ChEMBL 520 10 1 6 4.5 COc1ccc(S(=O)(=O)N[C@H]2CC[C@@H](N3CCC(c4ccccc4OCCF)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.04.098
118716698 114481 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 364 4 0 6 2.5 COc1ccccc1N1CCN(CC2COC3(CCSCC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342852 114481 0 None 1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 364 4 0 6 2.5 COc1ccccc1N1CCN(CC2COC3(CCSCC3)O2)CC1 10.1016/j.ejmech.2014.09.070
4165402 178181 8 None 1 2 Rat 8.1 pKi = 8.1 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 400 7 0 5 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)C3CCCCN3C2=O)CC1 10.1021/jm970216k
CHEMBL46881 178181 8 None 1 2 Rat 8.1 pKi = 8.1 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 400 7 0 5 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)C3CCCCN3C2=O)CC1 10.1021/jm970216k
9887378 97940 3 None 40 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 402 8 1 5 1.7 CC(C)Oc1ccccc1N1CCN(CCNC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL275469 97940 3 None 40 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 402 8 1 5 1.7 CC(C)Oc1ccccc1N1CCN(CCNC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
10790430 84381 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 431 9 1 5 4.5 COc1cccc(OC)c1OCCNC[C@@H]1C(=O)c2ccccc2C[C@H]1c1ccccc1 10.1007/s00044-010-9379-1
CHEMBL2234444 84381 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 431 9 1 5 4.5 COc1cccc(OC)c1OCCNC[C@@H]1C(=O)c2ccccc2C[C@H]1c1ccccc1 10.1007/s00044-010-9379-1
44431562 88839 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(OC)c(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)c1 10.1016/j.bmcl.2007.04.008
CHEMBL236832 88839 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 517 9 1 7 3.9 COc1ccc(OC)c(S(=O)(=O)N[C@H]2CC[C@@H](N3CCN(c4ccccc4OC(C)C)CC3)CC2)c1 10.1016/j.bmcl.2007.04.008
10651080 105449 0 None 23 6 Human 8.1 pKi = 8.1 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 592 9 3 6 4.7 CC1=C(C(N)=O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL312871 105449 0 None 23 6 Human 8.1 pKi = 8.1 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 592 9 3 6 4.7 CC1=C(C(N)=O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
10531532 205355 0 None 8 6 Human 8.1 pKi = 8.1 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 594 9 2 7 6.0 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL91956 205355 0 None 8 6 Human 8.1 pKi = 8.1 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 594 9 2 7 6.0 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
10531532 84855 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 594 9 2 7 5.2 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
CHEMBL2260371 84855 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 594 9 2 7 5.2 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1007/s00044-004-0120-9
10651080 105449 0 None 23 6 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 592 9 3 6 4.7 CC1=C(C(N)=O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
CHEMBL312871 105449 0 None 23 6 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 592 9 3 6 4.7 CC1=C(C(N)=O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1007/s00044-004-0120-9
10790430 84381 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 431 9 1 5 4.5 COc1cccc(OC)c1OCCNC[C@@H]1C(=O)c2ccccc2C[C@H]1c1ccccc1 10.1007/s00044-010-9379-1
CHEMBL2234444 84381 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 431 9 1 5 4.5 COc1cccc(OC)c1OCCNC[C@@H]1C(=O)c2ccccc2C[C@H]1c1ccccc1 10.1007/s00044-010-9379-1
44288841 100657 0 None 3 3 Human 8.1 pKi = 8.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 440 8 1 2 5.8 Cc1ccc(C(C(=O)NCCCN2CCC(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
CHEMBL295304 100657 0 None 3 3 Human 8.1 pKi = 8.1 Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
ChEMBL 440 8 1 2 5.8 Cc1ccc(C(C(=O)NCCCN2CCC(c3ccccc3)CC2)c2ccc(C)cc2)cc1 10.1016/s0960-894x(00)00307-3
57393627 68950 0 None 11 5 Pig 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928131 68950 0 None 11 5 Pig 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
10507651 204771 0 None 42 6 Human 8.1 pKi = 8.1 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 591 9 2 6 5.8 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
CHEMBL88388 204771 0 None 42 6 Human 8.1 pKi = 8.1 Binding
Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptorBinding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor
ChEMBL 591 9 2 6 5.8 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
10507651 204771 0 None 42 6 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 591 9 2 6 5.8 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1007/s00044-004-0120-9
CHEMBL88388 204771 0 None 42 6 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) alpha1A adrenergic receptorBinding affinity to Homo sapiens (human) alpha1A adrenergic receptor
ChEMBL 591 9 2 6 5.8 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1007/s00044-004-0120-9
4038180 202 11 None 2 6 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
480 202 11 None 2 6 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
CHEMBL109783 202 11 None 2 6 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
118716716 114499 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 571 7 0 8 3.3 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4ccc(OC(F)(F)F)cc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342869 114499 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 571 7 0 8 3.3 COc1ccccc1N1CCN(CC2COC3(CCN(S(=O)(=O)c4ccc(OC(F)(F)F)cc4)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
73350823 102044 0 None -5 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human adrenergic alpha-1A receptor by competitive binding assayBinding affinity to human adrenergic alpha-1A receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL2424668 102044 0 None -5 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human adrenergic alpha-1A receptor by competitive binding assayBinding affinity to human adrenergic alpha-1A receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL3040578 102044 0 None -5 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human adrenergic alpha-1A receptor by competitive binding assayBinding affinity to human adrenergic alpha-1A receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
13141186 130156 0 None 7 2 Bovine 7.1 pKi = 7.1 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 312 0 0 2 4.2 CN1CCC(=C2c3cc(Cl)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
CHEMBL368357 130156 0 None 7 2 Bovine 7.1 pKi = 7.1 Binding
Displacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortexDisplacement of [3H]- prazosin radioligand binding at the alpha 1-adrenergic binding site of calf cerebral cortex
ChEMBL 312 0 0 2 4.2 CN1CCC(=C2c3cc(Cl)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
10622156 198375 0 None 1 3 Rat 7.1 pKi = 7.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 422 6 0 5 3.7 COc1cc2c(cc1OC)CN(CCN1C[C@@H]3CCc4c(OC)cccc4[C@@H]3C1)CC2 10.1021/jm000541z
CHEMBL59575 198375 0 None 1 3 Rat 7.1 pKi = 7.1 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 422 6 0 5 3.7 COc1cc2c(cc1OC)CN(CCN1C[C@@H]3CCc4c(OC)cccc4[C@@H]3C1)CC2 10.1021/jm000541z
2771431 187688 47 None -1 2 Bovine 6.1 pKi = 6.1 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 231 1 1 3 1.8 Clc1cnc(N2CCNCC2)c(Cl)c1 10.1021/jm00366a007
CHEMBL50016 187688 47 None -1 2 Bovine 6.1 pKi = 6.1 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 231 1 1 3 1.8 Clc1cnc(N2CCNCC2)c(Cl)c1 10.1021/jm00366a007
13938357 101247 0 None -79 2 Bovine 5.1 pKi = 5.1 Binding
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortexEvaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN([C@H]1CCN2CCc3c(oc4ccccc34)[C@H]2C1)S(=O)(=O)CCO 10.1021/jm00150a002
CHEMBL299595 101247 0 None -79 2 Bovine 5.1 pKi = 5.1 Binding
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortexEvaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN([C@H]1CCN2CCc3c(oc4ccccc34)[C@H]2C1)S(=O)(=O)CCO 10.1021/jm00150a002
127025277 137313 0 None -44 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 376 7 1 5 1.6 COc1ccccc1N1CCN(CCCCNC(=O)N2CCOCC2)CC1 10.1016/j.bmcl.2015.12.068
CHEMBL3760063 137313 0 None -44 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 376 7 1 5 1.6 COc1ccccc1N1CCN(CCCCNC(=O)N2CCOCC2)CC1 10.1016/j.bmcl.2015.12.068
11801861 118270 0 None 181 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 609 6 2 6 4.0 CCC1=C(C(N)=O)C(c2ccc(F)cc2F)N(C(=O)N2CCC(N3CCC(C(=O)OC)(c4ccccc4)CC3)CC2)C(=O)N1 10.1021/jm990201h
CHEMBL342064 118270 0 None 181 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomesIn vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL 609 6 2 6 4.0 CCC1=C(C(N)=O)C(c2ccc(F)cc2F)N(C(=O)N2CCC(N3CCC(C(=O)OC)(c4ccccc4)CC3)CC2)C(=O)N1 10.1021/jm990201h
44222842 193412 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 505 4 1 9 3.0 COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1021/jm8016046
CHEMBL549764 193412 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells
ChEMBL 505 4 1 9 3.0 COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1021/jm8016046
10367857 17913 0 None -21379 4 Rat 5.1 pKi = 5.1 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 478 7 2 3 5.5 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm0211220
CHEMBL126889 17913 0 None -21379 4 Rat 5.1 pKi = 5.1 Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin bindingBinding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
ChEMBL 478 7 2 3 5.5 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm0211220
10199335 203029 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74467 203029 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranesAffinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
10764133 84135 0 None -6 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153560 84135 0 None -6 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220899 84135 0 None -6 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counterDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2c(OC)cccc2O1 10.1016/j.ejmech.2012.09.049
44318000 203676 0 None 51 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 480 7 0 7 4.0 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3C(=O)CC4(CCCC4)CC3=O)co2)CC1 10.1016/s0960-894x(02)00436-5
CHEMBL80036 203676 0 None 51 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 480 7 0 7 4.0 CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3C(=O)CC4(CCCC4)CC3=O)co2)CC1 10.1016/s0960-894x(02)00436-5
16041091 94764 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 468 7 2 4 4.5 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)NCc3cccc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
CHEMBL256041 94764 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptorDisplacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor
ChEMBL 468 7 2 4 4.5 CC(C)Oc1ccccc1N1CCN(C2CCC(NC(=O)NCc3cccc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.068
44267817 162687 0 None 53 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 420 8 1 5 1.9 CC(C)Oc1cc(F)ccc1N1CCN(CCNC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL418531 162687 0 None 53 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 420 8 1 5 1.9 CC(C)Oc1cc(F)ccc1N1CCN(CCNC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
44593557 183326 7 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL481322 183326 7 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
155513941 175694 0 None -53 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 407 12 2 5 3.8 COc1ccccc1OCCNCC(CO)OC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.05.024
CHEMBL4439658 175694 0 None -53 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 407 12 2 5 3.8 COc1ccccc1OCCNCC(CO)OC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.05.024
CHEMBL4595078 175694 0 None -53 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 407 12 2 5 3.8 COc1ccccc1OCCNCC(CO)OC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.05.024
9880254 9196 0 None 43 2 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 323 4 2 3 2.8 CCS(=O)(=O)Nc1cc(F)cc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL110975 9196 0 None 43 2 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 323 4 2 3 2.8 CCS(=O)(=O)Nc1cc(F)cc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
10739024 69475 0 None -33 6 Human 6.1 pKi = 6.1 Binding
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 388 4 3 8 0.9 COc1cc2nc(N3CCN[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
CHEMBL19376 69475 0 None -33 6 Human 6.1 pKi = 6.1 Binding
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptorCompound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
ChEMBL 388 4 3 8 0.9 COc1cc2nc(N3CCN[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC 10.1021/jm980053f
11049096 11077 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 389 8 0 4 4.3 CN(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
CHEMBL1178700 11077 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 389 8 0 4 4.3 CN(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
CHEMBL37962 11077 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Affinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assayAffinity constant towards human recombinant Alpha-1A adrenergic receptor using [3H]prazosin (from CHO cells) as radioligand by radioligand binding assay
ChEMBL 389 8 0 4 4.3 CN(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1021/jm021078o
11049096 11077 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 389 8 0 4 4.3 CN(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
CHEMBL1178700 11077 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 389 8 0 4 4.3 CN(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
CHEMBL37962 11077 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 389 8 0 4 4.3 CN(CCOc1ccccc1)CC1COC(c2ccccc2)(c2ccccc2)O1 10.1007/s00044-010-9379-1
11334596 9315 0 None -1 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 265 4 2 3 1.9 CC(c1cccc(NS(C)(=O)=O)c1)c1c[nH]cn1 10.1021/jm030551a
CHEMBL111682 9315 0 None -1 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 265 4 2 3 1.9 CC(c1cccc(NS(C)(=O)=O)c1)c1c[nH]cn1 10.1021/jm030551a
9922027 114898 0 None 1 3 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 289 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCC=C2c1c[nH]cn1 10.1021/jm030551a
CHEMBL3350265 114898 0 None 1 3 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 289 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCC=C2c1c[nH]cn1 10.1021/jm030551a
71062708 153760 0 None -47 12 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3986651 153760 0 None -47 12 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
2520 202301 65 None -147 12 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL1280 202301 65 None -147 12 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL6966 202301 65 None -147 12 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
10479323 34455 0 None -9 3 Human 7.1 pKi = 7.1 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 459 5 2 5 4.4 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccc(C(F)(F)F)cc1)C3 10.1021/jm030952q
CHEMBL143026 34455 0 None -9 3 Human 7.1 pKi = 7.1 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 459 5 2 5 4.4 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccc(C(F)(F)F)cc1)C3 10.1021/jm030952q
10479323 34455 0 None -9 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 459 5 2 5 4.4 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccc(C(F)(F)F)cc1)C3 10.1007/s00044-010-9379-1
CHEMBL143026 34455 0 None -9 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 459 5 2 5 4.4 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccc(C(F)(F)F)cc1)C3 10.1007/s00044-010-9379-1
46882088 5735 0 None -11 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 435 10 1 6 4.0 COc1cccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)c1OC 10.1016/j.bmcl.2010.01.030
CHEMBL1079066 5735 0 None -11 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 435 10 1 6 4.0 COc1cccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)c1OC 10.1016/j.bmcl.2010.01.030
3198 203792 73 None -1698 34 Rat 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203792 73 None -1698 34 Rat 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203792 73 None -1698 34 Rat 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
44318075 203645 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 460 7 0 6 4.7 O=C1CCCCCN1Cc1cc(CN2CCN(c3ccccc3Oc3ccccc3)CC2)on1 10.1016/s0960-894x(02)00436-5
CHEMBL79817 203645 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]HEAT from human Alpha-1A adrenergic receptorDisplacement of [125I]HEAT from human Alpha-1A adrenergic receptor
ChEMBL 460 7 0 6 4.7 O=C1CCCCCN1Cc1cc(CN2CCN(c3ccccc3Oc3ccccc3)CC2)on1 10.1016/s0960-894x(02)00436-5
122187556 122529 0 None -7 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 307 5 1 2 4.2 c1ccc2c(C3CCN(CCCn4cccc4)CC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
CHEMBL3609355 122529 0 None -7 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membraneDisplacement of [3H]prazosin from alpha1A adrenoceptor in rat submaxillary gland membrane
ChEMBL 307 5 1 2 4.2 c1ccc2c(C3CCN(CCCn4cccc4)CC3)c[nH]c2c1 10.1016/j.bmcl.2015.07.046
9844321 100381 0 None -478 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 407 4 0 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)ccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL293539 100381 0 None -478 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 407 4 0 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)ccc2Cl)CC1 10.1007/s00044-010-9379-1
42 2024 50 None -15 18 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/s0960-894x(98)00451-x
56971 2024 50 None -15 18 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/s0960-894x(98)00451-x
CHEMBL8412 2024 50 None -15 18 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/s0960-894x(98)00451-x
