Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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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
44354055 114697 0 None - 1 Human 8.0 pEC50 = 8 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1041 20 8 8 2.8 COc1c(I)cc(C[C@H](NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1I 10.1021/jm00020a029
CHEMBL334510 114697 0 None - 1 Human 8.0 pEC50 = 8 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1041 20 8 8 2.8 COc1c(I)cc(C[C@H](NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1I 10.1021/jm00020a029
CHEMBL1556461 207050 0 None - 1 Human 8.0 pEC50 = 8 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00020a029
11803290 106154 0 None - 1 Human 7.0 pEC50 = 7 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143277 106154 0 None - 1 Human 7.0 pEC50 = 7 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
9962227 99169 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 763 18 9 8 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284285 99169 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 763 18 9 8 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280767 114073 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 577 15 9 8 -1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33377 114073 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 577 15 9 8 -1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9960837 115021 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 629 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33532 115021 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 629 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL115543 206751 16 None - 1 Human 6.0 pEC50 = 6 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL407378 210901 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm00020a029
44281172 99200 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 589 15 9 9 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1cccs1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284474 99200 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 589 15 9 9 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1cccs1)C(N)=O 10.1016/s0960-894x(99)00197-3
9875337 98777 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2Cl)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL281753 98777 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2Cl)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
10461499 23809 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 617 20 8 7 -0.9 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL133808 23809 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 617 20 8 7 -0.9 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL337126 209836 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280949 102228 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 651 15 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc2c(c1)-c1ccccc1-2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL30484 102228 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 651 15 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc2c(c1)-c1ccccc1-2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9851501 116708 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33946 116708 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL336623 209829 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CN)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280660 99403 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 617 15 7 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285915 99403 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 617 15 7 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL131912 206945 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280685 99277 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 585 15 7 8 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csnn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285018 99277 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 585 15 7 8 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csnn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL132849 206959 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL132292 206949 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280899 114274 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33394 114274 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281047 167253 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 752 18 10 8 2.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2c[nH]c3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL430734 167253 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 752 18 10 8 2.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2c[nH]c3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44354285 22482 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1147 26 12 10 0.3 C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)NC(Cc1cc(I)c(O)c(I)c1)C(N)=O 10.1021/jm00020a029
CHEMBL132734 22482 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1147 26 12 10 0.3 C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)NC(Cc1cc(I)c(O)c(I)c1)C(N)=O 10.1021/jm00020a029
44354055 114697 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1041 20 8 8 2.8 COc1c(I)cc(C[C@H](NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1I 10.1021/jm00020a029
CHEMBL334510 114697 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1041 20 8 8 2.8 COc1c(I)cc(C[C@H](NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1I 10.1021/jm00020a029
CHEMBL130147 206933 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL1556461 207050 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00020a029
44280608 99628 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 731 18 9 8 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(F)=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287468 99628 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 731 18 9 8 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(F)=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL2431718 208707 0 None 44 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human PAR1 expressed in African green monkey COS7 cells assessed as stimulation of inositol triphosphate productionAgonist activity at human PAR1 expressed in African green monkey COS7 cells assessed as stimulation of inositol triphosphate production
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C 10.1021/jm400638v
10747898 106204 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143683 106204 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44826172 99513 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc([N+](=O)[O-])c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286648 99513 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc([N+](=O)[O-])c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44826171 116353 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2[N+](=O)[O-])n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33818 116353 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2[N+](=O)[O-])n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL134081 206973 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL33473 209644 18 None - 1 Human 6.7 pEC50 = 6.7 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm00020a029
CHEMBL335845 209810 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280804 99203 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284498 99203 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL263369 208816 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm00020a029
44280877 116358 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 589 15 9 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33820 116358 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 589 15 9 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1016/s0960-894x(99)00197-3
9875040 113912 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 713 18 9 8 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33318 113912 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 713 18 9 8 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL337502 209841 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None COc1ccc(C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm00020a029
44280935 99614 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc(Cl)c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287368 99614 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc(Cl)c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL133789 206970 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm00020a029
44281237 116216 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 604 16 7 6 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33742 116216 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 604 16 7 6 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
90663359 106175 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 761 21 8 7 0.8 CC(=O)NCCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143325 106175 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 761 21 8 7 0.8 CC(=O)NCCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL334746 209645 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(Cl)c(Cl)c1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL33473 209644 18 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1016/s0960-894x(99)00197-3
44280607 167277 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 789 19 9 8 3.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(=C/c2ccccc2)c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL430930 167277 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 789 19 9 8 3.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(=C/c2ccccc2)c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL130930 206938 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
9810477 98308 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 719 18 9 9 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccs2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL278216 98308 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 719 18 9 9 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccs2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281081 119185 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34738 119185 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44354323 24064 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1021 26 12 10 -0.4 C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)NC(Cc1ccc(O)c(I)c1)C(N)=O 10.1021/jm00020a029
CHEMBL134036 24064 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1021 26 12 10 -0.4 C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)NC(Cc1ccc(O)c(I)c1)C(N)=O 10.1021/jm00020a029
CHEMBL334746 209645 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(Cl)c(Cl)c1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280768 116659 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 569 14 9 8 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(99)00197-3
CHEMBL33940 116659 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 569 14 9 8 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(99)00197-3
CHEMBL434623 211901 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL264249 208855 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00020a029
CHEMBL3143260 209391 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10461499 23809 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 617 20 8 7 -0.9 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL133808 23809 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 617 20 8 7 -0.9 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
11803426 106203 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 793 20 10 7 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143682 106203 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 793 20 10 7 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
9937578 99482 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 555 15 7 8 0.3 NCCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286430 99482 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 555 15 7 8 0.3 NCCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL133837 206971 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL263319 208812 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280822 116032 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 594 15 8 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1nccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33629 116032 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 594 15 8 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1nccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9895920 99545 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 656 15 7 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cncc(Br)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286837 99545 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 656 15 7 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cncc(Br)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281079 116704 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(Cl)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33945 116704 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(Cl)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280955 118774 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 611 15 8 6 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc2[nH]cnc2c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34387 118774 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 611 15 8 6 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc2[nH]cnc2c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL2370701 208162 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm00020a029
CHEMBL337490 209840 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(Cl)c(Cl)c1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280651 114921 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 781 18 9 8 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33506 114921 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 781 18 9 8 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9961058 99476 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 645 15 7 7 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(=O)c2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286382 99476 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 645 15 7 7 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(=O)c2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280650 114608 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(Cl)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33435 114608 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(Cl)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280649 112147 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 743 19 8 9 1.3 COc1ccc(/C=C/C(=O)Nc2n[nH]c(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n2)cc1 10.1016/s0960-894x(99)00197-3
CHEMBL33033 112147 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 743 19 8 9 1.3 COc1ccc(/C=C/C(=O)Nc2n[nH]c(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n2)cc1 10.1016/s0960-894x(99)00197-3
44280667 102460 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 738 18 9 9 1.4 N#Cc1ccc(/C=C/C(=O)Nc2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n[nH]2)cc1 10.1016/s0960-894x(99)00197-3
CHEMBL30635 102460 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 738 18 9 9 1.4 N#Cc1ccc(/C=C/C(=O)Nc2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n[nH]2)cc1 10.1016/s0960-894x(99)00197-3
CHEMBL3143259 209390 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663347 106172 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 781 21 8 9 0.9 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)O 10.1021/jm960455s
CHEMBL3143312 106172 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 781 21 8 9 0.9 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)O 10.1021/jm960455s
CHEMBL133449 206967 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL130058 206932 1 None - 1 Human 4.2 pEC50 = 4.2 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(N)=O 10.1021/jm00020a029
CHEMBL2370948 208210 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL None None None COc1ccc(C[C@H](NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
9808447 102429 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 583 15 9 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL30612 102429 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 583 15 9 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280585 116465 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 727 18 8 8 1.7 C/C(=C\c1ccccc1)C(=O)Nc1n[nH]c(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)n1 10.1016/s0960-894x(99)00197-3
CHEMBL33873 116465 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 727 18 8 8 1.7 C/C(=C\c1ccccc1)C(=O)Nc1n[nH]c(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)n1 10.1016/s0960-894x(99)00197-3
44280936 116007 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 731 18 9 8 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33617 116007 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 731 18 9 8 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL337875 209843 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280683 98933 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL282733 98933 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL268064 208983 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None None 10.1021/jm00020a029
44281070 111843 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 633 15 7 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2s1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL32941 111843 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 633 15 7 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2s1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL3143248 209386 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)CCCN)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44281289 118044 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 599 15 10 9 -0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34156 118044 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 599 15 10 9 -0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/s0960-894x(99)00197-3
121469330 148080 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 474 4 1 5 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2cc[nH]n2)CC1(F)F 10.1021/acsmedchemlett.6b00327
CHEMBL3939323 148080 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 474 4 1 5 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2cc[nH]n2)CC1(F)F 10.1021/acsmedchemlett.6b00327
155526775 170606 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1309 45 6 19 5.6 NCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)nn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)NCc2ccccc2)nn1 10.1021/acsmedchemlett.8b00538
CHEMBL4459024 170606 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1309 45 6 19 5.6 NCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)nn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)NCc2ccccc2)nn1 10.1021/acsmedchemlett.8b00538
44306762 201402 0 None - 1 Human 7.0 pIC50 = 7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL63966 201402 0 None - 1 Human 7.0 pIC50 = 7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44306599 201949 0 None - 1 Human 7.0 pIC50 = 7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL67308 201949 0 None - 1 Human 7.0 pIC50 = 7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
51003683 75286 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL2047297 75286 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL4227548 75286 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
44338917 161361 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 409 8 0 4 5.9 Clc1cccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL415325 161361 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 409 8 0 4 5.9 Clc1cccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
44306903 101769 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303157 101769 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306404 201210 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL62775 201210 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44316184 103664 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 397 8 3 6 0.1 COC(=O)C(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL309531 103664 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 397 8 3 6 0.1 COC(=O)C(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
51003683 75286 0 None - 1 Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL2047297 75286 0 None - 1 Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL4227548 75286 0 None - 1 Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
137655130 158090 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 489 5 2 4 5.7 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2CCc1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4092540 158090 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 489 5 2 4 5.7 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2CCc1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/acs.jmedchem.7b00951
145971090 164472 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 323 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2N=[N+]=[N-])c1 10.1016/j.bmc.2018.04.016
CHEMBL4226195 164472 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 323 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2N=[N+]=[N-])c1 10.1016/j.bmc.2018.04.016
145967675 164533 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 370 5 2 2 4.1 C#CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL4227184 164533 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 370 5 2 2 4.1 C#CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
44306659 102286 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL305188 102286 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
137661486 158917 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4101591 158917 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
145386428 176513 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 478 6 2 5 4.7 C[C@H]1OC(=O)[C@]2(NCC(=O)O)C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
CHEMBL4633243 176513 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 478 6 2 5 4.7 C[C@H]1OC(=O)[C@]2(NCC(=O)O)C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
44316560 104284 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 375 7 3 5 0.0 O=C(NCCS(=O)(=O)O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL310859 104284 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 375 7 3 5 0.0 O=C(NCCS(=O)(=O)O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
44306660 202117 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL68458 202117 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL3143271 209398 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306894 102226 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304829 102226 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
12018762 109133 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL322282 109133 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
90663563 106205 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 829 22 9 8 2.0 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143684 106205 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 829 22 9 8 2.0 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
44339029 109191 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL322763 109191 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44338929 5753 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107919 5753 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
137632193 156109 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@H]2CC[C@@H]3COC(=O)[C@H]3[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
CHEMBL4069486 156109 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@H]2CC[C@@H]3COC(=O)[C@H]3[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
44339060 9317 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 323 5 2 3 3.5 CC(C)N(CC(O)c1ccc(C#N)cc1)C(=O)Nc1ccccc1 10.1016/s0960-894x(01)00745-4
CHEMBL111689 9317 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 323 5 2 3 3.5 CC(C)N(CC(O)c1ccc(C#N)cc1)C(=O)Nc1ccccc1 10.1016/s0960-894x(01)00745-4
12018759 110698 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL326456 110698 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
155564785 174937 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1786 52 6 24 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4578092 174937 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1786 52 6 24 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
44338929 5753 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107919 5753 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44339173 8125 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL109226 8125 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
10276545 9042 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL110024 9042 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44306349 102116 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304120 102116 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44306337 96376 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL265227 96376 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
44306499 201645 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL65004 201645 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
44328342 206343 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 881 21 8 7 5.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL97780 206343 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 881 21 8 7 5.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)C(=O)O 10.1016/s0960-894x(98)00730-6
44339157 109254 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 451 8 0 6 5.5 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL323054 109254 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 451 8 0 6 5.5 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL5085826 213210 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None CC1=NO[C@@]2(C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@@H](c1ccc(-c3cccc(F)c3)cn1)[C@@H]2C 10.1021/acs.jmedchem.1c02048