9844321 100381 0 None -478 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 407 4 0 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)ccc2Cl)CC1 10.1007/s00044-010-9379-1
CHEMBL293539 100381 0 None -478 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 407 4 0 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCN1CCN(c2cc(F)ccc2Cl)CC1 10.1007/s00044-010-9379-1
11994915 11712 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cc(-c2ccccc2)ccc1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182145 11712 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cc(-c2ccccc2)ccc1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL214762 11712 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cc(-c2ccccc2)ccc1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
25132566 186730 0 None -14 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 343 8 1 5 2.8 COc1ccccc1OCCNC[C@@H]1COC[C@@H](c2ccccc2)O1 10.1021/jm800461k
CHEMBL493041 186730 0 None -14 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 343 8 1 5 2.8 COc1ccccc1OCCNC[C@@H]1COC[C@@H](c2ccccc2)O1 10.1021/jm800461k
11234230 101218 0 None -162 5 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 375 4 0 3 3.6 O=C1CC2(CCCC2)CCN1CCN1CCN(c2ccccc2Cl)CC1 10.1021/jm030944+
CHEMBL299454 101218 0 None -162 5 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 375 4 0 3 3.6 O=C1CC2(CCCC2)CCN1CCN1CCN(c2ccccc2Cl)CC1 10.1021/jm030944+
49783419 17552 0 None -263 13 Human 7.1 pKi = 7.1 Binding
Binding affinity to human adrenergic alpha1A receptorBinding affinity to human adrenergic alpha1A receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258671 17552 0 None -263 13 Human 7.1 pKi = 7.1 Binding
Binding affinity to human adrenergic alpha1A receptorBinding affinity to human adrenergic alpha1A receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
130442480 174688 0 None -107 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174688 0 None -107 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-prazosin from recombinant human alpha1A adrenergic receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
46915370 54667 0 None -1 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 195 0 3 5 -1.6 Cn1c(=O)[nH]c2c([nH]c(=O)n2C)c1=N 10.1021/jm100490m
CHEMBL1241328 54667 0 None -1 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 195 0 3 5 -1.6 Cn1c(=O)[nH]c2c([nH]c(=O)n2C)c1=N 10.1021/jm100490m
CHEMBL1615596 54667 0 None -1 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to adrenergic alpha1A receptorBinding affinity to adrenergic alpha1A receptor
ChEMBL 195 0 3 5 -1.6 Cn1c(=O)[nH]c2c([nH]c(=O)n2C)c1=N 10.1021/jm100490m
12134987 203270 0 None 16 2 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 414 7 0 6 2.8 CC(C)Oc1ccccc1N1CCN(CC2=NOC(CN3CCCCC3=O)C2)CC1 10.1016/s0960-894x(00)00472-8
CHEMBL76643 203270 0 None 16 2 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 414 7 0 6 2.8 CC(C)Oc1ccccc1N1CCN(CC2=NOC(CN3CCCCC3=O)C2)CC1 10.1016/s0960-894x(00)00472-8
155565219 175981 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 403 10 1 4 4.6 c1ccc(OCCNCC[C@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4580335 175981 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 403 10 1 4 4.6 c1ccc(OCCNCC[C@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
CHEMBL4597359 175981 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 403 10 1 4 4.6 c1ccc(OCCNCC[C@H]2CO[C@H](C(c3ccccc3)c3ccccc3)O2)cc1 10.1016/j.ejmech.2019.05.024
44568918 186763 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 449 10 1 6 4.0 COc1cccc(OC)c1OCCNC[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/jm800461k
CHEMBL493284 186763 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells
ChEMBL 449 10 1 6 4.0 COc1cccc(OC)c1OCCNC[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/jm800461k
68712 99861 57 None -8 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1016/0960-894X(94)85032-1
CHEMBL289480 99861 57 None -8 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1016/0960-894X(94)85032-1
2351 3222 60 None -138 21 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3222 60 None -138 21 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3222 60 None -138 21 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3222 60 None -138 21 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3222 60 None -138 21 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
1016 3678 75 None -1737 35 Rat 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3678 75 None -1737 35 Rat 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3678 75 None -1737 35 Rat 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3678 75 None -1737 35 Rat 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3678 75 None -1737 35 Rat 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3678 75 None -1737 35 Rat 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
44316072 203297 0 None 4 3 Human 8.1 pKi = 8.1 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 425 7 0 6 3.0 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)nn2C)CC1 10.1016/s0960-894x(00)00472-8
CHEMBL76867 203297 0 None 4 3 Human 8.1 pKi = 8.1 Binding
Compound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptorCompound was evaluated for its binding affinity to COS cell membrane expressing the human Alpha-1A adrenergic receptor
ChEMBL 425 7 0 6 3.0 CC(C)Oc1ccccc1N1CCN(Cc2cc(CN3CCCCC3=O)nn2C)CC1 10.1016/s0960-894x(00)00472-8
11567620 15885 0 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 404 8 1 4 4.9 Fc1ccccc1N1CCN(CCCCNc2cc(-c3ccccc3)ccn2)CC1 10.1016/j.bmcl.2010.07.096
CHEMBL1223802 15885 0 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
ChEMBL 404 8 1 4 4.9 Fc1ccccc1N1CCN(CCCCNc2cc(-c3ccccc3)ccn2)CC1 10.1016/j.bmcl.2010.07.096
57395340 68943 0 None 1 5 Pig 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928124 68943 0 None 1 5 Pig 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
10095156 78119 0 None 1 3 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL2112073 78119 0 None 1 3 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 447 4 1 6 3.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5ccccc54)c3=O)C[C@@H]21 10.1021/jm990567u
10698907 120505 0 None 602 3 Human 8.0 pKi = 8.0 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 605 12 4 9 2.4 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(C(=O)OCCO)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
CHEMBL356623 120505 0 None 602 3 Human 8.0 pKi = 8.0 Binding
Binding affinity was determined for the alpha-1A adrenergic receptorBinding affinity was determined for the alpha-1A adrenergic receptor
ChEMBL 605 12 4 9 2.4 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(C(=O)OCCO)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980506g
44295133 188132 0 None 13 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 586 7 2 5 5.0 O=C1OCC2=C1C(c1ccc(F)c(F)c1)N(C(=O)NCCCN1CCC(c3ccccc3)(c3ccccc3)CC1)C(=O)N2 10.1016/s0960-894x(99)00653-8
CHEMBL50490 188132 0 None 13 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptorDisplacement of [3H]- prazosin from human recombinant Alpha-1A adrenergic receptor
ChEMBL 586 7 2 5 5.0 O=C1OCC2=C1C(c1ccc(F)c(F)c1)N(C(=O)NCCCN1CCC(c3ccccc3)(c3ccccc3)CC1)C(=O)N2 10.1016/s0960-894x(99)00653-8
71817710 101921 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL2419770 101921 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm400867d
CHEMBL3039705 101921 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 minsDisplacement of [3H]prazosin from human alpha-1A adrenoreceptor expressed in CHO cells after 30 mins
ChEMBL 355 7 1 6 3.3 COc1ccc2ccoc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm400867d
10430193 161038 0 None -60 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 385 3 1 7 2.2 COc1cc2nc(N3CCN(C(C)=O)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL4129461 161038 0 None -60 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration methodDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
ChEMBL 385 3 1 7 2.2 COc1cc2nc(N3CCN(C(C)=O)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
3038495 699 30 None -6 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2015.12.068
7625 699 30 None -6 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2015.12.068
CHEMBL25236 699 30 None -6 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2015.12.068
1588 2284 24 None -38 44 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2284 24 None -38 44 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2284 24 None -38 44 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2284 24 None -38 44 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2284 24 None -38 44 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
10582624 201095 0 None -1 3 Rat 8.0 pKi = 8.0 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 393 4 1 7 1.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4nccnc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL62206 201095 0 None -1 3 Rat 8.0 pKi = 8.0 Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary glandBinding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL 393 4 1 7 1.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4nccnc4c3=O)C[C@@H]21 10.1021/jm000541z
10530732 167477 0 None -1 3 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 515 4 1 6 4.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cc(C(F)(F)F)ccc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL43234 167477 0 None -1 3 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 515 4 1 6 4.6 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cc(C(F)(F)F)ccc54)c3=O)C[C@@H]21 10.1021/jm990567u
9887378 97940 3 None 40 3 Human 8.0 pKi = 8.0 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 402 8 1 5 1.7 CC(C)Oc1ccccc1N1CCN(CCNC(=O)CN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.11.032
CHEMBL275469 97940 3 None 40 3 Human 8.0 pKi = 8.0 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
ChEMBL 402 8 1 5 1.7 CC(C)Oc1ccccc1N1CCN(CCNC(=O)CN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.11.032
11995034 11713 0 None 3 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cccc(-c2ccccc2)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182148 11713 0 None 3 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cccc(-c2ccccc2)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL214952 11713 0 None 3 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cellsDisplacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
ChEMBL 391 8 1 5 4.2 COc1cccc(-c2ccccc2)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
44388495 63079 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranesInhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranes
ChEMBL 362 5 3 3 3.4 Nc1ccc(C(=O)NCCN2CCC(c3cccc4[nH]ccc34)CC2)cc1 10.1021/jm0491804
CHEMBL179721 63079 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranesInhibition of [3H]prazosin binding to human adrenergic alpha-1A receptor expressed in CHO-K1 cell membranes
ChEMBL 362 5 3 3 3.4 Nc1ccc(C(=O)NCCN2CCC(c3cccc4[nH]ccc34)CC2)cc1 10.1021/jm0491804
1212 1624 45 None -19 66 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1624 45 None -19 66 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1624 45 None -19 66 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1624 45 None -19 66 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1624 45 None -19 66 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
44268966 33203 0 None -7 6 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 476 7 1 7 3.6 COc1ccccc1N1CCN(CCCn2c(=O)[nH]c3scc(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
CHEMBL14199 33203 0 None -7 6 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards rat Alpha-1A adrenergic receptorBinding affinity towards rat Alpha-1A adrenergic receptor
ChEMBL 476 7 1 7 3.6 COc1ccccc1N1CCN(CCCn2c(=O)[nH]c3scc(-c4ccccc4)c3c2=O)CC1 10.1016/s0960-894x(01)00159-7
3584 3706 60 None -2 14 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
5401 3706 60 None -2 14 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
7302 3706 60 None -2 14 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
CHEMBL611 3706 60 None -2 14 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
DB01162 3706 60 None -2 14 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
10644152 99916 7 None 1 3 Rat 8.0 pKi = 8.0 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 390 6 0 4 2.7 O=C1C2CCCN2C(=O)N1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm970216k
CHEMBL290039 99916 7 None 1 3 Rat 8.0 pKi = 8.0 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 390 6 0 4 2.7 O=C1C2CCCN2C(=O)N1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm970216k
44431546 87699 0 None -1 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 482 7 1 6 3.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccccc3C#N)CC2)CC1 10.1016/j.bmcl.2007.04.008
CHEMBL234679 87699 0 None -1 4 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned adrenergic alpha-1A receptorBinding affinity to human cloned adrenergic alpha-1A receptor
ChEMBL 482 7 1 6 3.8 CC(C)Oc1ccccc1N1CCN([C@H]2CC[C@@H](NS(=O)(=O)c3ccccc3C#N)CC2)CC1 10.1016/j.bmcl.2007.04.008
57391897 68952 0 None 1 5 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928133 68952 0 None 1 5 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenateDisplacement of [3H]prazosin from pig adrenergic alpha1 receptor in cerebral cortex homogenate
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
44301573 201100 0 None 154 3 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 535 7 1 5 4.6 Cc1ccc(C2(c3ccc(C)cc3)CC(=O)N(CC(O)CN3CCC(C#N)(c4ccccc4C)CC3)C2=O)cc1 10.1016/s0960-894x(01)00320-1
CHEMBL62249 201100 0 None 154 3 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards cloned human Alpha-1A adrenergic receptorIn vitro binding affinity towards cloned human Alpha-1A adrenergic receptor
ChEMBL 535 7 1 5 4.6 Cc1ccc(C2(c3ccc(C)cc3)CC(=O)N(CC(O)CN3CCC(C#N)(c4ccccc4C)CC3)C2=O)cc1 10.1016/s0960-894x(01)00320-1
53327992 63060 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 461 7 0 5 3.6 COc1ccccc1N1CCN(CCCCN2C(=O)CC3(CCc4ccccc43)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796050 63060 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 461 7 0 5 3.6 COc1ccccc1N1CCN(CCCCN2C(=O)CC3(CCc4ccccc43)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
52948823 16861 0 None -8 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 421 13 1 5 4.9 COc1cccc(OC)c1CCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
CHEMBL1254659 16861 0 None -8 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cellsDisplacement of [3H]prazosin from human adrenergic alpha1A expressed in CHO cells
ChEMBL 421 13 1 5 4.9 COc1cccc(OC)c1CCCNCCOc1ccccc1OCc1ccccc1 10.1016/j.bmc.2010.08.002
118716702 114484 0 None 5 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 396 4 0 7 1.1 COc1ccccc1N1CCN(CC2COC3(CCS(=O)(=O)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL3342855 114484 0 None 5 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 396 4 0 7 1.1 COc1ccccc1N1CCN(CC2COC3(CCS(=O)(=O)CC3)O2)CC1 10.1016/j.ejmech.2014.09.070
4110501 168517 8 None -2 2 Rat 8.0 pKi = 8 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 386 6 0 5 2.0 COc1ccccc1N1CCN(CCCN2C(=O)C3CCCCN3C2=O)CC1 10.1021/jm970216k
CHEMBL43992 168517 8 None -2 2 Rat 8.0 pKi = 8 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 386 6 0 5 2.0 COc1ccccc1N1CCN(CCCN2C(=O)C3CCCCN3C2=O)CC1 10.1021/jm970216k
9805944 55919 31 None -16 9 Human 8.0 pKi = 8 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptorDisplacement of [125I]HEAT from adrenergic alpha1A receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
CHEMBL1627 55919 31 None -16 9 Human 8.0 pKi = 8 Binding
Displacement of [125I]HEAT from adrenergic alpha1A receptorDisplacement of [125I]HEAT from adrenergic alpha1A receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
2247 502 77 None -5 42 Rat 8.0 pKi = 8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -5 42 Rat 8.0 pKi = 8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -5 42 Rat 8.0 pKi = 8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -5 42 Rat 8.0 pKi = 8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -5 42 Rat 8.0 pKi = 8 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
44461012 103783 0 None 7 3 Human 7.1 pKi = 7.1 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 509 6 0 7 3.7 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3cc4c(cc32)CCCC4)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL309949 103783 0 None 7 3 Human 7.1 pKi = 7.1 Binding
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cellsAbility to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 509 6 0 7 3.7 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3cc4c(cc32)CCCC4)CC1 10.1016/s0960-894x(98)00446-6
9913449 105958 0 None 13 3 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparations
ChEMBL 489 6 0 7 3.5 O=C1c2cc(Cl)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
CHEMBL313990 105958 0 None 13 3 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparationsCompound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparations
ChEMBL 489 6 0 7 3.5 O=C1c2cc(Cl)ccc2S(=O)(=O)N1CCCCN1CCC(n2c(=O)oc3ccccc32)CC1 10.1016/s0960-894x(98)00446-6
5019971 172690 5 None -15 2 Rat 7.0 pKi = 7.0 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 424 5 0 4 3.0 O=C1C2CCCCN2C(=O)N1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm970216k
CHEMBL45253 172690 5 None -15 2 Rat 7.0 pKi = 7.0 Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membraneBinding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin as radioligand in rat cerebral cortex membrane
ChEMBL 424 5 0 4 3.0 O=C1C2CCCCN2C(=O)N1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm970216k
3805301 100854 76 None 1 2 Bovine 6.1 pKi = 6.1 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1ccc(N2CCNCC2)nc1 10.1021/jm00366a007