CHEMBL5077710 212730 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@@H]1[C@@H](C)[C@@H]2CNC[C@@]23C(=O)O[C@H](C)[C@H]3[C@H]1/C=C/c1ccc(-c2ccccc2C#N)cn1 10.1021/acs.jmedchem.1c02048
155549751 173336 0 None 16 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4540591 173336 0 None 16 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
44339002 9245 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111258 9245 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
12018762 109133 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL322282 109133 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44306500 167342 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL431369 167342 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
137637794 155461 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 5 1 4 5.5 CO[C@@H]1CC[C@@]2(C)[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@@]3(CC[C@@H]2[C@]1(C)CO)CO3 10.1021/acs.jmedchem.7b00951
CHEMBL4062114 155461 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 5 1 4 5.5 CO[C@@H]1CC[C@@]2(C)[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@@]3(CC[C@@H]2[C@]1(C)CO)CO3 10.1021/acs.jmedchem.7b00951
137653750 158170 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 439 5 2 4 4.8 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2CCc1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4093491 158170 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 439 5 2 4 4.8 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2CCc1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
44306337 96376 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL265227 96376 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
137645208 157411 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 421 4 1 3 5.9 C[C@H]1CC[C@H]2[C@@](C)(CC[C@@H](O)[C@@]2(C)C=O)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4084812 157411 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 421 4 1 3 5.9 C[C@H]1CC[C@H]2[C@@](C)(CC[C@@H](O)[C@@]2(C)C=O)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
44306761 168332 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL438551 168332 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44338885 7403 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 405 9 0 5 5.2 COc1cccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL108716 7403 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 405 9 0 5 5.2 COc1cccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL3143270 209397 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143299 209410 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(N)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
137661676 158793 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 450 5 2 4 5.1 CNC[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL4100310 158793 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 450 5 2 4 5.1 CNC[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL3143317 209419 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143311 209415 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL5078821 212806 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1OC(=O)[C@@H]2CC3(NC(=O)NC3=O)[C@@H](C)[C@H](c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
155549751 173336 0 None 16 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4540591 173336 0 None 16 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
145386406 176936 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 459 5 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NCC#N)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
CHEMBL4639789 176936 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 459 5 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NCC#N)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
9919038 166164 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL428311 166164 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL3143290 209408 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
9832212 203231 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL4226137 203231 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL7642 203231 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL3143254 209388 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm960455s
44306697 102246 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304924 102246 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
137638549 156311 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 435 3 1 4 5.3 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H](O)CC[C@]2(C)[C@@H]1CC[C@@H]1COC(=O)[C@H]12 10.1021/acs.jmedchem.7b00951
CHEMBL4071756 156311 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 435 3 1 4 5.3 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H](O)CC[C@]2(C)[C@@H]1CC[C@@H]1COC(=O)[C@H]12 10.1021/acs.jmedchem.7b00951
10161572 5461 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107667 5461 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
1048267 32197 87 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL1411333 32197 87 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
17222599 169192 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 3.8 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL4438936 169192 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 3.8 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL5084411 213132 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1OC(=O)[C@]2(O)CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
9832212 203231 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
CHEMBL4226137 203231 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
CHEMBL7642 203231 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
9832212 203231 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL4226137 203231 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL7642 203231 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
9825804 203772 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 466 8 3 5 2.9 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1cnc2ccccc2c1 10.1016/0960-894X(96)00438-6
CHEMBL80623 203772 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 466 8 3 5 2.9 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1cnc2ccccc2c1 10.1016/0960-894X(96)00438-6
10095734 203810 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 459 8 3 6 2.1 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00438-6
CHEMBL80942 203810 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 459 8 3 6 2.1 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00438-6
CHEMBL3143272 209399 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306698 102225 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304827 102225 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44306404 201210 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL62775 201210 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44338895 9200 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 8 0 4 6.4 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3ccc4ccccc4c3)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL110996 9200 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 8 0 4 6.4 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3ccc4ccccc4c3)on2)cc1 10.1016/s0960-894x(01)00745-4
10771636 106164 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143298 106164 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306696 101646 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL302433 101646 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44316045 102621 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 2 4 0.9 CN1CCC(CCC(=O)N2CCCC(C(=O)NCCC(=O)O)C2)CC1 10.1016/0960-894X(96)00438-6
CHEMBL307684 102621 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 2 4 0.9 CN1CCC(CCC(=O)N2CCCC(C(=O)NCCC(=O)O)C2)CC1 10.1016/0960-894X(96)00438-6
22611792 104634 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 3 4 1.0 CC(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL311426 104634 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 3 4 1.0 CC(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
137639606 156348 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H](OC(N)=O)CC[C@]2(C)[C@@H]1CC[C@@H]1COC(=O)[C@H]12 10.1021/acs.jmedchem.7b00951
CHEMBL4072202 156348 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H](OC(N)=O)CC[C@]2(C)[C@@H]1CC[C@@H]1COC(=O)[C@H]12 10.1021/acs.jmedchem.7b00951
44315780 203357 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 375 8 3 5 0.0 O=C(O)CCNC(=O)C1CCCN(S(=O)(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL77367 203357 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 375 8 3 5 0.0 O=C(O)CCNC(=O)C1CCCN(S(=O)(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL3143291 209409 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306499 201645 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL65004 201645 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
137654212 158119 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@H]2CC[C@@H]3COC(=O)[C@H]3[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
CHEMBL4092965 158119 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@H]2CC[C@@H]3COC(=O)[C@H]3[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
44338944 110880 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 481 9 0 7 5.5 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
CHEMBL327117 110880 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 481 9 0 7 5.5 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
90663337 106165 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 869 20 9 10 1.1 CC(=O)N(C(=O)c1cc2ccccc2oc1=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143301 106165 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 869 20 9 10 1.1 CC(=O)N(C(=O)c1cc2ccccc2oc1=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
17222599 169192 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 3.8 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL4438936 169192 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 3.8 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
44339001 108989 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
CHEMBL322093 108989 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
10276545 9042 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL110024 9042 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44306403 201165 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL62584 201165 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
137647264 157309 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 436 4 2 4 4.8 C[C@@]12CC[C@@H](O)[C@@](C)(CN)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4083850 157309 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 436 4 2 4 4.8 C[C@@]12CC[C@@H](O)[C@@](C)(CN)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
9853816 96875 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL269345 96875 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44306903 101769 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303157 101769 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
90663307 106150 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1ccc(Cl)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143267 106150 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1ccc(Cl)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44338787 6800 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
CHEMBL108428 6800 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
10077130 3932 49 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4047 3932 49 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4870 3932 49 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL493982 3932 49 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
DB09030 3932 49 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
10077130 3932 49 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2020.127046
4047 3932 49 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2020.127046
4870 3932 49 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2020.127046
CHEMBL493982 3932 49 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2020.127046
DB09030 3932 49 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2020.127046
90663294 106144 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 827 22 8 9 2.1 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143253 106144 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 827 22 8 9 2.1 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
90663318 106156 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 986 28 12 10 0.5 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143280 106156 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 986 28 12 10 0.5 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143309 209413 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)COc1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306500 167342 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL431369 167342 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
12018758 9242 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL111241 9242 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
9853816 96875 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL269345 96875 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL3143321 209422 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(O)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL5094099 213684 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@@H]1[C@@H](C)[C@@H]2CN(C)C[C@@]23C(=O)O[C@H](C)[C@H]3[C@H]1/C=C/c1ccc(-c2ccccc2C#N)cn1 10.1021/acs.jmedchem.1c02048
117909194 151692 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 485 4 1 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2n[nH]c(=O)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
CHEMBL3968866 151692 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 485 4 1 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2n[nH]c(=O)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
CHEMBL3143246 209385 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC#Cc1ccccc1C(=O)N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
22611774 203716 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 2 4 0.9 CN(CCC(=O)O)C(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80289 203716 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 2 4 0.9 CN(CCC(=O)O)C(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
145970191 164517 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 870 18 5 7 6.7 C#CCCC(=O)NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL4226980 164517 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 870 18 5 7 6.7 C#CCCC(=O)NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
90663334 106163 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 807 20 9 7 2.0 CC(=O)N(c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143297 106163 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 807 20 9 7 2.0 CC(=O)N(c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
137654568 158377 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 4 2 4 4.9 C[C@]1(C(=O)O)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL4095795 158377 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 4 2 4 4.9 C[C@]1(C(=O)O)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
12018757 108660 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
CHEMBL321437 108660 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
CHEMBL5085562 213190 1 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@]4(O)CC(F)(F)[C@H]3C)nc2)c1C#N 10.1021/acs.jmedchem.1c02048
CHEMBL5091232 213514 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1[C@H](c2ccc(-c3cccc(F)c3)cn2)[C@@H]2[C@@H](C)OC(=O)[C@@H]2C[C@@H]1C 10.1021/acs.jmedchem.1c02048
117909768 146801 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 491 4 1 8 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2nnc(N)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
CHEMBL3929336 146801 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 491 4 1 8 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2nnc(N)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
155536026 171529 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1698 46 6 22 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4472608 171529 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1698 46 6 22 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
10350886 178169 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against PAR1 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometryAntagonist activity against PAR1 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometry
ChEMBL 942 27 13 9 -0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O nan
CHEMBL46869 178169 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against PAR1 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometryAntagonist activity against PAR1 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometry
ChEMBL 942 27 13 9 -0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O nan
44328523 106140 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 786 21 10 7 1.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL314325 106140 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 786 21 10 7 1.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O 10.1016/s0960-894x(98)00730-6
44306697 102246 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304924 102246 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
10819322 203195 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL7610 203195 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44316522 203777 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80672 203777 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
137632009 156102 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 435 4 1 4 5.1 C[C@]1(C=O)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL4069403 156102 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 435 4 1 4 5.1 C[C@]1(C=O)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
90663339 106167 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 883 21 9 8 3.1 CC(=O)N(C(=O)c1cccc(C2CCCCC2)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143303 106167 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 883 21 9 8 3.1 CC(=O)N(C(=O)c1cccc(C2CCCCC2)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306403 201165 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL62584 201165 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
44316532 203744 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)[C@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80455 203744 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)[C@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
10459564 514 34 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
4048 514 34 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
CHEMBL2103856 514 34 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
DB12046 514 34 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
57892463 164493 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CCC2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmc.2018.04.016
CHEMBL4226439 164493 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CCC2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmc.2018.04.016
44306402 167634 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL433499 167634 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44328340 96241 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1095 30 12 10 3.0 CCC(=O)NCCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL264099 96241 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1095 30 12 10 3.0 CCC(=O)NCCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
10328351 206287 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 892 24 10 8 2.9 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CCc1ccc(C(=O)c2ccccc2)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL97498 206287 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 892 24 10 8 2.9 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CCc1ccc(C(=O)c2ccccc2)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O 10.1016/s0960-894x(98)00730-6
145970191 164517 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 870 18 5 7 6.7 C#CCCC(=O)NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL4226980 164517 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 870 18 5 7 6.7 C#CCCC(=O)NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
3109060 170086 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 384 4 2 3 4.5 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1ccco1 10.1016/j.bmc.2019.06.043
CHEMBL4451525 170086 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 384 4 2 3 4.5 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1ccco1 10.1016/j.bmc.2019.06.043
50910548 75287 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 374 5 2 2 4.7 CC(C)CC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL2047299 75287 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 374 5 2 2 4.7 CC(C)CC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
877874 23106 16 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL1332325 23106 16 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
877874 23106 16 None - 1 Human 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL1332325 23106 16 None - 1 Human 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
57892463 164493 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CCC2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmc.2018.04.016
CHEMBL4226439 164493 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CCC2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmc.2018.04.016
3109060 170086 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 384 4 2 3 4.5 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1ccco1 10.1016/j.bmc.2019.06.043
CHEMBL4451525 170086 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 384 4 2 3 4.5 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1ccco1 10.1016/j.bmc.2019.06.043
10279248 108342 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 511 9 0 8 4.7 CS(=O)(=O)c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL320990 108342 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 511 9 0 8 4.7 CS(=O)(=O)c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
44339002 9245 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111258 9245 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
137633371 155825 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 450 4 1 3 6.9 C[C@H]1CC[C@@H]2C(C)(C)[C@H](OC(N)=O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4066290 155825 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 450 4 1 3 6.9 C[C@H]1CC[C@@H]2C(C)(C)[C@H](OC(N)=O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
90663297 106145 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143256 106145 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44339055 9218 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
CHEMBL111101 9218 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
10459564 514 34 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
4048 514 34 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
CHEMBL2103856 514 34 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
DB12046 514 34 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
877874 23106 16 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL1332325 23106 16 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
44338886 162738 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 391 9 0 5 4.8 COc1cccc(CN(CCCN2CCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL418815 162738 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 391 9 0 5 4.8 COc1cccc(CN(CCCN2CCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL3143288 209406 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@H](Cc1cccs1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306761 168332 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL438551 168332 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44328381 97829 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1265 34 15 12 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCNC(=O)CCCC[C@H]1SC[C@H]2NC(=O)N[C@H]21)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL274769 97829 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1265 34 15 12 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCNC(=O)CCCC[C@H]1SC[C@H]2NC(=O)N[C@H]21)C(=O)O 10.1016/s0960-894x(98)00730-6
10161572 5461 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107667 5461 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
90663354 106173 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccccc1F)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143319 106173 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccccc1F)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
155549751 173336 0 None 16 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of thrombin-induced intracellular calcium mobilization preincubated for 15 mins followed by thrombin addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of thrombin-induced intracellular calcium mobilization preincubated for 15 mins followed by thrombin addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4540591 173336 0 None 16 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of thrombin-induced intracellular calcium mobilization preincubated for 15 mins followed by thrombin addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of thrombin-induced intracellular calcium mobilization preincubated for 15 mins followed by thrombin addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
44338864 7196 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 439 8 0 4 6.8 c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL108604 7196 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 439 8 0 4 6.8 c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
44306612 101677 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL302603 101677 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
154688307 172269 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cnco1 10.1016/j.bmc.2019.06.043
CHEMBL4514779 172269 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cnco1 10.1016/j.bmc.2019.06.043