CHEMBL296787 100854 76 None 1 2 Bovine 6.1 pKi = 6.1 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1ccc(N2CCNCC2)nc1 10.1021/jm00366a007
44414189 12690 0 None -12 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 342 5 1 5 3.3 Oc1nc2ccccc2n1C1CCN(CCCN2CCCCC2)CC1 10.1016/j.bmcl.2006.05.002
CHEMBL1188266 12690 0 None -12 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 342 5 1 5 3.3 Oc1nc2ccccc2n1C1CCN(CCCN2CCCCC2)CC1 10.1016/j.bmcl.2006.05.002
CHEMBL535838 12690 0 None -12 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranesDisplacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
ChEMBL 342 5 1 5 3.3 Oc1nc2ccccc2n1C1CCN(CCCN2CCCCC2)CC1 10.1016/j.bmcl.2006.05.002
71061709 148983 0 None -63 12 Mouse 5.0 pKi = 5.0 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3946540 148983 0 None -63 12 Mouse 5.0 pKi = 5.0 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
3658 4032 47 None -9 8 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1016/j.bmcl.2004.06.085
517 4032 47 None -9 8 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1016/j.bmcl.2004.06.085
5709 4032 47 None -9 8 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1016/j.bmcl.2004.06.085
CHEMBL312448 4032 47 None -9 8 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1016/j.bmcl.2004.06.085
DB06694 4032 47 None -9 8 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1016/j.bmcl.2004.06.085
44269078 98132 7 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
ChEMBL 202 1 1 2 2.3 CC(C)(C)c1ccc(C2=NCCN2)cc1 10.1016/j.bmcl.2004.06.085
CHEMBL276868 98132 7 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
ChEMBL 202 1 1 2 2.3 CC(C)(C)c1ccc(C2=NCCN2)cc1 10.1016/j.bmcl.2004.06.085
135 2486 38 None -46 58 Rat 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2486 38 None -46 58 Rat 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2486 38 None -46 58 Rat 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2486 38 None -46 58 Rat 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2486 38 None -46 58 Rat 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
44123711 84385 0 None -17 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 346 4 0 5 2.9 COc1ccccc1N1CCN(CC2COC3(CCCCC3)O2)CC1 10.1007/s00044-010-9379-1
CHEMBL2234448 84385 0 None -17 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 346 4 0 5 2.9 COc1ccccc1N1CCN(CC2COC3(CCCCC3)O2)CC1 10.1007/s00044-010-9379-1
9900133 8882 0 None 1 4 Rat 7.0 pKi = 7.0 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 271 2 2 3 3.1 COC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL109827 8882 0 None 1 4 Rat 7.0 pKi = 7.0 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 271 2 2 3 3.1 COC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
46881443 5499 0 None -34 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 405 9 1 5 4.0 COc1cccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)c1 10.1016/j.bmcl.2010.01.030
CHEMBL1077168 5499 0 None -34 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cellsDisplacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells
ChEMBL 405 9 1 5 4.0 COc1cccc(OCCNCC2COC(c3ccccc3)(c3ccccc3)O2)c1 10.1016/j.bmcl.2010.01.030
44123711 84385 0 None -17 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 346 4 0 5 2.9 COc1ccccc1N1CCN(CC2COC3(CCCCC3)O2)CC1 10.1016/j.ejmech.2014.09.070
CHEMBL2234448 84385 0 None -17 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 346 4 0 5 2.9 COc1ccccc1N1CCN(CC2COC3(CCCCC3)O2)CC1 10.1016/j.ejmech.2014.09.070
44123711 84385 0 None -17 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 346 4 0 5 2.9 COc1ccccc1N1CCN(CC2COC3(CCCCC3)O2)CC1 10.1016/j.ejmech.2016.09.050
CHEMBL2234448 84385 0 None -17 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
ChEMBL 346 4 0 5 2.9 COc1ccccc1N1CCN(CC2COC3(CCCCC3)O2)CC1 10.1016/j.ejmech.2016.09.050
11449200 78037 0 None 20 3 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCC[C@H]2c1c[nH]cn1 10.1021/jm030551a
CHEMBL2111710 78037 0 None 20 3 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCC[C@H]2c1c[nH]cn1 10.1021/jm030551a
9906677 100563 0 None -11 3 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 355 4 0 4 2.3 O=C1CCC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
CHEMBL294646 100563 0 None -11 3 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL 355 4 0 4 2.3 O=C1CCC(=O)N1CCN1CCN(c2cc(Cl)ccc2Cl)CC1 10.1021/jm030944+
44312198 202873 0 None -3 4 Human 4.0 pKi = 4.0 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 292 1 1 5 2.2 Brc1c(NC2=NCCO2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL73164 202873 0 None -3 4 Human 4.0 pKi = 4.0 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 292 1 1 5 2.2 Brc1c(NC2=NCCO2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
145947560 167136 0 None -4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 344 6 0 3 4.2 Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl 10.1016/j.bmcl.2018.04.059
CHEMBL4212812 167136 0 None -4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 344 6 0 3 4.2 Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl 10.1016/j.bmcl.2018.04.059
CHEMBL4302457 167136 0 None -4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting methodDisplacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
ChEMBL 344 6 0 3 4.2 Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl 10.1016/j.bmcl.2018.04.059
2146 3039 63 None -10 8 Bovine 6.0 pKi = 6.0 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
485 3039 63 None -10 8 Bovine 6.0 pKi = 6.0 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
6041 3039 63 None -10 8 Bovine 6.0 pKi = 6.0 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
CHEMBL1215 3039 63 None -10 8 Bovine 6.0 pKi = 6.0 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
DB00388 3039 63 None -10 8 Bovine 6.0 pKi = 6.0 Binding
Binding affinity towards bovine clonal Alpha-1A adrenergic receptorBinding affinity towards bovine clonal Alpha-1A adrenergic receptor
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
9965896 109872 0 None - 1 Rat 6.0 pKi = 6.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 293 4 2 4 1.8 CCS(=O)(=O)Nc1cccc2c1COC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL324238 109872 0 None - 1 Rat 6.0 pKi = 6.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 293 4 2 4 1.8 CCS(=O)(=O)Nc1cccc2c1COC2c1c[nH]cn1 10.1021/jm030551a
136 3228 28 None -1995 16 Bovine 6.0 pKi = 6.0 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00366a007
223 3228 28 None -1995 16 Bovine 6.0 pKi = 6.0 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00366a007
643606 3228 28 None -1995 16 Bovine 6.0 pKi = 6.0 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00366a007
CHEMBL10347 3228 28 None -1995 16 Bovine 6.0 pKi = 6.0 Binding
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligandBinding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00366a007
136 3228 28 None -1995 16 Bovine 6.0 pKi = 6.0 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00375a017
223 3228 28 None -1995 16 Bovine 6.0 pKi = 6.0 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00375a017
643606 3228 28 None -1995 16 Bovine 6.0 pKi = 6.0 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00375a017
CHEMBL10347 3228 28 None -1995 16 Bovine 6.0 pKi = 6.0 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00375a017
9929936 167338 0 None -9 5 Human 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 0 4 3.1 Cc1ccc(C)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1007/s00044-010-9379-1
CHEMBL431354 167338 0 None -9 5 Human 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 0 4 3.1 Cc1ccc(C)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1007/s00044-010-9379-1
76318763 84386 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 381 5 2 6 3.0 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccoc1)C3 10.1007/s00044-010-9379-1
CHEMBL2234449 84386 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 381 5 2 6 3.0 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccoc1)C3 10.1007/s00044-010-9379-1
11338016 35732 0 None -7 3 Human 7.0 pKi = 7.0 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 381 5 2 6 3.0 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccco1)C3 10.1021/jm030952q
CHEMBL144286 35732 0 None -7 3 Human 7.0 pKi = 7.0 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 381 5 2 6 3.0 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccco1)C3 10.1021/jm030952q
9929936 167338 0 None -9 5 Human 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 0 4 3.1 Cc1ccc(C)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1007/s00044-010-9379-1
CHEMBL431354 167338 0 None -9 5 Human 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
ChEMBL 383 4 0 4 3.1 Cc1ccc(C)c(N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2)c1 10.1007/s00044-010-9379-1
9926529 9284 2 None 1 5 Rat 7.0 pKi = 7.0 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
CHEMBL111496 9284 2 None 1 5 Rat 7.0 pKi = 7.0 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1007/s00044-004-0020-z
44361064 31385 0 None -3 6 Human 7.0 pKi = 7.0 Binding
Compound was tested for binding affinity against human hippocampus Alpha-1A adrenergic receptor using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against human hippocampus Alpha-1A adrenergic receptor using radioligand ([3H]prazosin) binding assay
ChEMBL 338 7 2 4 4.5 N=CCC(O)CC1CCN(c2ccccc2Oc2ccccc2)CC1 10.1021/jm960510x
CHEMBL140450 31385 0 None -3 6 Human 7.0 pKi = 7.0 Binding
Compound was tested for binding affinity against human hippocampus Alpha-1A adrenergic receptor using radioligand ([3H]prazosin) binding assayCompound was tested for binding affinity against human hippocampus Alpha-1A adrenergic receptor using radioligand ([3H]prazosin) binding assay
ChEMBL 338 7 2 4 4.5 N=CCC(O)CC1CCN(c2ccccc2Oc2ccccc2)CC1 10.1021/jm960510x
53328687 63057 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 483 8 0 5 4.4 COc1ccc(Cl)cc1N1CCN(CCCCN2C(=O)CC(C)(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
CHEMBL1796047 63057 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cellsDisplacement of [125I]BE-2254 from human adrenergic alpha1A receptor expressed in HEK293 cells
ChEMBL 483 8 0 5 4.4 COc1ccc(Cl)cc1N1CCN(CCCCN2C(=O)CC(C)(c3ccccc3)CC2=O)CC1 10.1016/j.ejmech.2011.03.054
10804826 23397 1 None 1 4 Rat 6.0 pKi = 6.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL133451 23397 1 None 1 4 Rat 6.0 pKi = 6.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
10065903 22087 0 None -257 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 341 5 2 5 2.4 O[C@H]1[C@@H](NC[C@@H]2COc3ccccc3O2)CC[C@@H]1Oc1ccccc1 10.1021/jm991065j
CHEMBL132378 22087 0 None -257 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptorDisplacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
ChEMBL 341 5 2 5 2.4 O[C@H]1[C@@H](NC[C@@H]2COc3ccccc3O2)CC[C@@H]1Oc1ccccc1 10.1021/jm991065j
44276536 96907 0 None -1584 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 373 8 1 4 3.3 COc1ccccc1N1CCN(CCCCNC(=O)C2CCCCC2)CC1 10.1016/j.bmcl.2015.12.068
CHEMBL26962 96907 0 None -1584 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-prazosin from human ADRA1A receptorDisplacement of [3H]-prazosin from human ADRA1A receptor
ChEMBL 373 8 1 4 3.3 COc1ccccc1N1CCN(CCCCNC(=O)C2CCCCC2)CC1 10.1016/j.bmcl.2015.12.068
10382537 202456 11 None -144 6 Human 6.0 pKi = 6.0 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 339 1 2 5 1.6 Ic1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL70676 202456 11 None -144 6 Human 6.0 pKi = 6.0 Binding
Binding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosinBinding affinity for human Alpha-1A adrenergic receptor from cultured LM(tk-) cells using [3H]-prazosin
ChEMBL 339 1 2 5 1.6 Ic1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
11488170 34989 0 None -24 3 Human 6.0 pKi = 6.0 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 467 10 2 8 3.6 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNCCOc1c(OC)cccc1OC)C3 10.1021/jm030952q
CHEMBL143558 34989 0 None -24 3 Human 6.0 pKi = 6.0 Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKiBinding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
ChEMBL 467 10 2 8 3.6 COc1cc2nc3c(c(N)c2cc1OC)CCC(CNCCOc1c(OC)cccc1OC)C3 10.1021/jm030952q
2146 3039 63 None -141 8 Rat 6.0 pKi = 6.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
485 3039 63 None -141 8 Rat 6.0 pKi = 6.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
6041 3039 63 None -141 8 Rat 6.0 pKi = 6.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
CHEMBL1215 3039 63 None -141 8 Rat 6.0 pKi = 6.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
DB00388 3039 63 None -141 8 Rat 6.0 pKi = 6.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glandsBinding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
2803 939 53 None -8 19 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
516 939 53 None -8 19 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
704 939 53 None -8 19 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
CHEMBL134 939 53 None -8 19 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
DB00575 939 53 None -8 19 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosinBinding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
155544514 175771 0 None -309 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 10 1 5 4.2 COc1ccccc1OCCNC[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4526865 175771 0 None -309 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 10 1 5 4.2 COc1ccccc1OCCNC[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
CHEMBL4595671 175771 0 None -309 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation countingDisplacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
ChEMBL 419 10 1 5 4.2 COc1ccccc1OCCNC[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)O1 10.1016/j.ejmech.2019.05.024
9944937 110837 0 None 1 2 Bovine 6.0 pKi = 6.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 320 4 2 3 2.1 CN(C)S(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL326862 110837 0 None 1 2 Bovine 6.0 pKi = 6.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
ChEMBL 320 4 2 3 2.1 CN(C)S(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
162265 200578 19 None -5 45 Rat 5.0 pKi = 5.0 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1007/s00044-004-0020-z
4786 200578 19 None -5 45 Rat 5.0 pKi = 5.0 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1007/s00044-004-0020-z
CHEMBL61006 200578 19 None -5 45 Rat 5.0 pKi = 5.0 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1007/s00044-004-0020-z
162265 200578 19 None -5 45 Rat 5.0 pKi = 5.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1021/jm030551a
4786 200578 19 None -5 45 Rat 5.0 pKi = 5.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1021/jm030551a
CHEMBL61006 200578 19 None -5 45 Rat 5.0 pKi = 5.0 Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assayIn vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1021/jm030551a
118718431 114842 0 None 11 2 Human 7.0 pKi = 7.0 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 504 8 0 6 3.9 CCOC(=O)[C@H]1CN(CCCCN2C(=O)c3cc(Cl)ccc3S2(=O)=O)CC[C@H]1c1ccccc1 10.1016/s0960-894x(98)00451-x
CHEMBL3349545 114842 0 None 11 2 Human 7.0 pKi = 7.0 Binding
Binding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assayBinding affinity against human Alpha-1a adrenergic receptor was evaluated by cloned receptor binding assay
ChEMBL 504 8 0 6 3.9 CCOC(=O)[C@H]1CN(CCCCN2C(=O)c3cc(Cl)ccc3S2(=O)=O)CC[C@H]1c1ccccc1 10.1016/s0960-894x(98)00451-x
44267912 16688 0 None 102 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 388 8 1 5 1.3 COc1ccccc1N1CCN(CCCNC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
CHEMBL12501 16688 0 None 102 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranesBinding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
ChEMBL 388 8 1 5 1.3 COc1ccccc1N1CCN(CCCNC(=O)CN2CCCCC2=O)CC1 10.1016/s0960-894x(00)00169-4
277 1269 55 None -117 46 Rat 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1269 55 None -117 46 Rat 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1269 55 None -117 46 Rat 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1269 55 None -117 46 Rat 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1269 55 None -117 46 Rat 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
10673466 161203 0 None -3 3 Rat 7.0 pKi = 7 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 481 4 1 6 4.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5c(Cl)cccc54)c3=O)C[C@@H]21 10.1021/jm990567u
CHEMBL41396 161203 0 None -3 3 Rat 7.0 pKi = 7 Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptorIn vitro binding affinity using [3H]prazosin as radioligand against alpha-1A adrenergic receptor
ChEMBL 481 4 1 6 4.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5c(Cl)cccc54)c3=O)C[C@@H]21 10.1021/jm990567u
10297 26890 29 None -37 44 Rat 5.0 pKi = 5.0 Binding
Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (6.2 - 15)Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (6.2 - 15)
ChEMBL 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 10.1021/jm025550h
CHEMBL136560 26890 29 None -37 44 Rat 5.0 pKi = 5.0 Binding
Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (6.2 - 15)Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (6.2 - 15)
ChEMBL 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 10.1021/jm025550h
25070031 65039 10 None -4897 4 Human 5.0 pKi = 5.0 Binding
Inhibition of adrenergic alpha 1A receptorInhibition of adrenergic alpha 1A receptor
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1 10.1021/jm200401v
CHEMBL1829335 65039 10 None -4897 4 Human 5.0 pKi = 5.0 Binding
Inhibition of adrenergic alpha 1A receptorInhibition of adrenergic alpha 1A receptor
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1 10.1021/jm200401v