10278388 110497 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 495 9 0 7 5.1 C[S+]([O-])c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL326247 110497 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 495 9 0 7 5.1 C[S+]([O-])c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
155519325 169837 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 2 2 4.6 O=C(CC(F)(F)F)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL4448258 169837 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 2 2 4.6 O=C(CC(F)(F)F)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
90663343 106171 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1cccc2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143308 106171 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1cccc2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306658 101712 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 835 19 6 9 5.0 COC(=O)c1ccc(Cn2cc(CN3CCCC3)c3ccc(NC(=O)N[C@@H](Cc4ccc(OC)cc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC4CCCCC4)cc32)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL302823 101712 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 835 19 6 9 5.0 COC(=O)c1ccc(Cn2cc(CN3CCCC3)c3ccc(NC(=O)N[C@@H](Cc4ccc(OC)cc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC4CCCCC4)cc32)cc1 10.1016/s0960-894x(01)00378-x
90663292 106142 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 857 22 9 9 1.4 COc1ccc(/C=C/C(=O)N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
CHEMBL3143251 106142 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 857 22 9 9 1.4 COc1ccc(/C=C/C(=O)N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
90663333 106162 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 843 23 9 8 2.4 CCCC(=O)c1ccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
CHEMBL3143296 106162 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 843 23 9 8 2.4 CCCC(=O)c1ccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
155519325 169837 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 2 2 4.6 O=C(CC(F)(F)F)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL4448258 169837 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 2 2 4.6 O=C(CC(F)(F)F)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
154688304 175627 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cocn1 10.1016/j.bmc.2019.06.043
CHEMBL4594058 175627 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cocn1 10.1016/j.bmc.2019.06.043
CHEMBL5069528 212437 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None CCOC(=O)N1C[C@H]2[C@H](C)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@]32C1 10.1021/acs.jmedchem.1c02048
117909666 148205 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 492 4 1 7 4.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2n[nH]c(=O)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
CHEMBL3940415 148205 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 492 4 1 7 4.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2n[nH]c(=O)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
155512671 169090 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1874 58 6 26 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4437508 169090 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1874 58 6 26 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
90663313 106151 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 982 27 12 10 -0.3 C#CC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143273 106151 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 982 27 12 10 -0.3 C#CC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
90663314 106152 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 984 28 11 11 0.6 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143274 106152 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 984 28 11 11 0.6 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
44338946 9201 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
CHEMBL110998 9201 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
44306659 102286 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL305188 102286 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44306611 201899 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL66958 201899 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
15887956 203711 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 415 8 3 4 2.3 O=C(O)CC(NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1)c1ccccc1 10.1016/0960-894X(96)00438-6
CHEMBL80232 203711 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 415 8 3 4 2.3 O=C(O)CC(NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1)c1ccccc1 10.1016/0960-894X(96)00438-6
44316106 203727 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 395 9 3 4 2.0 CC(C)CC(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80343 203727 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 395 9 3 4 2.0 CC(C)CC(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
90663330 106159 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1cccc(F)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143293 106159 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1cccc(F)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
15887960 203811 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 363 7 3 6 -0.1 O=C(NCCc1nnn[nH]1)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80943 203811 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 363 7 3 6 -0.1 O=C(NCCc1nnn[nH]1)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
44306657 101776 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303187 101776 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL3143264 209393 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm960455s
154688304 175627 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cocn1 10.1016/j.bmc.2019.06.043
CHEMBL4594058 175627 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cocn1 10.1016/j.bmc.2019.06.043
12018759 110698 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL326456 110698 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL4764659 212275 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Affinity Phenotypic Cellular interaction (Inhibition of platelet aggregation (human plasma, TRAP-6)) EUB0000291b F2RAffinity Phenotypic Cellular interaction (Inhibition of platelet aggregation (human plasma, TRAP-6)) EUB0000291b F2R
ChEMBL None None None O=C(N1CCS(=O)(=O)CC1)N1C[C@@](S)(c2ccc(OC(F)(F)F)cc2)C[C@@](S)(c2nc(C3CC3)no2)C1 nan
10206026 9337 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 479 9 0 7 6.1 CSc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111761 9337 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 479 9 0 7 6.1 CSc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
90663291 106141 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 18 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 18 uM) induced platelet aggregation by 50%
ChEMBL 877 21 9 8 2.7 CC(=O)N(C(=O)c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143250 106141 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 18 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 18 uM) induced platelet aggregation by 50%
ChEMBL 877 21 9 8 2.7 CC(=O)N(C(=O)c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306540 201338 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL63402 201338 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
10164471 9032 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 509 9 0 6 7.0 c1ccc(-c2ccc(-c3cc(N(CCCN4CCCCCC4)Cc4ccc5c(c4)OCO5)on3)cc2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL109946 9032 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 509 9 0 6 7.0 c1ccc(-c2ccc(-c3cc(N(CCCN4CCCCCC4)Cc4ccc5c(c4)OCO5)on3)cc2)cc1 10.1016/s0960-894x(01)00745-4
44306698 102225 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304827 102225 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
90663332 106161 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1ccc2ccccc2c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143295 106161 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1ccc2ccccc2c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44338946 9201 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
CHEMBL110998 9201 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
10077130 3932 49 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4047 3932 49 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4870 3932 49 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL493982 3932 49 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
DB09030 3932 49 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL3143275 209400 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm960455s
90663360 106176 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 795 21 9 9 1.2 CC(=O)N(Oc1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143326 106176 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 795 21 9 9 1.2 CC(=O)N(Oc1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306501 102205 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304683 102205 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44306657 101776 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303187 101776 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306402 167634 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL433499 167634 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
9832212 203231 4 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
CHEMBL4226137 203231 4 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
CHEMBL7642 203231 4 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
CHEMBL5077302 212711 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1OC(=O)[C@@H]2CC(F)(F)[C@@H](C)[C@H](c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
CHEMBL3143281 209402 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44338787 6800 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
CHEMBL108428 6800 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
44338875 109277 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 413 9 0 5 5.6 COc1cccc(CN(CCCN2C=CC=CC=C2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL323221 109277 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 413 9 0 5 5.6 COc1cccc(CN(CCCN2C=CC=CC=C2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
44339070 109830 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 8 0 4 6.4 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL323956 109830 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 8 0 4 6.4 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL3143284 209404 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306732 102118 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304128 102118 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44339056 8582 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 453 9 0 4 7.2 c1ccc(-c2cc(N(CCCCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL109564 8582 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 453 9 0 4 7.2 c1ccc(-c2cc(N(CCCCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
44338865 108622 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 7 0 4 6.4 c1ccc(-c2cc(N(CCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL321380 108622 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 7 0 4 6.4 c1ccc(-c2cc(N(CCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL3143313 209416 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44315792 203336 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 341 6 3 5 0.4 O=C(O)CCNC(=O)C1CCCN(C(=O)OCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL77179 203336 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 341 6 3 5 0.4 O=C(O)CCNC(=O)C1CCCN(C(=O)OCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
154688307 172269 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cnco1 10.1016/j.bmc.2019.06.043
CHEMBL4514779 172269 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cnco1 10.1016/j.bmc.2019.06.043
9847494 5756 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107920 5756 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL3143249 209387 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663299 106147 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 812 20 10 7 1.9 CC(=O)N(c1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143258 106147 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 812 20 10 7 1.9 CC(=O)N(c1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
145386419 176483 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 474 5 1 5 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cc1 10.1016/j.bmcl.2020.127046
CHEMBL4632907 176483 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 474 5 1 5 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cc1 10.1016/j.bmcl.2020.127046
137644873 157654 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 439 4 3 4 4.8 C[C@]1(O)CC[C@H]2[C@@](C)(CC[C@@H](O)[C@@]2(C)CO)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4088070 157654 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 439 4 3 4 4.8 C[C@]1(O)CC[C@H]2[C@@](C)(CC[C@@H](O)[C@@]2(C)CO)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
9919038 166164 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL428311 166164 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
1048267 32197 87 None - 1 Human 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL1411333 32197 87 None - 1 Human 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL5081773 212985 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1NC(=O)[C@]2(N)CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
90663316 106155 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 1002 28 11 11 0.7 CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143278 106155 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 1002 28 11 11 0.7 CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
44338882 5831 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 419 8 0 6 5.0 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL107971 5831 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 419 8 0 6 5.0 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
44306708 100430 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL293867 100430 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44306336 201844 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL66585 201844 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
44306599 201949 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL67308 201949 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44328562 167505 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 924 23 11 8 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL432578 167505 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 924 23 11 8 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
145386418 176550 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 512 5 1 6 6.1 Cc1ccnc(N[C@@H]2CC[C@@H]3[C@@H](C2)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]3/C=C/c2ccc(-c3cccc(F)c3)cn2)n1 10.1016/j.bmcl.2020.127046
CHEMBL4633888 176550 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 512 5 1 6 6.1 Cc1ccnc(N[C@@H]2CC[C@@H]3[C@@H](C2)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]3/C=C/c2ccc(-c3cccc(F)c3)cn2)n1 10.1016/j.bmcl.2020.127046
44306349 102116 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304120 102116 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44306336 201844 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL66585 201844 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
10077130 3932 49 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4047 3932 49 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4870 3932 49 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
CHEMBL493982 3932 49 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
DB09030 3932 49 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
44306540 201338 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL63402 201338 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306612 101677 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL302603 101677 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
90663305 106149 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 558 11 5 5 2.3 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(N)=O 10.1021/jm960455s
CHEMBL3143265 106149 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 558 11 5 5 2.3 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(N)=O 10.1021/jm960455s
44339030 9311 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 509 9 0 6 7.0 c1ccc(-c2cccc(-c3cc(N(CCCN4CCCCCC4)Cc4ccc5c(c4)OCO5)on3)c2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111653 9311 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 509 9 0 6 7.0 c1ccc(-c2cccc(-c3cc(N(CCCN4CCCCCC4)Cc4ccc5c(c4)OCO5)on3)c2)cc1 10.1016/s0960-894x(01)00745-4
15887958 104805 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 393 5 2 5 0.5 O=C(O)C1CN(C(=O)C2CCCN(C(=O)CCC3CCNCC3)C2)CCC1=O 10.1016/0960-894X(96)00438-6
CHEMBL311554 104805 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 393 5 2 5 0.5 O=C(O)C1CN(C(=O)C2CCCN(C(=O)CCC3CCNCC3)C2)CCC1=O 10.1016/0960-894X(96)00438-6
90663358 106174 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 903 22 9 8 3.1 CC(=O)N(C(=O)/C=C/c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143324 106174 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 903 22 9 8 3.1 CC(=O)N(C(=O)/C=C/c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663341 106169 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143306 106169 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3144093 209426 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)CSc1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL5081315 212959 1 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1OC(=O)[C@]2(N)CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
CHEMBL5088392 213373 2 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None CCNC(=O)N1C[C@H]2[C@H](C)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@]32C1 10.1021/acs.jmedchem.1c02048
CHEMBL5094869 213730 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None CNC(=O)N1C[C@H]2[C@H](C)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@]32C1 10.1021/acs.jmedchem.1c02048
44338944 110880 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 481 9 0 7 5.5 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
CHEMBL327117 110880 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 481 9 0 7 5.5 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
44306501 102205 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304683 102205 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44306762 201402 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL63966 201402 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
9801767 99853 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL289432 99853 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
137649563 156796 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 465 4 1 5 5.0 COC(=O)[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL4077763 156796 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 465 4 1 5 5.0 COC(=O)[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
44315793 203269 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 340 6 4 4 -0.0 O=C(O)CCNC(=O)C1CCCN(C(=O)NCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL76641 203269 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 340 6 4 4 -0.0 O=C(O)CCNC(=O)C1CCCN(C(=O)NCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
44316059 203817 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 325 7 3 4 0.2 O=C(O)CCNC(=O)C1CCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80975 203817 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 325 7 3 4 0.2 O=C(O)CCNC(=O)C1CCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
90663340 106168 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1ccsc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143304 106168 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1ccsc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
145386426 176928 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 459 5 1 5 5.1 C[C@H]1OC(=O)[C@]2(NCC#N)C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
CHEMBL4639680 176928 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 459 5 1 5 5.1 C[C@H]1OC(=O)[C@]2(NCC#N)C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
CHEMBL3143268 209395 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CCCCC/C=C/CC(=O)N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306696 101646 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL302433 101646 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
1048267 32197 87 None - 1 Human 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL1411333 32197 87 None - 1 Human 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL5093637 213650 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1OC(=O)[C@]2(O)CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
CHEMBL5094241 213697 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None CC[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F 10.1021/acs.jmedchem.1c02048
90663298 106146 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 120 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 120 uM) induced platelet aggregation by 50%
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143257 106146 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 120 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 120 uM) induced platelet aggregation by 50%
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10741717 102547 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 439 7 3 4 2.0 O=C(O)C[C@@H](C#Cc1ccccc1)NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL307065 102547 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 439 7 3 4 2.0 O=C(O)C[C@@H](C#Cc1ccccc1)NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
10526120 203139 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 419 7 3 4 2.0 CC(C)(C)C#C[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL75636 203139 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 419 7 3 4 2.0 CC(C)(C)C#C[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
44316156 203276 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 355 7 4 5 -0.4 O=C(O)C(O)CNC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL76719 203276 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 355 7 4 5 -0.4 O=C(O)C(O)CNC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL3143282 209403 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
22645287 203148 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 3 4 1.0 O=C(O)CCNC(=O)C1CCCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL75688 203148 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 3 4 1.0 O=C(O)CCNC(=O)C1CCCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
137653180 157998 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 5 1 4 5.5 COC[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL4091623 157998 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 5 1 4 5.5 COC[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
145967675 164533 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 370 5 2 2 4.1 C#CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL4227184 164533 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 370 5 2 2 4.1 C#CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
10162707 9223 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 478 9 0 8 5.3 O=[N+]([O-])c1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL111109 9223 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 478 9 0 8 5.3 O=[N+]([O-])c1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL3143266 209394 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(C)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663293 106143 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 998 29 11 11 1.0 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CCC(N)=O 10.1021/jm960455s
CHEMBL3143252 106143 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 998 29 11 11 1.0 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CCC(N)=O 10.1021/jm960455s
1048267 32197 87 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL1411333 32197 87 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
44306708 100430 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL293867 100430 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
90663302 106148 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 765 20 9 7 1.1 CC(=O)N(C1CCCC1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143262 106148 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 765 20 9 7 1.1 CC(=O)N(C1CCCC1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
137632975 155795 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 508 5 1 6 5.1 COC(=O)[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
CHEMBL4065905 155795 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 508 5 1 6 5.1 COC(=O)[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
CHEMBL3143310 209414 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@H](CCCN)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)/C=C/c1ccccc1 10.1021/jm960455s
137652024 156566 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 485 5 0 4 6.7 C[C@H]1CC[C@@H]2C(C)(C)[C@H](OS(C)(=O)=O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4074902 156566 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 485 5 0 4 6.7 C[C@H]1CC[C@@H]2C(C)(C)[C@H](OS(C)(=O)=O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL3143289 209407 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663338 106166 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 833 22 9 9 1.8 C=CC(=O)c1ccsc1N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143302 106166 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 833 22 9 9 1.8 C=CC(=O)c1ccsc1N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44338791 9221 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111106 9221 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
9847494 5756 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107920 5756 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44338791 9221 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111106 9221 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL3143249 209387 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10622095 203558 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 421 8 3 5 2.4 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1cccs1 10.1016/0960-894X(96)00438-6
CHEMBL79087 203558 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 421 8 3 5 2.4 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1cccs1 10.1016/0960-894X(96)00438-6
44306894 102226 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304829 102226 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306660 202117 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL68458 202117 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
44306732 102118 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304128 102118 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
10819322 203195 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL7610 203195 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
128205 9344 2 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 375 8 0 4 5.2 c1ccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111790 9344 2 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 375 8 0 4 5.2 c1ccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)cc1 10.1016/s0960-894x(01)00745-4
44328197 81958 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1051 28 10 9 5.0 CCC(=O)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL217237 81958 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1051 28 10 9 5.0 CCC(=O)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
90663321 106157 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 850 23 6 8 1.5 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143283 106157 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 850 23 6 8 1.5 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
12018758 9242 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL111241 9242 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
137659611 158893 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 437 4 2 4 4.9 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4101239 158893 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 437 4 2 4 4.9 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
145971090 164472 0 None - 1 Human 4.0 pIC50 = 4.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 323 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2N=[N+]=[N-])c1 10.1016/j.bmc.2018.04.016
CHEMBL4226195 164472 0 None - 1 Human 4.0 pIC50 = 4.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 323 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2N=[N+]=[N-])c1 10.1016/j.bmc.2018.04.016
90663331 106160 0 None - 1 Human 4.0 pIC50 = 4.0 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 773 20 9 7 1.4 CC(=O)N(c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143294 106160 0 None - 1 Human 4.0 pIC50 = 4.0 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 773 20 9 7 1.4 CC(=O)N(c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143266 209394 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(C)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
137631870 155791 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 487 4 2 4 5.7 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4065873 155791 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 487 4 2 4 5.7 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/acs.jmedchem.7b00951
155526775 170606 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1309 45 6 19 5.6 NCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)nn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)NCc2ccccc2)nn1 10.1021/acsmedchemlett.8b00538
CHEMBL4459024 170606 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1309 45 6 19 5.6 NCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)nn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)NCc2ccccc2)nn1 10.1021/acsmedchemlett.8b00538
51003683 75286 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL2047297 75286 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL4227548 75286 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
44328383 158405 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1222 32 12 11 5.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=O)CCCCC1SC[C@H]2NC(=O)N[C@@H]12)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL409602 158405 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1222 32 12 11 5.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=O)CCCCC1SC[C@H]2NC(=O)N[C@@H]12)C(=O)O 10.1016/s0960-894x(98)00730-6
44306611 201899 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL66958 201899 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
90663342 106170 0 None - 1 Human 5.0 pIC50 = 5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 828 21 10 8 1.6 CC(=O)N(Oc1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143307 106170 0 None - 1 Human 5.0 pIC50 = 5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 828 21 10 8 1.6 CC(=O)N(Oc1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44264790 97858 0 None - 0 Human 9.4 pKd = 9.4 Functional
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 862 18 7 8 5.8 NC(CCN[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1)C(=O)O 10.1021/jm000506s
CHEMBL275003 97858 0 None - 0 Human 9.4 pKd = 9.4 Functional
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 862 18 7 8 5.8 NC(CCN[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1)C(=O)O 10.1021/jm000506s
19323337 1580 1 None - 1 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl 10.1016/j.bmcl.2010.01.050
9255 1580 1 None - 1 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl 10.1016/j.bmcl.2010.01.050
CHEMBL559808 1580 1 None - 1 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl 10.1016/j.bmcl.2010.01.050
46865538 6045 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 389 5 0 6 2.7 N#Cc1ccccc1/C=C/c1c(N2CCN(Cc3ccsc3)CC2)c(=O)c1=O 10.1016/j.bmcl.2010.01.050
CHEMBL1080910 6045 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 389 5 0 6 2.7 N#Cc1ccccc1/C=C/c1c(N2CCN(Cc3ccsc3)CC2)c(=O)c1=O 10.1016/j.bmcl.2010.01.050
46880808 6242 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 376 4 1 2 4.5 O=C(/C=C\c1ccccc1Cl)N1CCC(Nc2ccc(F)cc2)C(F)C1 10.1016/j.bmcl.2010.01.050
CHEMBL1081998 6242 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 376 4 1 2 4.5 O=C(/C=C\c1ccccc1Cl)N1CCC(Nc2ccc(F)cc2)C(F)C1 10.1016/j.bmcl.2010.01.050
46880668 6073 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 389 5 0 5 3.0 N#Cc1ccccc1/C=C/c1c(N2CCN(CC3CCCCC3)CC2)c(=O)c1=O 10.1016/j.bmcl.2010.01.050
CHEMBL1081077 6073 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 389 5 0 5 3.0 N#Cc1ccccc1/C=C/c1c(N2CCN(CC3CCCCC3)CC2)c(=O)c1=O 10.1016/j.bmcl.2010.01.050
46865537 7382 0 None - 0 Human 6.2 pKd = 6.2 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 472 7 0 4 4.7 N#Cc1ccccc1/C=C\C(=O)N1CCC(N(Cc2ccc(F)cc2)Cc2ccccn2)C(F)C1 10.1016/j.bmcl.2010.01.050
CHEMBL1087016 7382 0 None - 0 Human 6.2 pKd = 6.2 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 472 7 0 4 4.7 N#Cc1ccccc1/C=C\C(=O)N1CCC(N(Cc2ccc(F)cc2)Cc2ccccn2)C(F)C1 10.1016/j.bmcl.2010.01.050
44251419 6209 0 None - 0 Human 6.0 pKd = 6.0 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 317 5 1 4 4.2 N#Cc1ccccc1/C=C/C(=O)c1ccc(NC2CCCC2)nc1 10.1016/j.bmcl.2010.01.050
CHEMBL1081797 6209 0 None - 0 Human 6.0 pKd = 6.0 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 317 5 1 4 4.2 N#Cc1ccccc1/C=C/C(=O)c1ccc(NC2CCCC2)nc1 10.1016/j.bmcl.2010.01.050
10077130 3932 49 None - 1 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium effluxAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4047 3932 49 None - 1 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium effluxAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4870 3932 49 None - 1 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium effluxAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL493982 3932 49 None - 1 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium effluxAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
DB09030 3932 49 None - 1 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium effluxAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
10077130 3932 49 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporationAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4047 3932 49 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporationAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4870 3932 49 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporationAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL493982 3932 49 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporationAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
DB09030 3932 49 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporationAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
10146183 3719 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9315351
3742 3719 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9315351
CHEMBL4065100 3719 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9315351
19323337 1580 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl None
9255 1580 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl None
CHEMBL559808 1580 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl None
3525 3355 8 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10535908
9853822 3355 8 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10535908
CHEMBL311626 3355 8 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10535908
10971 3489 24 None 158 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 11020444
4259181 3489 24 None 158 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 11020444
CHEMBL63426 3489 24 None 158 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 11020444
10459564 514 34 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 21300059
4048 514 34 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 21300059
CHEMBL2103856 514 34 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 21300059
DB12046 514 34 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 21300059


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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
CHEMBL2370701 208162 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric methodActivation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(N)=O 10.1016/j.bmc.2021.116498
CHEMBL5088108 213355 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Activation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric methodActivation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cc(F)c(F)c(F)c1F)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(N)=O 10.1016/j.bmc.2021.116498
CHEMBL5081145 212945 0 None - 0 Human 5.1 pEC50 = 5.1 Binding
Activation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric methodActivation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c(F)cc(F)c(F)c1F)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(N)=O 10.1016/j.bmc.2021.116498
CHEMBL5087962 213347 0 None - 0 Human 4.0 pEC50 = 4 Binding
Activation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric methodActivation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(N)=O 10.1016/j.bmc.2021.116498
127053962 149988 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 6 6.2 Cc1nnc(C[C@@]23CC(F)(F)[C@@H](C)[C@H](/C=C/c4ccc(-c5ccccc5Cl)cn4)C2[C@@H](C)OC3=O)o1 nan
CHEMBL3954641 149988 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 6 6.2 Cc1nnc(C[C@@]23CC(F)(F)[C@@H](C)[C@H](/C=C/c4ccc(-c5ccccc5Cl)cn4)C2[C@@H](C)OC3=O)o1 nan
127053955 159873 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cscn2)CC1(F)F nan
CHEMBL4111522 159873 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cscn2)CC1(F)F nan
127053997 148406 0 None - 0 Human 9.0 pIC50 = 9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 7 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nnnn2C)CC1(F)F nan
CHEMBL3942006 148406 0 None - 0 Human 9.0 pIC50 = 9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 7 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nnnn2C)CC1(F)F nan
10077130 3932 49 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4047 3932 49 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4870 3932 49 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
CHEMBL493982 3932 49 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
DB09030 3932 49 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
127053960 147107 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 499 5 0 6 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2ncon2)CC1(F)F nan
CHEMBL3931589 147107 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 499 5 0 6 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2ncon2)CC1(F)F nan
127053994 151394 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 1 5 4.7 Cc1cccc(-c2ccc(/C=C/[C@@H]3C4[C@@H](C)OC(=O)[C@]4(CN)CC(F)(F)[C@H]3C)nc2)c1C#N nan
CHEMBL3966338 151394 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 1 5 4.7 Cc1cccc(-c2ccc(/C=C/[C@@H]3C4[C@@H](C)OC(=O)[C@]4(CN)CC(F)(F)[C@H]3C)nc2)c1C#N nan
127053955 159873 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cscn2)CC1(F)F nan
CHEMBL4111522 159873 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cscn2)CC1(F)F nan
127053956 160151 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2nccs2)CC1(F)F nan
CHEMBL4113709 160151 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2nccs2)CC1(F)F nan
127053958 160299 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ncco2)CC1(F)F nan
CHEMBL4114937 160299 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ncco2)CC1(F)F nan
72547307 103379 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
CHEMBL3091980 103379 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
127053975 142758 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cncs2)CC1(F)F nan
CHEMBL3897109 142758 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cncs2)CC1(F)F nan
127053965 159314 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 489 4 0 7 4.8 Cc1cn([C@@]23CC(F)(F)C(C)[C@H](/C=C/c4ccc(-c5ccccc5C#N)cn4)C2[C@@H](C)OC3=O)nn1 nan
CHEMBL4106770 159314 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 489 4 0 7 4.8 Cc1cn([C@@]23CC(F)(F)C(C)[C@H](/C=C/c4ccc(-c5ccccc5C#N)cn4)C2[C@@H](C)OC3=O)nn1 nan
10077130 3932 49 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4047 3932 49 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4870 3932 49 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
CHEMBL493982 3932 49 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
DB09030 3932 49 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
127053995 147296 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 407 3 1 3 4.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2C(CC1(F)F)C(=O)N[C@@H]2C nan
CHEMBL3933019 147296 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 407 3 1 3 4.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2C(CC1(F)F)C(=O)N[C@@H]2C nan
127053938 147880 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 408 3 0 4 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3937747 147880 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 408 3 0 4 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
127053976 151625 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cscn2)CC1(F)F nan
CHEMBL3968240 151625 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cscn2)CC1(F)F nan
127053985 160136 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 545 5 1 5 5.8 C[C@H]1OC(=O)[C@]2(NC(=O)c3ccc(F)cc3)CC(F)(F)[C@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]12 nan
CHEMBL4113548 160136 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 545 5 1 5 5.8 C[C@H]1OC(=O)[C@]2(NC(=O)c3ccc(F)cc3)CC(F)(F)[C@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]12 nan
127053957 159762 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cocn2)CC1(F)F nan
CHEMBL4110608 159762 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cocn2)CC1(F)F nan
CHEMBL4764659 212275 0 None - 0 Human 8.0 pIC50 = 8 Binding
Affinity On-target Cellular interaction (Functional cellular assay in HEK cells expressing F2R) EUB0000291b F2RAffinity On-target Cellular interaction (Functional cellular assay in HEK cells expressing F2R) EUB0000291b F2R
ChEMBL None None None O=C(N1CCS(=O)(=O)CC1)N1C[C@@](S)(c2ccc(OC(F)(F)F)cc2)C[C@@](S)(c2nc(C3CC3)no2)C1 nan
127050657 140276 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 486 7 2 5 2.9 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCc2cccc(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3819038 140276 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 486 7 2 5 2.9 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCc2cccc(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
44432773 86586 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232534 86586 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
9889179 87530 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 5.9 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL234190 87530 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 5.9 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
44432790 96823 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL269006 96823 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
9931987 72205 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL199201 72205 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm0502236
71736052 146287 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 493 5 1 5 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC(C)(C)C)CC1(F)F nan
CHEMBL3924976 146287 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 493 5 1 5 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC(C)(C)C)CC1(F)F nan
121335751 148166 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 479 5 1 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC2COC2)CC1(F)F nan
CHEMBL3940064 148166 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 479 5 1 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC2COC2)CC1(F)F nan
44428104 143878 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
CHEMBL390630 143878 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
127053947 149744 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 445 4 1 4 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)O)CC1(F)F nan
CHEMBL3952737 149744 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 445 4 1 4 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)O)CC1(F)F nan
127049415 140309 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 473 5 2 6 2.7 N#C/N=C(/Nc1cccc(OC(F)F)c1)N1CC(N2CNCC2=O)C(c2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01890
CHEMBL3819515 140309 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 473 5 2 6 2.7 N#C/N=C(/Nc1cccc(OC(F)F)c1)N1CC(N2CNCC2=O)C(c2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01890
72547556 103392 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091993 103392 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44408851 75042 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL204009 75042 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44409253 75664 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 418 3 1 4 5.2 CC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL205683 75664 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 418 3 1 4 5.2 CC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
11576348 71663 0 None - 0 Human 7.0 pIC50 = 7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 466 4 1 5 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(S(N)(=O)=O)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL197523 71663 0 None - 0 Human 7.0 pIC50 = 7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 466 4 1 5 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(S(N)(=O)=O)c4)cn3)[C@H]12 10.1021/jm0502236
44305948 100120 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 399 4 1 5 5.3 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N5CCCCC5)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL291807 100120 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 399 4 1 5 5.3 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N5CCCCC5)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
44305954 162011 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 359 4 1 5 4.4 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL416862 162011 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 359 4 1 5 4.4 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL3143263 209392 0 None - 0 Human 6.0 pIC50 = 6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)c1ccccc1N)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
9805672 205358 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 491 5 3 3 5.8 C[C@H]1CC[C@@H]([C@@H](O)c2ccc(Cl)c(Cl)c2)N1C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL91987 205358 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 491 5 3 3 5.8 C[C@H]1CC[C@@H]([C@@H](O)c2ccc(Cl)c(Cl)c2)N1C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
44409265 74650 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 434 5 1 5 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(N)=O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL203376 74650 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 434 5 1 5 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(N)=O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44306404 201210 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL62775 201210 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
11502697 133887 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(Cl)cc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371751 133887 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(Cl)cc4)cn3)[C@H]12 10.1021/jm0502236
752812 2527 43 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 10.1016/j.bmcl.2014.08.021
9459 2527 43 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 10.1016/j.bmcl.2014.08.021
CHEMBL1609104 2527 43 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 10.1016/j.bmcl.2014.08.021
44187282 124610 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 482 11 1 8 4.0 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OC)cc(OCC2CCCCC2)c1 nan
CHEMBL3644439 124610 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 482 11 1 8 4.0 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OC)cc(OCC2CCCCC2)c1 nan
44290104 177976 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 735 19 7 8 2.8 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL46702 177976 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 735 19 7 8 2.8 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
44280898 99289 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 566 15 8 5 1.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285075 99289 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 566 15 8 5 1.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280876 99440 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 507 13 8 8 -2.0 C[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286141 99440 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 507 13 8 8 -2.0 C[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280731 99805 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 597 16 9 8 -0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CCc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL289020 99805 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 597 16 9 8 -0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CCc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281047 167253 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 752 18 10 8 2.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2c[nH]c3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL430734 167253 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 752 18 10 8 2.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2c[nH]c3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
23631377 92750 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 512 6 0 5 4.8 CCCS(=O)(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
CHEMBL244503 92750 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 512 6 0 5 4.8 CCCS(=O)(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
10162707 9223 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 478 9 0 8 5.3 O=[N+]([O-])c1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL111109 9223 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 478 9 0 8 5.3 O=[N+]([O-])c1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
90663347 106172 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 781 21 8 9 0.9 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)O 10.1021/jm960455s
CHEMBL3143312 106172 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 781 21 8 9 0.9 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)O 10.1021/jm960455s
58046056 132748 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 469 10 2 9 3.4 CCC(CC)Oc1cc(C)c2nn(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704461 132748 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 469 10 2 9 3.4 CCC(CC)Oc1cc(C)c2nn(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)c(=N)n2n1 nan
66760759 126736 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 394 7 1 3 3.9 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)CCOC)C2)cc1 nan
CHEMBL3658402 126736 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 394 7 1 3 3.9 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)CCOC)C2)cc1 nan
66761545 126743 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 399 4 2 2 4.2 CCc1ccc(C2CC(NC(=O)NC(C)(C)C)CN(C(=O)C3CCCC3)C2)cc1 nan
CHEMBL3658409 126743 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 399 4 2 2 4.2 CCc1ccc(C2CC(NC(=O)NC(C)(C)C)CN(C(=O)C3CCCC3)C2)cc1 nan
9804049 133027 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL371069 133027 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1016/j.bmcl.2006.06.042
44418858 82862 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 3 6.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218935 82862 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 3 6.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm061043e
9804049 133027 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL371069 133027 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
23631187 158913 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 528 4 0 5 6.1 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