2477 732 54 None - 29 Bovine 8.3 pIC50 = 8.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 732 54 None - 29 Bovine 8.3 pIC50 = 8.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 732 54 None - 29 Bovine 8.3 pIC50 = 8.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 732 54 None - 29 Bovine 8.3 pIC50 = 8.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 732 54 None - 29 Bovine 8.3 pIC50 = 8.3 Binding
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
1816 2494 99 None - 17 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2494 99 None - 17 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2494 99 None - 17 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2494 99 None - 17 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2494 99 None - 17 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
9952220 97791 5 None - 4 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
Drug Central 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)[C@H]2C)cc1Cl None
CHEMBL274491 97791 5 None - 4 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
Drug Central 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)[C@H]2C)cc1Cl None
135 2486 38 None -40 58 Human 8.2 pIC50 = 8.2 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 None -40 58 Human 8.2 pIC50 = 8.2 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 None -40 58 Human 8.2 pIC50 = 8.2 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 None -40 58 Human 8.2 pIC50 = 8.2 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 None -40 58 Human 8.2 pIC50 = 8.2 Binding
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
135398737 942 89 None - 92 Bovine 8.2 pIC50 = 8.2 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 None - 92 Bovine 8.2 pIC50 = 8.2 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 None - 92 Bovine 8.2 pIC50 = 8.2 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 None - 92 Bovine 8.2 pIC50 = 8.2 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 None - 92 Bovine 8.2 pIC50 = 8.2 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5656 201368 82 None - 43 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
Drug Central 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 201368 82 None - 43 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
Drug Central 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
125017 9345 94 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
Drug Central 263 4 2 3 2.7 CN(C)CC(c1ccc(O)cc1)C1(O)CCCCC1 None
CHEMBL1118 9345 94 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
Drug Central 263 4 2 3 2.7 CN(C)CC(c1ccc(O)cc1)C1(O)CCCCC1 None
1353 1872 85 None - 86 Bovine 8.1 pIC50 = 8.1 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 None - 86 Bovine 8.1 pIC50 = 8.1 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 None - 86 Bovine 8.1 pIC50 = 8.1 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 None - 86 Bovine 8.1 pIC50 = 8.1 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 None - 86 Bovine 8.1 pIC50 = 8.1 Binding
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2435 3520 78 None - 49 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3520 78 None - 49 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3520 78 None - 49 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3520 78 None - 49 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3520 78 None - 49 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1427 1974 50 None - 27 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1974 50 None - 27 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1974 50 None - 27 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1974 50 None - 27 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1974 50 None - 27 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
102 4051 44 None -346 50 Human 8.2 pKd = 8.2 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 None -346 50 Human 8.2 pKd = 8.2 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 None -346 50 Human 8.2 pKd = 8.2 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 None -346 50 Human 8.2 pKd = 8.2 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 None -346 50 Human 8.2 pKd = 8.2 Binding
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptorInhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2803 939 53 None -3 19 Rat 8.2 pKd = 8.2 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 939 53 None -3 19 Rat 8.2 pKd = 8.2 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 939 53 None -3 19 Rat 8.2 pKd = 8.2 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 939 53 None -3 19 Rat 8.2 pKd = 8.2 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 939 53 None -3 19 Rat 8.2 pKd = 8.2 Binding
The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
1353 1872 85 None -10 86 Rat 8.1 pKd = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 None -10 86 Rat 8.1 pKd = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 None -10 86 Rat 8.1 pKd = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 None -10 86 Rat 8.1 pKd = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 None -10 86 Rat 8.1 pKd = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aortaBinding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
4106 2456 16 3H-PRAZOSIN -1 34 Pig 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2456 16 3H-PRAZOSIN -1 34 Pig 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2456 16 3H-PRAZOSIN -1 34 Pig 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2456 16 3H-PRAZOSIN -1 34 Pig 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
None 214169 0 3H-PRAZOSIN -5 20 Pig 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 421 9 1 6 4.3 COC1=C(C(=CC=C1)OC)OCCNCC2C(OC3=CC=CC=C3O2)C4=CC=CC=C4 None
4209 3102 71 3H-PRAZOSIN -2 34 Pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3102 71 3H-PRAZOSIN -2 34 Pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3102 71 3H-PRAZOSIN -2 34 Pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3102 71 3H-PRAZOSIN -2 34 Pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3102 71 3H-PRAZOSIN -2 34 Pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3102 71 3H-PRAZOSIN -2 34 Pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4106 2456 16 3H-PRAZOSIN -1 34 Pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2456 16 3H-PRAZOSIN -1 34 Pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2456 16 3H-PRAZOSIN -1 34 Pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2456 16 3H-PRAZOSIN -1 34 Pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
2389 3267 114 3H-PRAZOSIN -6 68 Pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 3H-PRAZOSIN -6 68 Pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 3H-PRAZOSIN -6 68 Pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 3H-PRAZOSIN -6 68 Pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 3H-PRAZOSIN -6 68 Pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
None 214169 0 3H-PRAZOSIN -5 20 Pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 421 9 1 6 4.3 COC1=C(C(=CC=C1)OC)OCCNCC2C(OC3=CC=CC=C3O2)C4=CC=CC=C4 None
4209 3102 71 3H-PRAZOSIN -2 34 Pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3102 71 3H-PRAZOSIN -2 34 Pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3102 71 3H-PRAZOSIN -2 34 Pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3102 71 3H-PRAZOSIN -2 34 Pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3102 71 3H-PRAZOSIN -2 34 Pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3102 71 3H-PRAZOSIN -2 34 Pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
489 145 22 3H-PRAZOSIN -8 13 Pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C None
5640 145 22 3H-PRAZOSIN -8 13 Pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C None
CHEMBL420060 145 22 3H-PRAZOSIN -8 13 Pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C None
489 145 22 3H-PRAZOSIN -8 13 Pig 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C None
5640 145 22 3H-PRAZOSIN -8 13 Pig 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C None
CHEMBL420060 145 22 3H-PRAZOSIN -8 13 Pig 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C None
2389 3267 114 3H-PRAZOSIN -6 68 Pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 3H-PRAZOSIN -6 68 Pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 3H-PRAZOSIN -6 68 Pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 3H-PRAZOSIN -6 68 Pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 3H-PRAZOSIN -6 68 Pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
463 1373 17 None 5 13 Human 8.0 pKi = 8 Binding
GRAC: human a1A selective antagonistGRAC: human a1A selective antagonist
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
6918097 1373 17 None 5 13 Human 8.0 pKi = 8 Binding
GRAC: human a1A selective antagonistGRAC: human a1A selective antagonist
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
837 1373 17 None 5 13 Human 8.0 pKi = 8 Binding
GRAC: human a1A selective antagonistGRAC: human a1A selective antagonist
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
CHEMBL2051956 1373 17 None 5 13 Human 8.0 pKi = 8 Binding
GRAC: human a1A selective antagonistGRAC: human a1A selective antagonist
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
DB14068 1373 17 None 5 13 Human 8.0 pKi = 8 Binding
GRAC: human a1A selective antagonistGRAC: human a1A selective antagonist
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
4209 3102 71 None -3 34 Rat 8.0 pKi = 8.0 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3102 71 None -3 34 Rat 8.0 pKi = 8.0 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3102 71 None -3 34 Rat 8.0 pKi = 8.0 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3102 71 None -3 34 Rat 8.0 pKi = 8.0 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3102 71 None -3 34 Rat 8.0 pKi = 8.0 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3102 71 None -3 34 Rat 8.0 pKi = 8.0 Binding
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4209 3102 71 None -2 34 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3102 71 None -2 34 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3102 71 None -2 34 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3102 71 None -2 34 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3102 71 None -2 34 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3102 71 None -2 34 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cellsDisplacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4151 3537 85 None 16 3 Human 8.0 pKi = 8.0 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
Drug Central 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N None
493 3537 85 None 16 3 Human 8.0 pKi = 8.0 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
Drug Central 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N None
5312125 3537 85 None 16 3 Human 8.0 pKi = 8.0 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
Drug Central 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N None
CHEMBL24778 3537 85 None 16 3 Human 8.0 pKi = 8.0 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
Drug Central 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N None
DB06207 3537 85 None 16 3 Human 8.0 pKi = 8.0 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
Drug Central 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N None
129211 3680 75 None -2 16 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
2562 3680 75 None -2 16 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
488 3680 75 None -2 16 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
CHEMBL836 3680 75 None -2 16 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
DB00706 3680 75 None -2 16 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
129211 3680 75 None -1 16 Human 8.0 pKi = 8.0 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
2562 3680 75 None -1 16 Human 8.0 pKi = 8.0 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
488 3680 75 None -1 16 Human 8.0 pKi = 8.0 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
CHEMBL836 3680 75 None -1 16 Human 8.0 pKi = 8.0 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
DB00706 3680 75 None -1 16 Human 8.0 pKi = 8.0 Binding
Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligandBinding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
484 2804 45 3H-PRAZOSIN -67 36 Pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2804 45 3H-PRAZOSIN -67 36 Pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2804 45 3H-PRAZOSIN -67 36 Pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
2470 3583 46 3H-PRAZOSIN -478 60 Pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-PRAZOSIN -478 60 Pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-PRAZOSIN -478 60 Pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-PRAZOSIN -478 60 Pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-PRAZOSIN -478 60 Pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
100 3733 52 3H-PRAZOSIN -20 56 Pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3733 52 3H-PRAZOSIN -20 56 Pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3733 52 3H-PRAZOSIN -20 56 Pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3733 52 3H-PRAZOSIN -20 56 Pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3733 52 3H-PRAZOSIN -20 56 Pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2389 3267 114 3H-PRAZOSIN -6 68 Pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 3H-PRAZOSIN -6 68 Pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 3H-PRAZOSIN -6 68 Pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 3H-PRAZOSIN -6 68 Pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 3H-PRAZOSIN -6 68 Pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
100 3733 52 3H-PRAZOSIN -20 56 Pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3733 52 3H-PRAZOSIN -20 56 Pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3733 52 3H-PRAZOSIN -20 56 Pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3733 52 3H-PRAZOSIN -20 56 Pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3733 52 3H-PRAZOSIN -20 56 Pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
None 214169 0 3H-PRAZOSIN -5 20 Pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 421 9 1 6 4.3 COC1=C(C(=CC=C1)OC)OCCNCC2C(OC3=CC=CC=C3O2)C4=CC=CC=C4 None
2726 904 64 3H-PRAZOSIN -20 73 Pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 904 64 3H-PRAZOSIN -20 73 Pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 904 64 3H-PRAZOSIN -20 73 Pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 904 64 3H-PRAZOSIN -20 73 Pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 904 64 3H-PRAZOSIN -20 73 Pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
124 2921 44 3H-PRAZOSIN -36 33 Pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2921 44 3H-PRAZOSIN -36 33 Pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2921 44 3H-PRAZOSIN -36 33 Pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2921 44 3H-PRAZOSIN -36 33 Pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2921 44 3H-PRAZOSIN -36 33 Pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
None 214479 0 3H-PRAZOSIN -2 4 Pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 609 10 1 8 6.0 CC1=C(C(C(=C(N1)C)C(=O)OCCCN2CCC(CC2)(C3=CC=CC=C3)C4=CC=CC=C4)C5=CC(=CC=C5)[N+](=O)[O-])C(=O)OC None
126225 94522 4 3H-PRAZOSIN -41 8 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 None
CHEMBL25467 94522 4 3H-PRAZOSIN -41 8 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 None
None 214479 0 3H-PRAZOSIN -2 4 Pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 609 10 1 8 6.0 CC1=C(C(C(=C(N1)C)C(=O)OCCCN2CCC(CC2)(C3=CC=CC=C3)C4=CC=CC=C4)C5=CC(=CC=C5)[N+](=O)[O-])C(=O)OC None
135398737 942 89 3H-PRAZOSIN -9 92 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-PRAZOSIN -9 92 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-PRAZOSIN -9 92 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-PRAZOSIN -9 92 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-PRAZOSIN -9 92 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
489 145 22 3H-PRAZOSIN -8 13 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C None
5640 145 22 3H-PRAZOSIN -8 13 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C None
CHEMBL420060 145 22 3H-PRAZOSIN -8 13 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C None
124 2921 44 3H-PRAZOSIN -36 33 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2921 44 3H-PRAZOSIN -36 33 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2921 44 3H-PRAZOSIN -36 33 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2921 44 3H-PRAZOSIN -36 33 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2921 44 3H-PRAZOSIN -36 33 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
None 214479 0 3H-PRAZOSIN -2 4 Pig 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 609 10 1 8 6.0 CC1=C(C(C(=C(N1)C)C(=O)OCCCN2CCC(CC2)(C3=CC=CC=C3)C4=CC=CC=C4)C5=CC(=CC=C5)[N+](=O)[O-])C(=O)OC None
100 3733 52 3H-PRAZOSIN -20 56 Pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3733 52 3H-PRAZOSIN -20 56 Pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3733 52 3H-PRAZOSIN -20 56 Pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3733 52 3H-PRAZOSIN -20 56 Pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3733 52 3H-PRAZOSIN -20 56 Pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1028 287 69 3H-PRAZOSIN -741 30 Pig 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 3H-PRAZOSIN -741 30 Pig 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 3H-PRAZOSIN -741 30 Pig 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 3H-PRAZOSIN -741 30 Pig 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 3H-PRAZOSIN -741 30 Pig 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 3H-PRAZOSIN -741 30 Pig 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
3016 1380 0 None 46 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
3364 1380 0 None 46 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
852 1380 0 None 46 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