CHEMBL410157 158913 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 528 4 0 5 6.1 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
44432714 86253 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 393 3 0 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccsc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231727 86253 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 393 3 0 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccsc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
9804049 133027 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL371069 133027 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
11553497 132917 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
CHEMBL370656 132917 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
9804049 133027 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371069 133027 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
66701293 126749 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 469 5 1 4 4.4 O=C(NC1CC(c2ccc(OC(F)(F)F)cc2)CN(C(=O)c2ccncc2)C1)c1ccccc1 nan
CHEMBL3658414 126749 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 469 5 1 4 4.4 O=C(NC1CC(c2ccc(OC(F)(F)F)cc2)CN(C(=O)c2ccncc2)C1)c1ccccc1 nan
46931523 126998 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 474 5 1 4 4.2 CCc1ccc(C2CC(NC(=O)c3cccc(OC)c3)CN(C(=O)N3CCC(C#N)CC3)C2)cc1 nan
CHEMBL3662512 126998 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 474 5 1 4 4.2 CCc1ccc(C2CC(NC(=O)c3cccc(OC)c3)CN(C(=O)N3CCC(C#N)CC3)C2)cc1 nan
90663334 106163 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 807 20 9 7 2.0 CC(=O)N(c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143297 106163 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 807 20 9 7 2.0 CC(=O)N(c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143264 209393 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm960455s
44183021 132743 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 465 10 1 8 4.5 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(OCC4CC4)cc(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704456 132743 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 465 10 1 8 4.5 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(OCC4CC4)cc(C(C)(C)C)c3)c(=N)n2n1 nan
10184176 205265 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 477 5 3 3 5.4 CC(C)(C)C(=O)NCc1ccc(NC(=O)N2CCC[C@H]2[C@@H](O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL91441 205265 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 477 5 3 3 5.4 CC(C)(C)C(=O)NCc1ccc(NC(=O)N2CCC[C@H]2[C@@H](O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/s0960-894x(01)00538-8
72547305 103382 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 335 3 0 2 5.3 O=C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091983 103382 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 335 3 0 2 5.3 O=C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44306349 102116 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304120 102116 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
11652756 132288 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
CHEMBL370151 132288 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
17187534 59671 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 316 5 2 2 4.3 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Cl)c1 10.1021/ml2002696
CHEMBL1734760 59671 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 316 5 2 2 4.3 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Cl)c1 10.1021/ml2002696
23631375 142070 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 449 3 1 4 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(N)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL389148 142070 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 449 3 1 4 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(N)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL3143317 209419 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
807100 75288 13 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 5 2 2 4.2 Cc1ccccc1C(=O)Nc1cccc(NC(=O)CC(C)C)c1 10.1021/ml2002696
CHEMBL2047300 75288 13 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 5 2 2 4.2 Cc1ccccc1C(=O)Nc1cccc(NC(=O)CC(C)C)c1 10.1021/ml2002696
44306659 102286 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL305188 102286 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
58136855 132767 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 526 10 2 10 2.4 CCNC(=O)c1nn2/c(=N/C)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704480 132767 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 526 10 2 10 2.4 CCNC(=O)c1nn2/c(=N/C)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
23631810 92507 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 526 4 0 4 6.1 CC(C)C(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
CHEMBL244107 92507 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 526 4 0 4 6.1 CC(C)C(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
44187280 124609 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 412 9 1 7 3.2 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OC)cc(C(C)C)c1 nan
CHEMBL3644438 124609 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 412 9 1 7 3.2 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OC)cc(C(C)C)c1 nan
44432707 146118 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 379 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(C4CCCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL392370 146118 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 379 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(C4CCCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
12018758 9242 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL111241 9242 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL3143269 209396 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None COc1ccc(C[C@H](NC(=O)[C@H](Cc2ccc(F)cc2)N(C(C)=O)C(=O)/C=C/c2ccccc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
58046049 132758 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 512 11 2 10 3.4 CCN(CC)c1nn2c(=N)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704471 132758 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 512 11 2 10 3.4 CCN(CC)c1nn2c(=N)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3143284 209404 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44418855 136024 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 3 6.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL373836 136024 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 3 6.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm061043e
44432711 87117 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 377 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccco4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL233546 87117 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 377 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccco4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44432843 87705 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 371 3 0 4 4.4 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)OC[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL234690 87705 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 371 3 0 4 4.4 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)OC[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
44309477 102730 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 803 16 5 6 6.8 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCc1ccccc1 10.1016/s0960-894x(03)00325-1
CHEMBL308435 102730 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 803 16 5 6 6.8 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCc1ccccc1 10.1016/s0960-894x(03)00325-1
10077130 3932 49 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4047 3932 49 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4870 3932 49 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
CHEMBL493982 3932 49 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
DB09030 3932 49 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
10300275 205136 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 493 8 3 3 6.0 CC[C@@H](C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL90698 205136 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 493 8 3 3 6.0 CC[C@@H](C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
44432774 145159 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL391625 145159 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
76313663 103375 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 424 4 0 3 6.0 CN(C)C(=S)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091976 103375 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 424 4 0 3 6.0 CN(C)C(=S)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
10120960 205131 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 578 9 4 5 4.5 CC(C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)c2ccc(S(N)(=O)=O)cc2)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL90682 205131 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 578 9 4 5 4.5 CC(C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)c2ccc(S(N)(=O)=O)cc2)cc1 10.1016/s0960-894x(01)00538-8
44338946 9201 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
CHEMBL110998 9201 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
44280936 116007 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 731 18 9 8 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33617 116007 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 731 18 9 8 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44432831 144373 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 291 2 0 3 3.2 O=C1OC[C@H]2[C@H](/C=C/c3ccccn3)c3ccccc3C[C@@H]12 10.1016/j.bmcl.2007.04.061
CHEMBL391025 144373 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 291 2 0 3 3.2 O=C1OC[C@H]2[C@H](/C=C/c3ccccn3)c3ccccc3C[C@@H]12 10.1016/j.bmcl.2007.04.061
44306065 201740 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 345 2 2 5 4.1 CC(C)(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL65778 201740 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 345 2 2 5 4.1 CC(C)(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
44409082 137951 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 405 4 0 4 5.7 CCOc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL377486 137951 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 405 4 0 4 5.7 CCOc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
44409083 76172 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 467 5 0 4 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL206110 76172 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 467 5 0 4 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
11559190 71744 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 340 3 1 4 4.1 CNc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197782 71744 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 340 3 1 4 4.1 CNc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44305882 201320 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 387 5 0 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N(C)C)nc(N(C)C)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL63305 201320 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 387 5 0 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N(C)C)nc(N(C)C)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
58045963 132757 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 499 11 2 10 3.4 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704470 132757 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 499 11 2 10 3.4 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
90663333 106162 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 843 23 9 8 2.4 CCCC(=O)c1ccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
CHEMBL3143296 106162 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 843 23 9 8 2.4 CCCC(=O)c1ccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
50910547 75429 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 350 5 2 2 4.7 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2C(F)(F)F)c1 10.1021/ml2002696
CHEMBL2048420 75429 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 350 5 2 2 4.7 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2C(F)(F)F)c1 10.1021/ml2002696
44432779 86248 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1cc(F)ccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL231713 86248 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1cc(F)ccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
23631185 92666 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 423 3 0 4 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244294 92666 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 423 3 0 4 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm070704k
59110452 72888 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(Cl)c2Cl)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012497 72888 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(Cl)c2Cl)cn1 10.1016/j.bmcl.2012.01.138
11611061 71711 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
CHEMBL197686 71711 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
44310323 202563 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 791 16 6 7 5.9 NCCCNC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL71246 202563 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 791 16 6 7 5.9 NCCCNC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
127050672 140268 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 491 5 2 5 3.8 CCN(C(=O)CN)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3818932 140268 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 491 5 2 5 3.8 CCN(C(=O)CN)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
90663321 106157 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 850 23 6 8 1.5 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143283 106157 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 850 23 6 8 1.5 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663342 106170 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 828 21 10 8 1.6 CC(=O)N(Oc1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143307 106170 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 828 21 10 8 1.6 CC(=O)N(Oc1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44432704 86590 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 399 3 0 3 6.0 Cc1nc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)ccc1-c1ccccc1 10.1016/j.bmcl.2007.06.002
CHEMBL232539 86590 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 399 3 0 3 6.0 Cc1nc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)ccc1-c1ccccc1 10.1016/j.bmcl.2007.06.002
44306708 100430 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL293867 100430 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44306698 102225 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304827 102225 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
10819322 203195 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL7610 203195 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44280804 99203 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284498 99203 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281069 117562 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 653 16 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34055 117562 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 653 16 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44186917 124607 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 466 10 1 7 4.1 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OCC2CC2)cc(C(C)(C)C)c1 nan
CHEMBL3644436 124607 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 466 10 1 7 4.1 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OCC2CC2)cc(C(C)(C)C)c1 nan
44432716 86255 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 377 3 1 4 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ncc[nH]4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231729 86255 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 377 3 1 4 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ncc[nH]4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44328579 206211 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 537 5 2 5 7.5 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(Cc3ccc(Cl)c(Cl)c3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
CHEMBL97110 206211 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 537 5 2 5 7.5 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(Cc3ccc(Cl)c(Cl)c3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
58136992 124606 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 484 11 1 8 4.1 CCOc1cc(C(=O)C[n+]2nc(N)n3nc(OC(CC)CC)ccc32)cc(C(C)(C)C)c1OCC nan
CHEMBL3644435 124606 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 484 11 1 8 4.1 CCOc1cc(C(=O)C[n+]2nc(N)n3nc(OC(CC)CC)ccc32)cc(C(C)(C)C)c1OCC nan
44432770 86501 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 469 3 0 3 6.6 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232332 86501 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 469 3 0 3 6.6 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
44418847 83001 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4C[C@H](O)CC[C@H]43)nc2)cc1 10.1021/jm061043e
CHEMBL219701 83001 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4C[C@H](O)CC[C@H]43)nc2)cc1 10.1021/jm061043e
11567556 168048 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
CHEMBL436130 168048 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
44432798 144916 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL391436 144916 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
44432817 154167 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 401 3 0 3 5.5 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL399820 154167 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 401 3 0 3 5.5 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
66701509 126995 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 473 3 1 2 5.3 C[C@@H]1CC[C@@H](C)N1C(=O)N1CC(NC(=O)c2ccccc2)CC(c2ccc(C(F)(F)F)cc2)C1 nan
CHEMBL3662509 126995 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 473 3 1 2 5.3 C[C@@H]1CC[C@@H](C)N1C(=O)N1CC(NC(=O)c2ccccc2)CC(c2ccc(C(F)(F)F)cc2)C1 nan
72547554 103388 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091989 103388 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
58136847 132749 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 471 11 2 10 2.3 COCCCOc1cc(C(=O)Cn2nc3c(C)cc(OCCO)nn3c2=N)cc(C(C)(C)C)c1 nan
CHEMBL3704462 132749 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 471 11 2 10 2.3 COCCCOc1cc(C(=O)Cn2nc3c(C)cc(OCCO)nn3c2=N)cc(C(C)(C)C)c1 nan
58136785 132766 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 483 9 2 10 2.3 Cc1cc(OCC2(C)COC2)nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc12 nan
CHEMBL3704479 132766 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 483 9 2 10 2.3 Cc1cc(OCC2(C)COC2)nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc12 nan
58137006 124614 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 551 10 1 9 4.1 CCC(CC)Oc1nn2c(N)n[n+](CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c2cc1C1CC1 nan
CHEMBL3644443 124614 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 551 10 1 9 4.1 CCC(CC)Oc1nn2c(N)n[n+](CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c2cc1C1CC1 nan
9875337 98777 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2Cl)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL281753 98777 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2Cl)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280650 114608 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(Cl)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33435 114608 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(Cl)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
3378161 75528 7 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 360 4 2 2 4.3 CC(C)C(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL2049121 75528 7 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 360 4 2 2 4.3 CC(C)C(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
11603083 70020 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 367 5 0 3 5.4 CCCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL194526 70020 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 367 5 0 3 5.4 CCCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44432717 145698 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 391 3 0 5 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cncn4C)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL392046 145698 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 391 3 0 5 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cncn4C)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44418844 82926 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4C[C@H](O)CC[C@H]43)nc2)c1 10.1021/jm061043e
CHEMBL219282 82926 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4C[C@H](O)CC[C@H]43)nc2)c1 10.1021/jm061043e
58045908 132759 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 513 12 2 10 3.5 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(CC)c1CC nan
CHEMBL3704472 132759 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 513 12 2 10 3.5 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(CC)c1CC nan
44408873 76342 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL206502 76342 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
44408873 76342 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL206502 76342 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
44418850 82974 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 441 3 0 3 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL219522 82974 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 441 3 0 3 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm061043e
23631812 92687 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 484 4 0 5 4.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(S(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244315 92687 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 484 4 0 5 4.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(S(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
9886874 72882 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 393 4 0 3 5.8 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012491 72882 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 393 4 0 3 5.8 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2012.01.138
66761741 126996 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 509 3 1 4 3.1 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCS(=O)(=O)CC2)C1)c1ccccc1 nan
CHEMBL3662510 126996 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 509 3 1 4 3.1 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCS(=O)(=O)CC2)C1)c1ccccc1 nan
44432783 86519 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 437 3 0 3 5.8 O=C1OC[C@H]2[C@@H]1Cc1c(ccc(F)c1F)[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232348 86519 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 437 3 0 3 5.8 O=C1OC[C@H]2[C@@H]1Cc1c(ccc(F)c1F)[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
23631374 92510 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244109 92510 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
127053988 143934 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 486 4 0 6 4.3 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(S(C)(=O)=O)CC1(F)F nan
CHEMBL3906737 143934 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 486 4 0 6 4.3 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(S(C)(=O)=O)CC1(F)F nan
66761350 126750 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 405 4 2 3 3.3 Cc1ccc(C2CC(NC(=O)c3ccccc3)CN(C(=O)C3(N)CCC3)C2)cc1C nan
CHEMBL3658415 126750 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 405 4 2 3 3.3 Cc1ccc(C2CC(NC(=O)c3ccccc3)CN(C(=O)C3(N)CCC3)C2)cc1C nan
44416562 79578 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 373 2 0 3 5.6 CC1(C)OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL212788 79578 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 373 2 0 3 5.6 CC1(C)OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@@H]21 10.1016/j.bmcl.2006.06.042
44416690 80672 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 359 2 0 3 5.2 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL215579 80672 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 359 2 0 3 5.2 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
9847494 5756 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107920 5756 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44408616 74066 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 375 2 0 3 5.6 Cc1ccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL202678 74066 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 375 2 0 3 5.6 Cc1ccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2c1 10.1016/j.bmcl.2005.12.042
44416690 80672 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 359 2 0 3 5.2 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL215579 80672 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 359 2 0 3 5.2 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2007.06.002
11537143 71420 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL196727 71420 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
11544606 71682 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 337 3 0 3 4.7 C=Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197618 71682 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 337 3 0 3 4.7 C=Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44416541 82041 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 373 3 0 3 5.6 CC[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL217611 82041 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 373 3 0 3 5.6 CC[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
11515660 71067 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 341 3 1 4 3.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(CO)n3)[C@H]12 10.1021/jm0502236
CHEMBL196002 71067 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 341 3 1 4 3.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(CO)n3)[C@H]12 10.1021/jm0502236
10925413 140156 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@H]3CCCC[C@@H]3C[C@@H]3C(=O)O[C@@H](C)[C@@H]32)n1 10.1021/jm0502236
CHEMBL381628 140156 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@H]3CCCC[C@@H]3C[C@@H]3C(=O)O[C@@H](C)[C@@H]32)n1 10.1021/jm0502236
44328728 205892 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 379 3 2 5 4.8 CC(C)(C)c1cc(C(=O)Cn2c(N)nc3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
CHEMBL95216 205892 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 379 3 2 5 4.8 CC(C)(C)c1cc(C(=O)Cn2c(N)nc3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
44280935 99614 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc(Cl)c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287368 99614 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc(Cl)c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44189604 124605 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 454 10 1 7 3.9 CCOCc1cc(C(=O)C[n+]2nc(N)n3nc(OC(CC)CC)ccc32)cc(C(C)(C)C)c1 nan
CHEMBL3644434 124605 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 454 10 1 7 3.9 CCOCc1cc(C(=O)C[n+]2nc(N)n3nc(OC(CC)CC)ccc32)cc(C(C)(C)C)c1 nan
23631639 92746 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.3 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
CHEMBL244485 92746 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.3 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
90663358 106174 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 903 22 9 8 3.1 CC(=O)N(C(=O)/C=C/c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143324 106174 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 903 22 9 8 3.1 CC(=O)N(C(=O)/C=C/c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
58045767 132763 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 9 2 9 2.8 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c(CC)c1C nan
CHEMBL3704476 132763 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 9 2 9 2.8 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c(CC)c1C nan
44408874 139705 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 395 2 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(Cl)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL380544 139705 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 395 2 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(Cl)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44432712 87118 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 393 3 0 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccs4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL233548 87118 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 393 3 0 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccs4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44418849 136433 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 6.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4Cl)cn3)[C@H]12 10.1021/jm061043e
CHEMBL374503 136433 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 6.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4Cl)cn3)[C@H]12 10.1021/jm061043e
23631813 148870 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 508 6 0 6 4.8 COCCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
CHEMBL394576 148870 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 508 6 0 6 4.8 COCCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
90663314 106152 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 984 28 11 11 0.6 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143274 106152 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 984 28 11 11 0.6 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
44309750 103085 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 779 15 5 7 6.3 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccco1 10.1016/s0960-894x(03)00325-1
CHEMBL308588 103085 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 779 15 5 7 6.3 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccco1 10.1016/s0960-894x(03)00325-1
90663330 106159 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1cccc(F)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143293 106159 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1cccc(F)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
137661486 158917 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4101591 158917 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
9810474 100674 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 719 19 7 8 2.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
CHEMBL295437 100674 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 719 19 7 8 2.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
9961058 99476 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 645 15 7 7 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(=O)c2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286382 99476 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 645 15 7 7 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(=O)c2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44826171 116353 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2[N+](=O)[O-])n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33818 116353 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2[N+](=O)[O-])n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280684 98668 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 594 15 7 6 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C1C=CC=NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL281079 98668 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 594 15 7 6 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C1C=CC=NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9962227 99169 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 763 18 9 8 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284285 99169 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 763 18 9 8 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280954 116035 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 633 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C1=COc2ccccc2O1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33630 116035 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 633 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C1=COc2ccccc2O1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
90663343 106171 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1cccc2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143308 106171 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1cccc2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
68075447 126745 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 375 3 1 4 2.2 CCc1ccc(C2CC(NC(=O)OC)CN(C(=O)N3CCOCC3)C2)cc1 nan
CHEMBL3658410 126745 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 375 3 1 4 2.2 CCc1ccc(C2CC(NC(=O)OC)CN(C(=O)N3CCOCC3)C2)cc1 nan
877874 23106 16 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL1332325 23106 16 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL3143254 209388 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm960455s
44137613 153975 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3978297 153975 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990813 153975 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
9890926 82861 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218933 82861 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
23631103 143613 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 4 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL390399 143613 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 4 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
127053948 146294 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 488 6 2 5 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NCCO)CC1(F)F nan
CHEMBL3925032 146294 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 488 6 2 5 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NCCO)CC1(F)F nan
66701371 126993 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 461 3 1 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCOCC2)C1)c1ccccc1 nan
CHEMBL3662507 126993 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 461 3 1 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCOCC2)C1)c1ccccc1 nan
66761956 126741 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 420 4 2 2 4.4 CCc1ccc(C2CC(NC(=O)Nc3ccccc3)CN(C(=O)N3CCCC3)C2)cc1 nan
CHEMBL3658407 126741 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 420 4 2 2 4.4 CCc1ccc(C2CC(NC(=O)Nc3ccccc3)CN(C(=O)N3CCCC3)C2)cc1 nan
CHEMBL3143310 209414 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@H](CCCN)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)/C=C/c1ccccc1 10.1021/jm960455s
117072551 140240 30 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 524 7 2 6 3.8 CCN(C(=O)CO)[C@H]1CN(/C(=N\C#N)Nc2cccc(OC(F)F)c2)N=C1c1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.5b01890
CHEMBL3818617 140240 30 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 524 7 2 6 3.8 CCN(C(=O)CO)[C@H]1CN(/C(=N\C#N)Nc2cccc(OC(F)F)c2)N=C1c1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.5b01890
58137003 124613 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 511 8 1 9 3.1 CCOc1nn2c(NC)n[n+](CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c2c(C)c1C nan
CHEMBL3644442 124613 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 511 8 1 9 3.1 CCOc1nn2c(NC)n[n+](CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c2c(C)c1C nan
9895920 99545 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 656 15 7 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cncc(Br)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286837 99545 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 656 15 7 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cncc(Br)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
58045926 132761 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 512 9 2 10 2.0 CCNC(=O)c1nn2/c(=N/C)n(CC(=O)c3cc(OCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704474 132761 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 512 9 2 10 2.0 CCNC(=O)c1nn2/c(=N/C)n(CC(=O)c3cc(OCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
44305942 201304 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 353 2 2 5 4.3 Cc1ccc2cc(Cn3ccc4c5c(N)nc(N)nc5ccc43)ccc2c1 10.1016/s0960-894x(99)00339-x
CHEMBL63192 201304 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 353 2 2 5 4.3 Cc1ccc2cc(Cn3ccc4c5c(N)nc(N)nc5ccc43)ccc2c1 10.1016/s0960-894x(99)00339-x
16046150 165289 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 459 5 2 3 6.2 C[C@@H](O)[C@@H]1[C@H](CO)C[C@@H]2CCCC[C@H]2[C@@H]1/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2006.06.042
CHEMBL424893 165289 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 459 5 2 3 6.2 C[C@@H](O)[C@@H]1[C@H](CO)C[C@@H]2CCCC[C@H]2[C@@H]1/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2006.06.042
70687427 72896 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(OC)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012506 72896 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(OC)c2)cn1 10.1016/j.bmcl.2012.01.138
68074840 126747 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 437 4 1 4 4.1 CCc1ccc(C2CC(OC(=O)Nc3ccccc3)CN(C(=O)N3CCOCC3)C2)cc1 nan
CHEMBL3658412 126747 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 437 4 1 4 4.1 CCc1ccc(C2CC(OC(=O)Nc3ccccc3)CN(C(=O)N3CCOCC3)C2)cc1 nan
23631376 152373 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 477 4 1 4 4.8 CCNC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
CHEMBL397480 152373 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 477 4 1 4 4.8 CCNC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
16214871 18119 3 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of PAR1-mediated aggregation of TRAP-stimulated human plateletInhibition of PAR1-mediated aggregation of TRAP-stimulated human platelet
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270738 18119 3 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of PAR1-mediated aggregation of TRAP-stimulated human plateletInhibition of PAR1-mediated aggregation of TRAP-stimulated human platelet
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cn1 10.1016/j.bmcl.2010.09.009
44306696 101646 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL302433 101646 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
17222608 75284 15 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 316 5 2 2 3.7 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Cl)c1 10.1021/ml2002696
CHEMBL2047284 75284 15 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 316 5 2 2 3.7 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Cl)c1 10.1021/ml2002696
44281174 110968 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 498 11 6 7 0.2 C[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL32762 110968 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 498 11 6 7 0.2 C[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
58045878 132755 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 11 2 10 2.9 CCOc1cc(CC)c2nn(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704469 132755 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 11 2 10 2.9 CCOc1cc(CC)c2nn(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
10771636 106164 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143298 106164 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143281 209402 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3144093 209426 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)CSc1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
23631184 92505 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 423 3 0 4 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244103 92505 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 423 3 0 4 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm070704k
11690507 71745 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 429 4 0 3 6.9 CC(C)c1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
CHEMBL197783 71745 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 429 4 0 3 6.9 CC(C)c1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
11647382 134181 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 5 0 4 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(OCc4ccccc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371850 134181 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 5 0 4 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(OCc4ccccc4)cn3)[C@H]12 10.1021/jm0502236
46931634 126739 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 549 6 1 3 6.6 CCc1ccc(C2CC(NC(=O)c3ccc(-c4cccc(C(F)(F)F)c4)cn3)CN(C(=O)C3CCCC3)C2)cc1 nan
CHEMBL3658405 126739 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 549 6 1 3 6.6 CCc1ccc(C2CC(NC(=O)c3ccc(-c4cccc(C(F)(F)F)c4)cn3)CN(C(=O)C3CCCC3)C2)cc1 nan
9808447 102429 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 583 15 9 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL30612 102429 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 583 15 9 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
127053943 142857 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 424 3 1 5 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
CHEMBL3897962 142857 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 424 3 1 5 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
127053963 146951 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 7 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nnn(C)n2)CC1(F)F nan
CHEMBL3930471 146951 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 7 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nnn(C)n2)CC1(F)F nan
72547307 103379 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
CHEMBL3091980 103379 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
127053957 159762 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cocn2)CC1(F)F nan
CHEMBL4110608 159762 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cocn2)CC1(F)F nan
127053971 159829 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2nccs2)CC1(F)F nan
CHEMBL4111197 159829 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2nccs2)CC1(F)F nan
127053993 146584 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 437 4 1 5 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CN)CC1(F)F nan
CHEMBL3927578 146584 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 437 4 1 5 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CN)CC1(F)F nan
121335547 147279 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 527 5 1 5 5.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccccc2)CC1(F)F nan
CHEMBL3932907 147279 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 527 5 1 5 5.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccccc2)CC1(F)F nan
127053974 159687 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 504 6 1 7 5.0 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2cocn2)CC1(F)F nan
CHEMBL4109959 159687 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 504 6 1 7 5.0 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2cocn2)CC1(F)F nan
117826535 153586 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 438 4 0 5 4.9 CO[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]1[C@@H](C)OC2=O nan
CHEMBL3985342 153586 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 438 4 0 5 4.9 CO[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]1[C@@H](C)OC2=O nan
127053956 160151 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2nccs2)CC1(F)F nan
CHEMBL4113709 160151 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2nccs2)CC1(F)F nan
72547556 103392 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091993 103392 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
127053981 144036 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 477 6 1 5 5.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC2CC2)CC1(F)F nan
CHEMBL3907652 144036 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 477 6 1 5 5.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC2CC2)CC1(F)F nan
127053950 146948 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 438 4 1 5 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CO)CC1(F)F nan
CHEMBL3930467 146948 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 438 4 1 5 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CO)CC1(F)F nan
121335737 150818 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 552 5 1 6 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2cccc(C#N)c2)CC1(F)F nan
CHEMBL3961310 150818 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 552 5 1 6 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2cccc(C#N)c2)CC1(F)F nan
127053940 153076 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 417 3 0 3 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3980810 153076 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 417 3 0 3 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
121335758 145150 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 534 5 1 7 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2nccs2)CC1(F)F nan
CHEMBL3916203 145150 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 534 5 1 7 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2nccs2)CC1(F)F nan
72547556 103392 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091993 103392 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
121335739 144147 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 552 5 1 6 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccc(C#N)cc2)CC1(F)F nan
CHEMBL3908486 144147 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 552 5 1 6 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccc(C#N)cc2)CC1(F)F nan
CHEMBL3143249 209387 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
70685279 72885 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 389 4 0 3 5.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2C)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012494 72885 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 389 4 0 3 5.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2C)cn1 10.1016/j.bmcl.2012.01.138
70683199 72894 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 416 4 1 5 4.6 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012503 72894 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 416 4 1 5 4.6 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1016/j.bmcl.2012.01.138
10246587 71747 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197791 71747 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44432791 154088 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL399407 154088 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
44416542 141168 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 345 2 0 3 4.8 O=C1OC[C@H]2[C@@H](/C=C/c3ccc4ccccc4n3)[C@@H]3CCCCC3=C[C@@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL385694 141168 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 345 2 0 3 4.8 O=C1OC[C@H]2[C@@H](/C=C/c3ccc4ccccc4n3)[C@@H]3CCCCC3=C[C@@H]12 10.1016/j.bmcl.2006.06.042
23630914 143337 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 505 3 0 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CS(=O)(=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL390182 143337 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 505 3 0 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CS(=O)(=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
44309450 202352 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1cccc2c1c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
CHEMBL70013 202352 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1cccc2c1c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
44416588 80772 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 363 2 1 3 5.0 C[C@H]1O[C@@H](O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL215837 80772 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 363 2 1 3 5.0 C[C@H]1O[C@@H](O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
76309942 103387 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 3 5.8 CCOC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091988 103387 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 3 5.8 CCOC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44280767 114073 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 577 15 9 8 -1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33377 114073 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 577 15 9 8 -1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280877 116358 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 589 15 9 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33820 116358 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 589 15 9 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1016/s0960-894x(99)00197-3
9851501 116708 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33946 116708 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281081 119185 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34738 119185 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44584152 14713 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]thrombin from thrombin receptor in human platelet membraneDisplacement of [125I]thrombin from thrombin receptor in human platelet membrane
ChEMBL 602 7 5 9 3.3 O=S(=O)(O)OC(=C\c1cc(O)c(O)c(Br)c1)/C(=C\c1ccc(O)c(Br)c1)OS(=O)(=O)O 10.1021/np50120a023
CHEMBL1207950 14713 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]thrombin from thrombin receptor in human platelet membraneDisplacement of [125I]thrombin from thrombin receptor in human platelet membrane
ChEMBL 602 7 5 9 3.3 O=S(=O)(O)OC(=C\c1cc(O)c(O)c(Br)c1)/C(=C\c1ccc(O)c(Br)c1)OS(=O)(=O)O 10.1021/np50120a023
CHEMBL462733 14713 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]thrombin from thrombin receptor in human platelet membraneDisplacement of [125I]thrombin from thrombin receptor in human platelet membrane
ChEMBL 602 7 5 9 3.3 O=S(=O)(O)OC(=C\c1cc(O)c(O)c(Br)c1)/C(=C\c1ccc(O)c(Br)c1)OS(=O)(=O)O 10.1021/np50120a023
11611425 71885 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)cc1 10.1021/jm0502236
CHEMBL198175 71885 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)cc1 10.1021/jm0502236
58045970 132760 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 511 12 2 10 3.4 COc1c(OCCCCO)cc(C(=O)Cn2nc3c(C)cc(OCC4CC4)nn3c2=N)cc1C(C)(C)C nan
CHEMBL3704473 132760 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 511 12 2 10 3.4 COc1c(OCCCCO)cc(C(=O)Cn2nc3c(C)cc(OCC4CC4)nn3c2=N)cc1C(C)(C)C nan
44432720 146765 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 404 3 0 4 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc[n+]([O-])c4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL392905 146765 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 404 3 0 4 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc[n+]([O-])c4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44137613 153975 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3978297 153975 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990813 153975 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3143309 209413 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)COc1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
23631186 92667 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 4 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4Cl)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244295 92667 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 4 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4Cl)cn3)[C@H]12 10.1021/jm070704k
70687424 72887 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 400 4 0 4 5.5 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012496 72887 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 400 4 0 4 5.5 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1016/j.bmcl.2012.01.138
46931416 127000 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 467 3 2 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)C1CCCC1 nan
CHEMBL3662514 127000 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 467 3 2 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)C1CCCC1 nan
9869359 86354 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 471 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1c(F)cc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232172 86354 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 471 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1c(F)cc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