CHEMBL12 1380 0 None 46 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
DB00829 1380 0 None 46 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
4508 3078 91 None 1 13 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
4866774 3078 91 None 1 13 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
509 3078 91 None 1 13 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
838 3078 91 None 1 13 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
CHEMBL1740 3078 91 None 1 13 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
162265 200578 19 None -5 45 Rat 8.3 pKi = 8.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
Drug Central 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 200578 19 None -5 45 Rat 8.3 pKi = 8.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
Drug Central 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 200578 19 None -5 45 Rat 8.3 pKi = 8.3 Binding
Binding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assayBinding affinity to alpha1A adrenoreceptor in Rattus norvegicus (rat) submaxillary gland by radioligand displacement assay
Drug Central 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
2470 3583 46 3H-PRAZOSIN -478 60 Pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-PRAZOSIN -478 60 Pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-PRAZOSIN -478 60 Pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-PRAZOSIN -478 60 Pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-PRAZOSIN -478 60 Pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
68712 99861 57 None -8 5 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 None
CHEMBL289480 99861 57 None -8 5 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 None
2146 3039 63 None -23 8 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
485 3039 63 None -23 8 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
6041 3039 63 None -23 8 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
CHEMBL1215 3039 63 None -23 8 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
DB00388 3039 63 None -23 8 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
2695 3768 76 None 9 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
5504 3768 76 None 9 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
7310 3768 76 None 9 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
CHEMBL770 3768 76 None 9 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
DB00797 3768 76 None 9 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
2435 713 98 None -21 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
395 713 98 None -21 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
520 713 98 None -21 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
5386 713 98 None -21 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
CHEMBL844 713 98 None -21 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
DB00484 713 98 None -21 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
1830 2542 39 None 2 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2542 39 None 2 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2542 39 None 2 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2542 39 None 2 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2542 39 None 2 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
2162 41258 97 None -3 6 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
Drug Central 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl None
CHEMBL1491 41258 97 None -3 6 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Alpha-1a adrenergic receptorBinding affinity against human Alpha-1a adrenergic receptor
Drug Central 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl None
446220 132985 13 None 19 46 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 132985 13 None 19 46 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1028 287 69 None -30 30 Human 8.2 pKi = 8.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 None -30 30 Human 8.2 pKi = 8.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 None -30 30 Human 8.2 pKi = 8.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 None -30 30 Human 8.2 pKi = 8.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 None -30 30 Human 8.2 pKi = 8.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 None -30 30 Human 8.2 pKi = 8.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
1960 2805 64 None -38 26 Human 8.2 pKi = 8.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2805 64 None -38 26 Human 8.2 pKi = 8.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2805 64 None -38 26 Human 8.2 pKi = 8.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2805 64 None -38 26 Human 8.2 pKi = 8.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2805 64 None -38 26 Human 8.2 pKi = 8.2 Binding
Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
126225 94522 4 3H-PRAZOSIN -41 8 Pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 None
CHEMBL25467 94522 4 3H-PRAZOSIN -41 8 Pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 None
484 2804 45 3H-PRAZOSIN -67 36 Pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2804 45 3H-PRAZOSIN -67 36 Pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2804 45 3H-PRAZOSIN -67 36 Pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
2146 3039 63 None -10 8 Bovine 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
485 3039 63 None -10 8 Bovine 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
6041 3039 63 None -10 8 Bovine 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
CHEMBL1215 3039 63 None -10 8 Bovine 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
DB00388 3039 63 None -10 8 Bovine 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
2202 3071 91 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3071 91 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3071 91 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3071 91 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3071 91 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
135398737 942 89 3H-PRAZOSIN -9 92 Pig 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-PRAZOSIN -9 92 Pig 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-PRAZOSIN -9 92 Pig 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-PRAZOSIN -9 92 Pig 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-PRAZOSIN -9 92 Pig 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1960 2805 64 None -10 26 Bovine 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2805 64 None -10 26 Bovine 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2805 64 None -10 26 Bovine 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2805 64 None -10 26 Bovine 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2805 64 None -10 26 Bovine 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
5284550 215967 0 None 1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC\C=C1/C2=CC=CC=C2CSC2=CC=CC=C12 None
2477 732 54 None 1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 732 54 None 1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 732 54 None 1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 732 54 None 1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 732 54 None 1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
37 764 56 None -18 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 764 56 None -18 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 764 56 None -18 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 764 56 None -18 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 764 56 None -18 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
66265 93566 12 None -1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 93566 12 None -1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
3151 1429 93 None -8 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 1429 93 None -8 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 1429 93 None -8 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 1429 93 None -8 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 1429 93 None -8 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
16362 3064 67 None -35 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3064 67 None -35 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3064 67 None -35 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3064 67 None -35 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3064 67 None -35 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
15387 214199 0 None 1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
68617 203806 60 None 3 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 203806 60 None 3 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 203806 60 None 3 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
2470 3583 46 3H-PRAZOSIN -478 60 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 3H-PRAZOSIN -478 60 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 3H-PRAZOSIN -478 60 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 3H-PRAZOSIN -478 60 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 3H-PRAZOSIN -478 60 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
126225 94522 4 3H-PRAZOSIN -41 8 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 None
CHEMBL25467 94522 4 3H-PRAZOSIN -41 8 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 None
135398737 942 89 3H-PRAZOSIN -9 92 Pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-PRAZOSIN -9 92 Pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-PRAZOSIN -9 92 Pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-PRAZOSIN -9 92 Pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-PRAZOSIN -9 92 Pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
484 2804 45 3H-PRAZOSIN -67 36 Pig 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2804 45 3H-PRAZOSIN -67 36 Pig 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2804 45 3H-PRAZOSIN -67 36 Pig 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
2995 202690 49 None 3 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 202690 49 None 3 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 202690 49 None 3 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
3947 214368 0 None -1 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1C2=CC=CC=C2CCC3=CC=CC=C31)CC(=O)C4=CC=C(C=C4)Cl None
3658 4032 47 None -9 8 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
517 4032 47 None -9 8 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5709 4032 47 None -9 8 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
CHEMBL312448 4032 47 None -9 8 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
DB06694 4032 47 None -9 8 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Alpha-1 adrenergic receptorBinding affinity towards human Alpha-1 adrenergic receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
2448 214174 0 None -5 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 419 6 1 3 4.5 C1CN(CCC1(C2=CC=C(C=C2)Br)O)CCCC(=O)C3=CC=C(C=C3)F None
21302490 112295 26 None -10 9 Human 8.2 pKi = 8.2 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3233142 112295 26 None -10 9 Human 8.2 pKi = 8.2 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3306803 112295 26 None -10 9 Human 8.2 pKi = 8.2 Binding
Inhibition of adrenergic alpha1A receptor (unknown origin)Inhibition of adrenergic alpha1A receptor (unknown origin)
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
242 467 117 None -14 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 None -14 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 None -14 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 None -14 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 None -14 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
125564 659 88 None -12 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
388 659 88 None -12 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
7670 659 88 None -12 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
CHEMBL178803 659 88 None -12 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
DB09223 659 88 None -12 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
4543 169972 36 None -1 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL1201156 169972 36 None -1 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL445 169972 36 None -1 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
2267 553 64 None -15 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
271 553 64 None -15 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
7121 553 64 None -15 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
CHEMBL639 553 64 None -15 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
DB00972 553 64 None -15 7 Human 8.1 pKi = 8.1 Binding
Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblastsBinding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
2267 553 64 None -15 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
271 553 64 None -15 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
7121 553 64 None -15 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
CHEMBL639 553 64 None -15 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
DB00972 553 64 None -15 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
135 2486 38 None -9 58 Bovine 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 None -9 58 Bovine 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 None -9 58 Bovine 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 None -9 58 Bovine 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 None -9 58 Bovine 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptorDisplacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
277 1269 55 None -20 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1269 55 None -20 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1269 55 None -20 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1269 55 None -20 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1269 55 None -20 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
3294 1967 106 None -10 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1967 106 None -10 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1967 106 None -10 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1967 106 None -10 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1967 106 None -10 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1613 2306 44 None -2 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2306 44 None -2 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2306 44 None -2 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2306 44 None -2 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2306 44 None -2 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
240 929 39 None -4 25 Rat 8.1 pKi = 8.1 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 929 39 None -4 25 Rat 8.1 pKi = 8.1 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 929 39 None -4 25 Rat 8.1 pKi = 8.1 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 929 39 None -4 25 Rat 8.1 pKi = 8.1 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 929 39 None -4 25 Rat 8.1 pKi = 8.1 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 929 39 None -4 25 Rat 8.1 pKi = 8.1 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 929 39 None -4 25 Rat 8.1 pKi = 8.1 Binding
The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brainThe ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
3584 3706 60 None -3 14 Bovine 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
5401 3706 60 None -3 14 Bovine 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
7302 3706 60 None -3 14 Bovine 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
CHEMBL611 3706 60 None -3 14 Bovine 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
DB01162 3706 60 None -3 14 Bovine 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
2274 3112 53 None -3 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3112 53 None -3 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3112 53 None -3 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3112 53 None -3 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3112 53 None -3 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
214 3787 52 None -9 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3787 52 None -9 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3787 52 None -9 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3787 52 None -9 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3787 52 None -9 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3787 52 None -9 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1225 1438 24 None -26 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1438 24 None -26 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1438 24 None -26 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1438 24 None -26 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1438 24 None -26 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
115 340 66 None -2 7 Bovine 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C None
2092 340 66 None -2 7 Bovine 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C None
7109 340 66 None -2 7 Bovine 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C None
CHEMBL709 340 66 None -2 7 Bovine 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C None
DB00346 340 66 None -2 7 Bovine 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C None
135398737 942 89 None -5 92 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 None -5 92 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 None -5 92 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 None -5 92 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 None -5 92 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398745 2858 108 None -39 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 None -39 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 None -39 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 None -39 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1890 2708 44 None -1 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