90663293 106143 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 998 29 11 11 1.0 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CCC(N)=O 10.1021/jm960455s
CHEMBL3143252 106143 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 998 29 11 11 1.0 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CCC(N)=O 10.1021/jm960455s
72547551 103380 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
CHEMBL3091981 103380 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
72547308 103390 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091991 103390 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
11544845 133032 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 351 3 0 3 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(C4CC4)n3)[C@H]12 10.1021/jm0502236
CHEMBL371109 133032 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 351 3 0 3 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(C4CC4)n3)[C@H]12 10.1021/jm0502236
44187825 124612 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 453 6 1 8 2.2 CCc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(N2CCOCC2)c(OC)c(C(C)(C)C)c1 nan
CHEMBL3644441 124612 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 453 6 1 8 2.2 CCc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(N2CCOCC2)c(OC)c(C(C)(C)C)c1 nan
10227544 204790 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 477 7 3 3 5.4 CC(C)(C)C(=O)NCc1ccc(NC(=O)N(C[C@@H](O)c2ccc(Cl)c(Cl)c2)C2CC2)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL88513 204790 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 477 7 3 3 5.4 CC(C)(C)C(=O)NCc1ccc(NC(=O)N(C[C@@H](O)c2ccc(Cl)c(Cl)c2)C2CC2)cc1 10.1016/s0960-894x(01)00538-8
76309941 103371 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3091972 103371 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
11688420 134730 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1ccnc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)c1 10.1021/jm0502236
CHEMBL372591 134730 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1ccnc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)c1 10.1021/jm0502236
44338787 6800 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
CHEMBL108428 6800 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
44432719 86298 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccncc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231944 86298 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccncc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44409039 140736 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 460 3 1 4 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(NC(=O)C(C)(C)C)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL383216 140736 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 460 3 1 4 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(NC(=O)C(C)(C)C)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44416654 79991 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 407 4 0 4 5.7 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)O[C@@H](OC)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL214575 79991 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 407 4 0 4 5.7 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)O[C@@H](OC)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
58045981 132762 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 8 2 9 3.0 Cc1c(OC(C)C)nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c1C nan
CHEMBL3704475 132762 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 8 2 9 3.0 Cc1c(OC(C)C)nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c1C nan
44409077 76234 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 480 4 1 4 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(NC(=O)c5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL206325 76234 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 480 4 1 4 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(NC(=O)c5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
23630913 92665 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 473 3 0 4 6.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CSCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244290 92665 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 473 3 0 4 6.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CSCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
59110450 72881 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 393 4 0 3 5.8 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2F)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012490 72881 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 393 4 0 3 5.8 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2F)cn1 10.1016/j.bmcl.2012.01.138
44432718 86296 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccn4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231942 86296 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccn4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
9908345 86297 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccnc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231943 86297 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccnc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
9844209 71987 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm0502236
CHEMBL198473 71987 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm0502236
90663360 106176 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 795 21 9 9 1.2 CC(=O)N(Oc1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143326 106176 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 795 21 9 9 1.2 CC(=O)N(Oc1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
72547306 103372 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 337 3 1 2 5.1 OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091973 103372 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 337 3 1 2 5.1 OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
9853816 96875 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL269345 96875 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
49766546 75433 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 358 6 2 2 5.3 CCCC(=O)Nc1cccc(NC(=O)c2cccc(-c3ccccc3)c2)c1 10.1021/ml2002696
CHEMBL2048430 75433 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 358 6 2 2 5.3 CCCC(=O)Nc1cccc(NC(=O)c2cccc(-c3ccccc3)c2)c1 10.1021/ml2002696
44280608 99628 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 731 18 9 8 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(F)=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287468 99628 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 731 18 9 8 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(F)=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44309838 96091 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1cccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c12)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
CHEMBL262932 96091 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1cccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c12)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
44339001 108989 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
CHEMBL322093 108989 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
23631554 92745 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.3 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
CHEMBL244484 92745 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.3 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
44432842 144768 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 399 3 0 4 5.2 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)OC(C)(C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL391324 144768 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 399 3 0 4 5.2 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)OC(C)(C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
44432771 154284 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 469 3 0 3 6.6 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL400435 154284 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 469 3 0 3 6.6 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
70687423 72878 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 445 5 0 3 6.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1CCc1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012487 72878 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 445 5 0 3 6.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1CCc1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2012.01.138
53245483 75524 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 394 5 2 2 5.1 CCCC(=O)Nc1cccc(NC(=O)c2c(Cl)cccc2Br)c1 10.1021/ml2002696
CHEMBL2049116 75524 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 394 5 2 2 5.1 CCCC(=O)Nc1cccc(NC(=O)c2c(Cl)cccc2Br)c1 10.1021/ml2002696
90663338 106166 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 833 22 9 9 1.8 C=CC(=O)c1ccsc1N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143302 106166 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 833 22 9 9 1.8 C=CC(=O)c1ccsc1N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143246 209385 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC#Cc1ccccc1C(=O)N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143249 209387 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
9934461 136223 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL374106 136223 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
44309461 202105 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 795 15 5 7 6.8 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1cccs1 10.1016/s0960-894x(03)00325-1
CHEMBL68372 202105 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 795 15 5 7 6.8 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1cccs1 10.1016/s0960-894x(03)00325-1
76331784 103386 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 336 3 1 2 5.1 NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091987 103386 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 336 3 1 2 5.1 NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
76324547 103389 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 404 5 1 2 5.6 O=C(NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)C1CC1 10.1021/ml400235c
CHEMBL3091990 103389 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 404 5 1 2 5.6 O=C(NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)C1CC1 10.1021/ml400235c
44306903 101769 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303157 101769 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44280683 98933 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL282733 98933 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281070 111843 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 633 15 7 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2s1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL32941 111843 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 633 15 7 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2s1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
90663339 106167 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 883 21 9 8 3.1 CC(=O)N(C(=O)c1cccc(C2CCCCC2)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143303 106167 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 883 21 9 8 3.1 CC(=O)N(C(=O)c1cccc(C2CCCCC2)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
58045960 132765 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 453 7 1 8 4.1 CCOc1nn2c(=N)n(CC(=O)c3cc(C(C)(C)C)cc(C(C)(C)OC)c3)nc2c(C)c1C nan
CHEMBL3704478 132765 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 453 7 1 8 4.1 CCOc1nn2c(=N)n(CC(=O)c3cc(C(C)(C)C)cc(C(C)(C)OC)c3)nc2c(C)c1C nan
46931633 126742 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 433 5 1 2 5.0 CCc1ccc(C2CC(NC(=O)N(C)c3ccccc3)CN(C(=O)C3CCCC3)C2)cc1 nan
CHEMBL3658408 126742 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 433 5 1 2 5.0 CCc1ccc(C2CC(NC(=O)N(C)c3ccccc3)CN(C(=O)C3CCCC3)C2)cc1 nan
10557086 106153 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143276 106153 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10747898 106204 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143683 106204 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143311 209415 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143320 209421 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None C/C=C/C=C/CC(=O)N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
60003490 72879 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012488 72879 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2012.01.138
9804049 133027 2 None - 1 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371069 133027 2 None - 1 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
44306697 102246 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304924 102246 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44280949 102228 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 651 15 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc2c(c1)-c1ccccc1-2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL30484 102228 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 651 15 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc2c(c1)-c1ccccc1-2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281079 116704 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(Cl)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33945 116704 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(Cl)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
58045994 132745 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 458 5 1 9 2.7 COc1c(N2CCOCC2)cc(C(=O)Cn2nc3ccc(Cl)nn3c2=N)cc1C(C)(C)C nan
CHEMBL3704458 132745 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 458 5 1 9 2.7 COc1c(N2CCOCC2)cc(C(=O)Cn2nc3ccc(Cl)nn3c2=N)cc1C(C)(C)C nan
44290206 172960 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 763 20 7 8 3.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(C)c2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL45317 172960 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 763 20 7 8 3.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(C)c2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
44290207 172963 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 729 19 7 8 2.1 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL45318 172963 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 729 19 7 8 2.1 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL3143313 209416 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
46931630 126746 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 454 7 1 3 4.2 CCc1ccc(C2CC(NS(=O)(=O)Cc3ccccc3)CN(C(=O)C3CCCC3)C2)cc1 nan
CHEMBL3658411 126746 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 454 7 1 3 4.2 CCc1ccc(C2CC(NS(=O)(=O)Cc3ccccc3)CN(C(=O)C3CCCC3)C2)cc1 nan
9897054 102669 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 773 16 5 7 5.9 CSCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN 10.1016/s0960-894x(03)00325-1
CHEMBL308050 102669 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 773 16 5 7 5.9 CSCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN 10.1016/s0960-894x(03)00325-1
11803290 106154 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143277 106154 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663316 106155 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 1002 28 11 11 0.7 CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143278 106155 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 1002 28 11 11 0.7 CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
70854697 126999 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 476 3 1 4 3.4 Cc1cccc(C(=O)NC2CC(c3ccc(C(F)(F)F)cc3)CN(C(=O)N3CCOCC3)C2)n1 nan
CHEMBL3662513 126999 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 476 3 1 4 3.4 Cc1cccc(C(=O)NC2CC(c3ccc(C(F)(F)F)cc3)CN(C(=O)N3CCOCC3)C2)n1 nan
44409057 140654 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 510 6 1 5 6.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)Nc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL382830 140654 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 510 6 1 5 6.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)Nc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
23631105 141477 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 407 3 0 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm070704k
CHEMBL387603 141477 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 407 3 0 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm070704k
23631464 152382 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 590 5 0 5 7.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)OCc4ccccc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL397491 152382 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 590 5 0 5 7.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)OCc4ccccc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
59110475 72883 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 0 3 6.3 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2Cl)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012492 72883 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 0 3 6.3 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2Cl)cn1 10.1016/j.bmcl.2012.01.138
11583548 71956 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 465 3 0 3 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Br)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL198375 71956 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 465 3 0 3 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Br)c4)cn3)[C@H]12 10.1021/jm0502236
11502485 168489 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 412 3 0 4 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL439681 168489 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 412 3 0 4 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@H]12 10.1021/jm0502236
44339173 8125 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL109226 8125 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
11610042 133068 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 353 4 0 3 5.1 CCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL371294 133068 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 353 4 0 3 5.1 CCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
58045796 132751 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 11 1 10 2.9 CCOc1cc(C)c2nn(CC(=O)c3cc(OC(COC)COC)cc(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704464 132751 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 11 1 10 2.9 CCOc1cc(C)c2nn(CC(=O)c3cc(OC(COC)COC)cc(C(C)(C)C)c3)c(=N)n2n1 nan
44306657 101776 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303187 101776 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306403 201165 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL62584 201165 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
44280805 99302 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 567 15 7 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccoc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285186 99302 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 567 15 7 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccoc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
58045925 132754 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 515 11 3 11 2.6 CCOc1cc(C(C)(C)O)c2nn(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704468 132754 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 515 11 3 11 2.6 CCOc1cc(C(C)(C)O)c2nn(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
11803426 106203 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 793 20 10 7 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143682 106203 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 793 20 10 7 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10459564 514 34 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
4048 514 34 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
CHEMBL2103856 514 34 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
DB12046 514 34 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
23631104 92414 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 407 3 0 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL243913 92414 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 407 3 0 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
23631106 92504 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 425 3 0 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4F)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244102 92504 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 425 3 0 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4F)cn3)[C@H]12 10.1021/jm070704k
72547552 103393 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3091994 103393 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
127053982 145122 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 465 4 1 5 4.4 CC(=O)N[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)C1[C@@H](C)OC2=O nan
CHEMBL3915979 145122 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 465 4 1 5 4.4 CC(=O)N[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)C1[C@@H](C)OC2=O nan
11582568 140351 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm0502236
CHEMBL382104 140351 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm0502236
90663297 106145 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143256 106145 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10276545 9042 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL110024 9042 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
1048267 32197 87 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL1411333 32197 87 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
44306540 201338 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL63402 201338 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306499 201645 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL65004 201645 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
44280905 99602 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 646 15 7 6 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc(Cl)c(Cl)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287270 99602 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 646 15 7 6 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc(Cl)c(Cl)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44306066 100155 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 333 4 2 6 3.2 CCOc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL292032 100155 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 333 4 2 6 3.2 CCOc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
44432706 86295 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 339 3 0 3 4.7 CCc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1016/j.bmcl.2007.06.002
CHEMBL231938 86295 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 339 3 0 3 4.7 CCc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1016/j.bmcl.2007.06.002
50910549 75285 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 362 4 2 3 4.3 CCOC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL2047286 75285 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 362 4 2 3 4.3 CCOC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
59110483 72890 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 1 4 4.9 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012499 72890 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 1 4 4.9 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2012.01.138
9865055 70939 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 387 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL195729 70939 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 387 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
9865055 70939 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 387 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL195729 70939 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 387 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL3143248 209386 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)CCCN)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44290102 100825 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 820 21 8 9 2.5 CC(C)C(N)C(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL296565 100825 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 820 21 8 9 2.5 CC(C)C(N)C(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
44290300 177911 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 798 21 8 9 2.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC2CCCCC2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL46658 177911 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 798 21 8 9 2.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC2CCCCC2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
44280835 99629 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 573 15 10 9 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287469 99629 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 573 15 10 9 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1016/s0960-894x(99)00197-3
44409228 140127 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 520 6 1 6 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCCNC(=O)OC(C)(C)C)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL381506 140127 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 520 6 1 6 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCCNC(=O)OC(C)(C)C)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44182739 123947 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 510 9 1 10 3.6 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3640033 123947 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 510 9 1 10 3.6 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
11432492 154014 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3912154 154014 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3991167 154014 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3143271 209398 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143282 209403 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44409034 75039 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 446 5 1 4 6.0 CCCC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL203992 75039 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 446 5 1 4 6.0 CCCC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