4449 2708 44 None -1 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
7247 2708 44 None -1 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
CHEMBL623 2708 44 None -1 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
DB01149 2708 44 None -1 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
2470 3583 46 None -316 60 Bovine 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 None -316 60 Bovine 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 None -316 60 Bovine 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 None -316 60 Bovine 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 None -316 60 Bovine 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
124 2921 44 None -14 33 Bovine 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2921 44 None -14 33 Bovine 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2921 44 None -14 33 Bovine 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2921 44 None -14 33 Bovine 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2921 44 None -14 33 Bovine 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2389 3267 114 None -7 68 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 None -7 68 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 None -7 68 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 None -7 68 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 None -7 68 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1353 1872 85 None -6 86 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 None -6 86 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 None -6 86 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 None -6 86 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 None -6 86 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1443 1989 30 None -2 11 Bovine 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
33625 1989 30 None -2 11 Bovine 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
501 1989 30 None -2 11 Bovine 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
CHEMBL279516 1989 30 None -2 11 Bovine 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
DB08950 1989 30 None -2 11 Bovine 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
212 3734 43 None -7 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3734 43 None -7 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3734 43 None -7 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3734 43 None -7 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3734 43 None -7 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2726 904 64 3H-PRAZOSIN -20 73 Pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 904 64 3H-PRAZOSIN -20 73 Pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 904 64 3H-PRAZOSIN -20 73 Pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 904 64 3H-PRAZOSIN -20 73 Pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 904 64 3H-PRAZOSIN -20 73 Pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
4106 2456 16 3H-PRAZOSIN -1 34 Pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2456 16 3H-PRAZOSIN -1 34 Pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2456 16 3H-PRAZOSIN -1 34 Pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2456 16 3H-PRAZOSIN -1 34 Pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
209 2996 94 None -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 2996 94 None -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 2996 94 None -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 2996 94 None -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 2996 94 None -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2865 4064 67 None -14 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4064 67 None -14 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4064 67 None -14 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4064 67 None -14 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4064 67 None -14 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
115 340 66 None -3 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
Drug Central 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C None
2092 340 66 None -3 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
Drug Central 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C None
7109 340 66 None -3 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
Drug Central 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C None
CHEMBL709 340 66 None -3 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
Drug Central 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C None
DB00346 340 66 None -3 7 Human 8.1 pKi = 8.1 Binding
Binding affinity against Alpha-1A adrenergic receptor from human cloneBinding affinity against Alpha-1A adrenergic receptor from human clone
Drug Central 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C None
2470 3583 46 None -208 60 Human 8.1 pKi = 8.1 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 None -208 60 Human 8.1 pKi = 8.1 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 None -208 60 Human 8.1 pKi = 8.1 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 None -208 60 Human 8.1 pKi = 8.1 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 None -208 60 Human 8.1 pKi = 8.1 Binding
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately activeBinding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
135398737 942 89 None -5 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 None -5 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 None -5 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 None -5 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 None -5 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2470 3583 46 None -398 60 Rat 8.1 pKi = 8.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3583 46 None -398 60 Rat 8.1 pKi = 8.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3583 46 None -398 60 Rat 8.1 pKi = 8.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3583 46 None -398 60 Rat 8.1 pKi = 8.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3583 46 None -398 60 Rat 8.1 pKi = 8.1 Binding
Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary glandOverall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
103 4074 56 None -6 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4074 56 None -6 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4074 56 None -6 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4074 56 None -6 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4074 56 None -6 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2142 3035 54 None -1 37 Bovine 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3035 54 None -1 37 Bovine 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3035 54 None -1 37 Bovine 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3035 54 None -1 37 Bovine 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3035 54 None -1 37 Bovine 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3035 54 None -1 37 Bovine 8.1 pKi = 8.1 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
1212 1624 45 None -16 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1624 45 None -16 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1624 45 None -16 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1624 45 None -16 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1624 45 None -16 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
124 2921 44 None -13 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2921 44 None -13 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2921 44 None -13 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2921 44 None -13 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2921 44 None -13 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
3389 215972 0 None -1 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
463 1373 17 None -7 13 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
6918097 1373 17 None -7 13 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
837 1373 17 None -7 13 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
CHEMBL2051956 1373 17 None -7 13 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
DB14068 1373 17 None -7 13 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
1524 2141 89 None -5 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2141 89 None -5 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2141 89 None -5 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2141 89 None -5 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2141 89 None -5 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2141 89 None -5 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
124 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2284 3121 27 None -3 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3121 27 None -3 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3121 27 None -3 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3121 27 None -3 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3121 27 None -3 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
1588 2284 24 None -26 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2284 24 None -26 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2284 24 None -26 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2284 24 None -26 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2284 24 None -26 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
31101 719 39 None -12 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 719 39 None -12 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 719 39 None -12 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 719 39 None -12 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 719 39 None -12 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
2142 3035 54 None -2 37 Human 8.1 pKi = 8.1 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3035 54 None -2 37 Human 8.1 pKi = 8.1 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3035 54 None -2 37 Human 8.1 pKi = 8.1 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3035 54 None -2 37 Human 8.1 pKi = 8.1 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3035 54 None -2 37 Human 8.1 pKi = 8.1 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3035 54 None -2 37 Human 8.1 pKi = 8.1 Binding
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cellsBinding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
11978813 712 72 None -10 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 712 72 None -10 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 712 72 None -10 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 712 72 None -10 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 712 72 None -10 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
4418 33985 80 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 None
CHEMBL142635 33985 80 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 None
1443 1989 30 None 1 11 Human 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
33625 1989 30 None 1 11 Human 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
501 1989 30 None 1 11 Human 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
CHEMBL279516 1989 30 None 1 11 Human 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
DB08950 1989 30 None 1 11 Human 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
102 4051 44 None -85 50 Bovine 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4051 44 None -85 50 Bovine 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4051 44 None -85 50 Bovine 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4051 44 None -85 50 Bovine 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4051 44 None -85 50 Bovine 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2801 161313 56 None 1 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL1200710 161313 56 None 1 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL415 161313 56 None 1 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
2601 3709 30 None -5 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3709 30 None -5 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3709 30 None -5 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3709 30 None -5 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3709 30 None -5 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
2389 3267 114 None -14 68 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 None -14 68 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 None -14 68 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 None -14 68 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 None -14 68 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
115237 55281 113 None -36 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55281 113 None -36 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
2585 788 100 None -14 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 788 100 None -14 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 788 100 None -14 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 788 100 None -14 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 788 100 None -14 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
5440 215991 0 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 399 6 0 5 5.0 CCSC1=CC=C2SC3=CC=CC=C3N(CCCN3CCN(C)CC3)C2=C1 None
2435 3520 78 None -16 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3520 78 None -16 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3520 78 None -16 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3520 78 None -16 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3520 78 None -16 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
3157 1437 69 None -2 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
7170 1437 69 None -2 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
954 1437 69 None -2 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
CHEMBL707 1437 69 None -2 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
DB00590 1437 69 None -2 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
5639 98425 70 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 None
CHEMBL279229 98425 70 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 None
46780481 107032 18 None -52 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107032 18 None -52 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107032 18 None -52 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107032 18 None -52 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
3584 3706 60 None -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
5401 3706 60 None -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
7302 3706 60 None -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
CHEMBL611 3706 60 None -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
DB01162 3706 60 None -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
3584 3706 60 None -2 14 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
5401 3706 60 None -2 14 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
7302 3706 60 None -2 14 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
CHEMBL611 3706 60 None -2 14 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
DB01162 3706 60 None -2 14 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1AIn vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
1238 201475 21 None -3 17 Bovine 8.0 pKi = 8.0 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 201475 21 None -3 17 Bovine 8.0 pKi = 8.0 Binding
Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cellsDisplacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
2865 4064 67 None -4 54 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4064 67 None -4 54 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4064 67 None -4 54 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4064 67 None -4 54 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4064 67 None -4 54 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cellsDisplacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
463 1373 17 None -8 13 Bovine 8.0 pKi = 8.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
6918097 1373 17 None -8 13 Bovine 8.0 pKi = 8.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
837 1373 17 None -8 13 Bovine 8.0 pKi = 8.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
CHEMBL2051956 1373 17 None -8 13 Bovine 8.0 pKi = 8.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
DB14068 1373 17 None -8 13 Bovine 8.0 pKi = 8.0 Binding
Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligandBinding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
2435 3520 78 None -3 49 Bovine 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3520 78 None -3 49 Bovine 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3520 78 None -3 49 Bovine 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3520 78 None -3 49 Bovine 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3520 78 None -3 49 Bovine 8.0 pKi = 8.0 Binding
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cellsDisplacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
4209 3102 71 None -4 34 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3102 71 None -4 34 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3102 71 None -4 34 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3102 71 None -4 34 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3102 71 None -4 34 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3102 71 None -4 34 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against Alpha-1A adrenergic receptor from bovine cloneBinding affinity against Alpha-1A adrenergic receptor from bovine clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
129211 3680 75 None -7 16 Bovine 8.0 pKi = 8 Binding
NoneNone
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
2562 3680 75 None -7 16 Bovine 8.0 pKi = 8 Binding
NoneNone
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
488 3680 75 None -7 16 Bovine 8.0 pKi = 8 Binding
NoneNone
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
CHEMBL836 3680 75 None -7 16 Bovine 8.0 pKi = 8 Binding
NoneNone
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
DB00706 3680 75 None -7 16 Bovine 8.0 pKi = 8 Binding
NoneNone
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
4151 3537 85 None 16 3 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 32608144
4151 3537 85 None 16 3 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 7651358
493 3537 85 None 16 3 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 32608144
493 3537 85 None 16 3 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 7651358
5312125 3537 85 None 16 3 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 32608144
5312125 3537 85 None 16 3 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 7651358
CHEMBL24778 3537 85 None 16 3 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 32608144
CHEMBL24778 3537 85 None 16 3 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 7651358
DB06207 3537 85 None 16 3 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 32608144
DB06207 3537 85 None 16 3 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 7651358
129211 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10334511
129211 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10369480
129211 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 32608144
129211 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 7651358
129211 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 9249248
129211 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 9490024
2562 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10334511
2562 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10369480
2562 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 32608144
2562 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 7651358
2562 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 9249248
2562 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 9490024
488 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10334511
488 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10369480
488 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 32608144
488 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 7651358
488 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 9249248
488 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 9490024
CHEMBL836 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10334511
CHEMBL836 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10369480
CHEMBL836 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 32608144
CHEMBL836 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 7651358
CHEMBL836 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 9249248
CHEMBL836 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 9490024
DB00706 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10334511
DB00706 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10369480
DB00706 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 32608144
DB00706 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 7651358
DB00706 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 9249248
DB00706 3680 75 None -1 16 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 9490024
247704 288 26 None -10 5 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@H](c1ccc(c(c1)O)O)O 7651358
4450 288 26 None -10 5 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@H](c1ccc(c(c1)O)O)O 7651358
CHEMBL42280 288 26 None -10 5 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@H](c1ccc(c(c1)O)O)O 7651358
507 3264 0 None -2511 2 Rat 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12824165
1753 2458 26 None -7 5 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10433504
1753 2458 26 None -7 5 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 7651358
483 2458 26 None -7 5 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10433504
483 2458 26 None -7 5 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 7651358
6082 2458 26 None -7 5 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10433504
6082 2458 26 None -7 5 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 7651358
CHEMBL524 2458 26 None -7 5 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10433504
CHEMBL524 2458 26 None -7 5 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 7651358
DB00723 2458 26 None -7 5 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10433504
DB00723 2458 26 None -7 5 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 7651358
2146 3039 63 None -23 8 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10433504
485 3039 63 None -23 8 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10433504
6041 3039 63 None -23 8 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10433504
CHEMBL1215 3039 63 None -23 8 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10433504
DB00388 3039 63 None -23 8 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10433504
1960 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10433504
1960 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 20978120
1960 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 28444738
1960 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 34355529
1960 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 7651358
1960 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 8564227
439260 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10433504
439260 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 20978120
439260 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 28444738
439260 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 34355529
439260 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 7651358
439260 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 8564227
505 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10433504
505 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 20978120
505 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 28444738
505 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 34355529
505 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 7651358
505 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 8564227
CHEMBL1437 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10433504
CHEMBL1437 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 20978120
CHEMBL1437 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 28444738
CHEMBL1437 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 34355529
CHEMBL1437 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 7651358
CHEMBL1437 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 8564227
DB00368 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10433504
DB00368 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 20978120
DB00368 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 28444738
DB00368 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 34355529
DB00368 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 7651358
DB00368 2805 64 None -38 26 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 8564227
1028 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 34355529
1028 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 7651358
1028 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 8564227
139148732 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 34355529
139148732 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 7651358
139148732 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 8564227
479 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 34355529
479 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 7651358
479 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 8564227
5816 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 34355529
5816 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 7651358
5816 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 8564227
CHEMBL679 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 34355529
CHEMBL679 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 7651358
CHEMBL679 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 8564227
DB00668 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 34355529
DB00668 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 7651358
DB00668 287 69 None -30 30 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 8564227
216249 1273 44 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 14678390
3469 1273 44 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 14678390
CHEMBL257978 1273 44 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 14678390
10453764 2158 0 None -1 3 Rat 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 402 4 0 8 0.9 Clc1ccccc1N1CCN(CC1)CCn1cnc2c1c(=O)n(C)c(=O)n2C 17639498
8896 2158 0 None -1 3 Rat 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 402 4 0 8 0.9 Clc1ccccc1N1CCN(CC1)CCn1cnc2c1c(=O)n(C)c(=O)n2C 17639498
115 340 66 None -3 7 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10812954
115 340 66 None -3 7 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 32608144
2092 340 66 None -3 7 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10812954
2092 340 66 None -3 7 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 32608144
7109 340 66 None -3 7 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10812954
7109 340 66 None -3 7 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 32608144
CHEMBL709 340 66 None -3 7 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10812954
CHEMBL709 340 66 None -3 7 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 32608144
DB00346 340 66 None -3 7 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10812954
DB00346 340 66 None -3 7 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 32608144
124 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10433504
124 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7651358
124 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 8564227
124 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 8719417
2032 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10433504
2032 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7651358
2032 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 8564227
2032 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 8719417
4636 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10433504
4636 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7651358
4636 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 8564227
4636 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 8719417
CHEMBL762 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10433504
CHEMBL762 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7651358
CHEMBL762 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 8564227
CHEMBL762 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 8719417
DB00935 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10433504
DB00935 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7651358
DB00935 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 8564227
DB00935 2921 44 None -14 33 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 8719417
3584 3706 60 None -2 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 32608144
3584 3706 60 None -2 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 9379432
5401 3706 60 None -2 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 32608144
5401 3706 60 None -2 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 9379432
7302 3706 60 None -2 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 32608144
7302 3706 60 None -2 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 9379432
CHEMBL611 3706 60 None -2 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 32608144
CHEMBL611 3706 60 None -2 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 9379432
DB01162 3706 60 None -2 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 32608144
DB01162 3706 60 None -2 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 9379432
2142 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 32608144
2142 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7651358
4920903 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 32608144
4920903 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7651358
502 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 32608144
502 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7651358
5775 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 32608144
5775 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7651358
CHEMBL597 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 32608144
CHEMBL597 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7651358
DB00692 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 32608144
DB00692 3035 54 None -2 37 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7651358
3894573 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10334511
3894573 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 32608144
3894573 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 8632751
3894573 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 9249248
3894573 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 9490024
495 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10334511
495 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 32608144
495 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 8632751
495 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 9249248
495 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 9490024
CHEMBL88272 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 10334511
CHEMBL88272 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 32608144
CHEMBL88272 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 8632751
CHEMBL88272 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 9249248
CHEMBL88272 3329 4 None -1 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 10 2 3 5.6 Clc1ccc2c(c1)c(c[nH]2)CC(NCCOc1ccccc1OCC1CC1)(C)C 9490024
3157 1437 69 None -2 12 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 32608144
7170 1437 69 None -2 12 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 32608144
954 1437 69 None -2 12 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 32608144
CHEMBL707 1437 69 None -2 12 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 32608144
DB00590 1437 69 None -2 12 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 32608144
498 3561 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 608 10 2 7 5.6 COC(=O)C1=C(C)NC(=C([C@H]1c1ccc(cc1)[N+](=O)[O-])C(=O)NCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10812954
498 3561 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 608 10 2 7 5.6 COC(=O)C1=C(C)NC(=C([C@H]1c1ccc(cc1)[N+](=O)[O-])C(=O)NCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 32608144
498 3561 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 608 10 2 7 5.6 COC(=O)C1=C(C)NC(=C([C@H]1c1ccc(cc1)[N+](=O)[O-])C(=O)NCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 7752182
498 3561 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 608 10 2 7 5.6 COC(=O)C1=C(C)NC(=C([C@H]1c1ccc(cc1)[N+](=O)[O-])C(=O)NCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 9190863
5311437 3561 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 608 10 2 7 5.6 COC(=O)C1=C(C)NC(=C([C@H]1c1ccc(cc1)[N+](=O)[O-])C(=O)NCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10812954
5311437 3561 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 608 10 2 7 5.6 COC(=O)C1=C(C)NC(=C([C@H]1c1ccc(cc1)[N+](=O)[O-])C(=O)NCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 32608144
5311437 3561 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 608 10 2 7 5.6 COC(=O)C1=C(C)NC(=C([C@H]1c1ccc(cc1)[N+](=O)[O-])C(=O)NCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 7752182
5311437 3561 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 608 10 2 7 5.6 COC(=O)C1=C(C)NC(=C([C@H]1c1ccc(cc1)[N+](=O)[O-])C(=O)NCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 9190863
6663 3262 0 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20015090
6663 3262 0 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 23935897
4209 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10334511
4209 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10369480
4209 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 32608144
4209 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7651358
4209 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9249248
4209 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9490024
4893 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10334511
4893 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10369480
4893 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 32608144
4893 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7651358
4893 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9249248
4893 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9490024
503 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10334511
503 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10369480
503 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 32608144
503 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7651358
503 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9249248
503 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9490024
5385 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10334511
5385 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10369480
5385 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 32608144
5385 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7651358
5385 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9249248
5385 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9490024
CHEMBL2 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10334511
CHEMBL2 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10369480
CHEMBL2 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 32608144
CHEMBL2 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7651358
CHEMBL2 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9249248
CHEMBL2 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9490024
DB00457 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10334511
DB00457 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10369480
DB00457 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 32608144
DB00457 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7651358
DB00457 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9249248
DB00457 3102 71 None -2 34 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 9490024
487 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 32608144
487 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 7651358
487 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 9249248
60602 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 32608144
60602 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 7651358
60602 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 9249248
CHEMBL405355 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 32608144
CHEMBL405355 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 7651358
CHEMBL405355 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 9249248
DB09239 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 32608144
DB09239 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 7651358
DB09239 3564 17 None -1 12 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 9249248
3567002 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 10369480
3567002 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 32608144
7381 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 10369480
7381 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 32608144
CHEMBL56331 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 10369480
CHEMBL56331 3323 5 None 58 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 6 2.0 O=c1[nH]cc(c(=O)n1CCCN1CCN(CC1)c1ccccc1OCC(F)(F)F)C 32608144
444 214235 0 None 6 18 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 239 3 1 2 3.3 CC(C(=O)C1=CC(=CC=C1)Cl)NC(C)(C)C None
146570 43193 60 None 1 4 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1508 43193 60 None 1 4 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
228 441 26 None -1 24 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 441 26 None -1 24 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 441 26 None -1 24 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 441 26 None -1 24 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 441 26 None -1 24 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
1209 1620 69 None -1 32 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1620 69 None -1 32 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1620 69 None -1 32 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1620 69 None -1 32 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1620 69 None -1 32 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2105 2993 34 None -9 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 2993 34 None -9 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 2993 34 None -9 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 2993 34 None -9 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 2993 34 None -9 33 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
2803 939 53 None -8 19 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 939 53 None -8 19 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 939 53 None -8 19 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 939 53 None -8 19 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 939 53 None -8 19 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
3337 214431 0 None 13 41 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 None 13 41 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 None 13 41 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 None 13 41 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
521 1372 64 None -16 7 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
5311068 1372 64 None -16 7 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
835 1372 64 None -16 7 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
CHEMBL778 1372 64 None -16 7 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
DB00633 1372 64 None -16 7 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
2726 904 64 None -5 73 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 904 64 None -5 73 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 904 64 None -5 73 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 904 64 None -5 73 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 904 64 None -5 73 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
4431 2679 18 None 1 12 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 11459121
73 2679 18 None 1 12 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 11459121
CHEMBL8618 2679 18 None 1 12 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 11459121
499 4002 15 None -1 15 Rat 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 11331292
5685 4002 15 None -1 15 Rat 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 11331292
CHEMBL25554 4002 15 None -1 15 Rat 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 11331292
2202 3071 91 None -2 21 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
4850 3071 91 None -2 21 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
49 3071 91 None -2 21 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
CHEMBL1371770 3071 91 None -2 21 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
DB12478 3071 91 None -2 21 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
481 2836 5 None 4 3 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 8719417
9838763 2836 5 None 4 3 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 8719417
CHEMBL72958 2836 5 None 4 3 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 8719417
37 764 56 None -18 17 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 764 56 None -18 17 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 764 56 None -18 17 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 764 56 None -18 17 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 764 56 None -18 17 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
2419 687 22 None -275 12 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 11354357
2419 687 22 None -275 12 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 11459121
9 687 22 None -275 12 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 11354357
9 687 22 None -275 12 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 11459121
CHEMBL13647 687 22 None -275 12 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 11354357
CHEMBL13647 687 22 None -275 12 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 11459121
2419 687 22 None -288 12 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 11354357
9 687 22 None -288 12 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 11354357
CHEMBL13647 687 22 None -288 12 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 5 0 5 2.5 COc1ccccc1N1CCN(CC1)CCN1C(=O)CC2(CC1=O)CCCC2 11354357
5268 3586 34 None -158 18 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 11459121
53 3586 34 None -158 18 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 11459121
CHEMBL300555 3586 34 None -158 18 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 11459121
277 1269 55 None -20 46 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 11459121
2913 1269 55 None -20 46 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 11459121
765 1269 55 None -20 46 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 11459121
CHEMBL516 1269 55 None -20 46 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 11459121
DB00434 1269 55 None -20 46 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 11459121
135 2486 38 None -40 58 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 11459121
1796 2486 38 None -40 58 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 11459121
4184 2486 38 None -40 58 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 11459121
CHEMBL6437 2486 38 None -40 58 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 11459121
DB06148 2486 38 None -40 58 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 11459121
132266 1247 9 None -48 9 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 8917649
486 1247 9 None -48 9 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 8917649
CHEMBL423294 1247 9 None -48 9 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 8917649
135398737 942 89 None -5 92 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11459121
38 942 89 None -5 92 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11459121
722 942 89 None -5 92 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11459121
CHEMBL42 942 89 None -5 92 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11459121
DB00363 942 89 None -5 92 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11459121
2142 3035 54 None -2 37 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 11331292
4920903 3035 54 None -2 37 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 11331292
502 3035 54 None -2 37 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 11331292
5775 3035 54 None -2 37 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 11331292
CHEMBL597 3035 54 None -2 37 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 11331292
DB00692 3035 54 None -2 37 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 11331292
1524 2141 89 None -5 52 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 11459121
197 2141 89 None -5 52 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 11459121
3822 2141 89 None -5 52 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 11459121
88 2141 89 None -5 52 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 11459121
CHEMBL51 2141 89 None -5 52 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 11459121
DB12465 2141 89 None -5 52 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 11459121
1588 2284 24 None -26 44 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864 2284 24 None -26 44 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
43 2284 24 None -26 44 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL157138 2284 24 None -26 44 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB00589 2284 24 None -26 44 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
2470 3583 46 None -208 60 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 11459121
3300 3583 46 None -208 60 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 11459121
5265 3583 46 None -208 60 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 11459121
99 3583 46 None -208 60 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 11459121
CHEMBL267930 3583 46 None -208 60 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 11459121
491 191 4 None -50 12 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 11354357
9891167 191 4 None -50 12 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 11354357
CHEMBL13856 191 4 None -50 12 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 11354357
1443 1989 30 None 1 11 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10334511
1443 1989 30 None 1 11 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 9249248
33625 1989 30 None 1 11 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10334511
33625 1989 30 None 1 11 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 9249248
501 1989 30 None 1 11 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10334511
501 1989 30 None 1 11 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 9249248
CHEMBL279516 1989 30 None 1 11 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10334511
CHEMBL279516 1989 30 None 1 11 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 9249248
DB08950 1989 30 None 1 11 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10334511
DB08950 1989 30 None 1 11 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 9249248
2389 3267 114 None -14 68 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 11459121
5073 3267 114 None -14 68 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 11459121
96 3267 114 None -14 68 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 11459121
CHEMBL85 3267 114 None -14 68 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 11459121
DB00734 3267 114 None -14 68 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 11459121
5074 3268 75 None -7 30 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11459121
97 3268 75 None -7 30 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11459121
CHEMBL267777 3268 75 None -7 30 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11459121
DB12693 3268 75 None -7 30 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11459121
491 191 4 None -44 12 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 11354357
9891167 191 4 None -44 12 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 11354357
CHEMBL13856 191 4 None -44 12 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 11354357
2601 3709 30 None -5 21 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
443951 3709 30 None -5 21 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
56 3709 30 None -5 21 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL73151 3709 30 None -5 21 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB13399 3709 30 None -5 21 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
490 190 5 None -25 12 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 11354357
490 190 5 None -36 12 Rat 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 11354357
9890547 190 5 None -25 12 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 11354357
9890547 190 5 None -36 12 Rat 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 11354357
CHEMBL268758 190 5 None -25 12 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 11354357
CHEMBL268758 190 5 None -36 12 Rat 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 11354357
219050 3309 21 None -15 21 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
52 3309 21 None -15 21 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
CHEMBL431367 3309 21 None -15 21 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
497 3301 6 None 61 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10369480
9872515 3301 6 None 61 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10369480
CHEMBL24777 3301 6 None 61 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 7 1 6 2.1 Fc1ccc(c(c1)OCC(F)(F)F)N1CCN(CC1)CCCn1c(=O)[nH]cc(c1=O)C 10369480
489 145 22 None -2 13 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 11331292
5640 145 22 None -2 13 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 11331292
CHEMBL420060 145 22 None -2 13 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 11331292
489 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 11459121
489 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 7651358
489 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 8764344
489 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 9249248
489 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 9490024
5640 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 11459121
5640 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 7651358
5640 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 8764344
5640 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 9249248
5640 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 9490024
CHEMBL420060 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 11459121
CHEMBL420060 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 7651358
CHEMBL420060 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 8764344
CHEMBL420060 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 9249248
CHEMBL420060 145 22 None -3 13 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 9490024
487 3564 17 None -4 12 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 11331292
60602 3564 17 None -4 12 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 11331292
CHEMBL405355 3564 17 None -4 12 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 11331292
DB09239 3564 17 None -4 12 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 11331292
4209 3102 71 None -3 34 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 11331292
4893 3102 71 None -3 34 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 11331292
503 3102 71 None -3 34 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 11331292
5385 3102 71 None -3 34 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 11331292
CHEMBL2 3102 71 None -3 34 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 11331292
DB00457 3102 71 None -3 34 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 11331292
148842 3871 21 None 8 5 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 9249248
496 3871 21 None 8 5 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 9249248
CHEMBL278865 3871 21 None 8 5 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C 9249248
499 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10334511
499 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7651358
499 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 9249248
499 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 9490024
5685 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10334511
5685 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7651358
5685 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 9249248
5685 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 9490024
CHEMBL25554 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10334511
CHEMBL25554 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7651358
CHEMBL25554 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 9249248
CHEMBL25554 4002 15 None 1 15 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 9490024