44418854 82246 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 441 3 0 3 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm061043e
CHEMBL217958 82246 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 441 3 0 3 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm061043e
44418838 82994 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL219643 82994 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm061043e
16100352 136395 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@H]3[C@@H](CCC[C@H]3O)[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL374265 136395 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@H]3[C@@H](CCC[C@H]3O)[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
59110442 72884 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 0 3 6.3 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012493 72884 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 0 3 6.3 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2012.01.138
11661666 140028 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
CHEMBL381226 140028 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
76317165 103373 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 427 6 0 2 7.3 Fc1cccc(-c2ccc(/C=C/[C@H]3C(OCc4ccccc4)C[C@@H]4CCCC[C@@H]43)nc2)c1 10.1021/ml400235c
CHEMBL3091974 103373 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 427 6 0 2 7.3 Fc1cccc(-c2ccc(/C=C/[C@H]3C(OCc4ccccc4)C[C@@H]4CCCC[C@@H]43)nc2)c1 10.1021/ml400235c
44432705 86752 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 413 4 0 3 6.2 CCc1nc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)ccc1-c1ccccc1 10.1016/j.bmcl.2007.06.002
CHEMBL232726 86752 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 413 4 0 3 6.2 CCc1nc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)ccc1-c1ccccc1 10.1016/j.bmcl.2007.06.002
1047178 206408 4 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 490 6 2 6 5.6 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(CCN3CCCCC3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
CHEMBL98231 206408 4 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 490 6 2 6 5.6 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(CCN3CCCCC3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
10628873 106139 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 749 20 10 8 0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccoc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143247 106139 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 749 20 10 8 0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccoc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
66761216 126735 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 410 6 1 2 4.8 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)C(C)(C)CF)C2)cc1 nan
CHEMBL3658401 126735 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 410 6 1 2 4.8 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)C(C)(C)CF)C2)cc1 nan
11249717 153890 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3903962 153890 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990074 153890 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
44432775 86587 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232536 86587 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
11618945 140151 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 435 5 1 5 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL381593 140151 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 435 5 1 5 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44432708 86944 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 380 3 0 4 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL233343 86944 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 380 3 0 4 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44339002 9245 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111258 9245 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
44409278 77268 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 6 1 5 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)NC5CC5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL208835 77268 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 6 1 5 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)NC5CC5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
50910548 75287 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 374 5 2 2 4.7 CC(C)CC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL2047299 75287 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 374 5 2 2 4.7 CC(C)CC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
44281080 99447 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286211 99447 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
90663332 106161 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1ccc2ccccc2c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143295 106161 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1ccc2ccccc2c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
23631640 168175 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 485 4 0 6 5.1 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
CHEMBL437171 168175 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 485 4 0 6 5.1 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
127053980 142851 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 517 6 1 7 4.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2nccn2C)CC1(F)F nan
CHEMBL3897916 142851 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 517 6 1 7 4.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2nccn2C)CC1(F)F nan
121335755 144437 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 562 5 1 6 5.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccc(Cl)nc2)CC1(F)F nan
CHEMBL3910807 144437 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 562 5 1 6 5.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccc(Cl)nc2)CC1(F)F nan
121335757 153668 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 545 5 1 5 5.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2cccc(F)c2)CC1(F)F nan
CHEMBL3985965 153668 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 545 5 1 5 5.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2cccc(F)c2)CC1(F)F nan
127053954 160148 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 5 1 6 5.6 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ccccn2)CC1(F)F nan
CHEMBL4113629 160148 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 5 1 6 5.6 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ccccn2)CC1(F)F nan
127053978 143958 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2ccccn2)CC1(F)F nan
CHEMBL3906932 143958 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2ccccn2)CC1(F)F nan
127053964 148897 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 476 4 0 8 3.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(n2cnnn2)CC1(F)F nan
CHEMBL3945945 148897 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 476 4 0 8 3.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(n2cnnn2)CC1(F)F nan
127053958 160299 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ncco2)CC1(F)F nan
CHEMBL4114937 160299 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ncco2)CC1(F)F nan
127053959 144283 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 456 4 0 4 6.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(CC#N)CC1(F)F nan
CHEMBL3909563 144283 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 456 4 0 4 6.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(CC#N)CC1(F)F nan
127053990 151950 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 437 3 1 5 4.5 Cc1cccc(-c2ccc(/C=C/[C@@H]3C4[C@@H](C)OC(=O)[C@]4(N)CC(F)(F)[C@H]3C)nc2)c1C#N nan
CHEMBL3971211 151950 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 437 3 1 5 4.5 Cc1cccc(-c2ccc(/C=C/[C@@H]3C4[C@@H](C)OC(=O)[C@]4(N)CC(F)(F)[C@H]3C)nc2)c1C#N nan
127053953 160241 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 5 5.1 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NC2CCC2)CC1(F)F nan
CHEMBL4114406 160241 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 5 5.1 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NC2CCC2)CC1(F)F nan
121335756 152738 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 532 5 1 7 5.0 Cc1cc(C(=O)N[C@@]23CC(F)(F)[C@@H](C)[C@H](/C=C/c4ccc(-c5ccccc5C#N)cn4)[C@@H]2[C@@H](C)OC3=O)no1 nan
CHEMBL3977807 152738 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 532 5 1 7 5.0 Cc1cc(C(=O)N[C@@]23CC(F)(F)[C@@H](C)[C@H](/C=C/c4ccc(-c5ccccc5C#N)cn4)[C@@H]2[C@@H](C)OC3=O)no1 nan
127053946 153055 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 459 4 0 5 4.9 COC(=O)[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)C1[C@@H](C)OC2=O nan
CHEMBL3980639 153055 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 459 4 0 5 4.9 COC(=O)[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)C1[C@@H](C)OC2=O nan
121335541 142179 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 491 5 1 5 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)C2CC2)CC1(F)F nan
CHEMBL3892331 142179 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 491 5 1 5 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)C2CC2)CC1(F)F nan
127053986 159380 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 531 5 1 7 4.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@@]2(NC(=O)c2ccn(C)n2)CC1(F)F nan
CHEMBL4107269 159380 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 531 5 1 7 4.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@@]2(NC(=O)c2ccn(C)n2)CC1(F)F nan
127053972 160338 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2ccncc2)CC1(F)F nan
CHEMBL4115204 160338 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2ccncc2)CC1(F)F nan
127050673 140234 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 506 6 1 5 4.5 CCN(C(=O)COC)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3818510 140234 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 506 6 1 5 4.5 CCN(C(=O)COC)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
127050934 140264 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 404 7 2 5 1.8 CCCCN/C(=N/C#N)N1CC(N(CC)C(=O)CO)C(c2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01890
CHEMBL3818898 140264 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 404 7 2 5 1.8 CCCCN/C(=N/C#N)N1CC(N(CC)C(=O)CO)C(c2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01890
11432492 154014 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3912154 154014 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3991167 154014 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
44409232 75543 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 376 2 1 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(N)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL204955 75543 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 376 2 1 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(N)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44305776 100160 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR1 (unknown origin) assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 (unknown origin) assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 331 3 2 5 3.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1039/c4md00485j
CHEMBL292089 100160 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR1 (unknown origin) assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 (unknown origin) assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 331 3 2 5 3.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1039/c4md00485j
11537143 71420 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
CHEMBL196727 71420 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
44409076 140008 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 443 3 0 4 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5cccs5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL381121 140008 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 443 3 0 4 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5cccs5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44409033 140782 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 505 3 0 3 7.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5cccc(C(F)(F)F)c5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL383479 140782 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 505 3 0 3 7.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5cccc(C(F)(F)F)c5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44306762 201402 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL63966 201402 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
11537143 71420 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL196727 71420 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44305776 100160 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 331 3 2 5 3.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL292089 100160 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 331 3 2 5 3.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
50910530 75526 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 5 2 2 4.3 CCCC(=O)Nc1cccc(NC(=O)c2c(C)cccc2C)c1 10.1021/ml2002696
CHEMBL2049118 75526 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 5 2 2 4.3 CCCC(=O)Nc1cccc(NC(=O)c2c(C)cccc2C)c1 10.1021/ml2002696
44280660 99403 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 617 15 7 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285915 99403 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 617 15 7 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280651 114921 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 781 18 9 8 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33506 114921 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 781 18 9 8 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9831601 100004 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 704 17 6 7 3.5 CC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
CHEMBL290927 100004 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 704 17 6 7 3.5 CC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
10077130 3932 49 None - 1 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4047 3932 49 None - 1 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4870 3932 49 None - 1 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
CHEMBL493982 3932 49 None - 1 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
DB09030 3932 49 None - 1 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
44432767 86549 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 453 3 0 3 6.0 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232372 86549 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 453 3 0 3 6.0 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
44309777 202602 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 810 17 5 7 6.0 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
CHEMBL71444 202602 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 810 17 5 7 6.0 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
90663340 106168 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1ccsc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143304 106168 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1ccsc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306660 202117 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL68458 202117 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
9960837 115021 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 629 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33532 115021 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 629 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280607 167277 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 789 19 9 8 3.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(=C/c2ccccc2)c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL430930 167277 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 789 19 9 8 3.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(=C/c2ccccc2)c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280667 102460 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 738 18 9 9 1.4 N#Cc1ccc(/C=C/C(=O)Nc2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n[nH]2)cc1 10.1016/s0960-894x(99)00197-3
CHEMBL30635 102460 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 738 18 9 9 1.4 N#Cc1ccc(/C=C/C(=O)Nc2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n[nH]2)cc1 10.1016/s0960-894x(99)00197-3
1361448 75525 7 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 350 5 2 2 5.0 CCCC(=O)Nc1cccc(NC(=O)c2cccc(Cl)c2Cl)c1 10.1021/ml2002696
CHEMBL2049117 75525 7 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 350 5 2 2 5.0 CCCC(=O)Nc1cccc(NC(=O)c2cccc(Cl)c2Cl)c1 10.1021/ml2002696
44432840 87704 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)O[C@@H](C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL234688 87704 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)O[C@@H](C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL3143270 209397 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306894 102226 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304829 102226 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44305944 101754 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 373 5 1 5 4.9 CNc1nc(N(C)C)nc2ccc3c(ccn3Cc3ccc(C(C)C)cc3)c12 10.1016/s0960-894x(99)00339-x
CHEMBL303084 101754 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 373 5 1 5 4.9 CNc1nc(N(C)C)nc2ccc3c(ccn3Cc3ccc(C(C)C)cc3)c12 10.1016/s0960-894x(99)00339-x
11509594 69320 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)cc1 10.1021/jm0502236
CHEMBL193537 69320 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)cc1 10.1021/jm0502236
11702885 70035 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 341 3 0 4 4.1 COc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
CHEMBL194533 70035 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 341 3 0 4 4.1 COc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
44432778 145432 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL391833 145432 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
76328107 103391 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 351 3 1 2 5.5 CC1(O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091992 103391 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 351 3 1 2 5.5 CC1(O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
59110479 72892 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 405 4 1 4 5.0 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2C)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012501 72892 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 405 4 1 4 5.0 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2C)cn1 10.1016/j.bmcl.2012.01.138
2858257 112092 12 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 483 5 2 5 6.5 Cc1ccc(Cn2c(=N)n(CC(=O)c3cc(C(C)(C)C)c(O)c(C(C)(C)C)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00555-8
CHEMBL330204 112092 12 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 483 5 2 5 6.5 Cc1ccc(Cn2c(=N)n(CC(=O)c3cc(C(C)(C)C)c(O)c(C(C)(C)C)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00555-8
71736053 143330 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 532 5 1 7 5.0 Cc1oncc1C(=O)N[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]1[C@@H](C)OC2=O nan
CHEMBL3901770 143330 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 532 5 1 7 5.0 Cc1oncc1C(=O)N[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]1[C@@H](C)OC2=O nan
23631275 92668 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 461 4 0 6 4.4 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3ccccn3)cn2)C1 10.1021/jm070704k
CHEMBL244298 92668 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 461 4 0 6 4.4 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3ccccn3)cn2)C1 10.1021/jm070704k
66761314 126994 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 475 3 2 3 3.9 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)c1ccccc1 nan
CHEMBL3662508 126994 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 475 3 2 3 3.9 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)c1ccccc1 nan
44309751 102670 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccn1 10.1016/s0960-894x(03)00325-1
CHEMBL308052 102670 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccn1 10.1016/s0960-894x(03)00325-1
44432786 86256 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1cccc(F)c1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL231732 86256 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1cccc(F)c1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
44432710 154312 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 471 4 0 5 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCN(c5ccccc5)CC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL400634 154312 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 471 4 0 5 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCN(c5ccccc5)CC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44306611 201899 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL66958 201899 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL3143266 209394 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(C)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143279 209401 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143315 209417 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
51003683 75286 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL2047297 75286 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL4227548 75286 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL3143287 209405 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@H](Cc1cccnc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
127053992 150057 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 1 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3-c3nnn[nH]3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3955189 150057 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 1 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3-c3nnn[nH]3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
44309958 202596 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 795 15 5 7 6.5 NCCNC(=O)[C@H](Cc1cccs1)NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL71411 202596 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 795 15 5 7 6.5 NCCNC(=O)[C@H](Cc1cccs1)NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL3143268 209395 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CCCCC/C=C/CC(=O)N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
70685280 72893 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 405 4 1 4 5.0 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012502 72893 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 405 4 1 4 5.0 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C)c2)cn1 10.1016/j.bmcl.2012.01.138
11697104 71784 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL197903 71784 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm0502236
90663341 106169 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143306 106169 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44432692 87796 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 323 2 0 3 4.3 Cc1cccc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)n1 10.1016/j.bmcl.2007.06.002
CHEMBL234804 87796 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 323 2 0 3 4.3 Cc1cccc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)n1 10.1016/j.bmcl.2007.06.002
44416563 137872 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 341 3 1 3 4.5 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)O[C@@H](O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
CHEMBL377378 137872 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 341 3 1 3 4.5 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)O[C@@H](O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
44306658 101712 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 835 19 6 9 5.0 COC(=O)c1ccc(Cn2cc(CN3CCCC3)c3ccc(NC(=O)N[C@@H](Cc4ccc(OC)cc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC4CCCCC4)cc32)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL302823 101712 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 835 19 6 9 5.0 COC(=O)c1ccc(Cn2cc(CN3CCCC3)c3ccc(NC(=O)N[C@@H](Cc4ccc(OC)cc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC4CCCCC4)cc32)cc1 10.1016/s0960-894x(01)00378-x
11703925 140580 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 395 7 0 3 6.2 CCCCCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL382733 140580 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 395 7 0 3 6.2 CCCCCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
66701444 126740 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 384 4 1 2 4.3 CCc1ccc(C2CC(NC(=O)C(C)(C)C)CN(C(=O)C3CCCC3)C2)cc1 nan
CHEMBL3658406 126740 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 384 4 1 2 4.3 CCc1ccc(C2CC(NC(=O)C(C)(C)C)CN(C(=O)C3CCCC3)C2)cc1 nan
3751851 206366 10 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 435 6 2 5 5.9 CCCCn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
CHEMBL97952 206366 10 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 435 6 2 5 5.9 CCCCn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
44432713 145435 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 427 3 0 4 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(Cl)s4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL391834 145435 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 427 3 0 4 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(Cl)s4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
76317166 103385 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 456 5 1 3 7.3 O=C(Nc1ccccc1)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091986 103385 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 456 5 1 3 7.3 O=C(Nc1ccccc1)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44432691 87795 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 309 2 0 3 4.0 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccccn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL234803 87795 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 309 2 0 3 4.0 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccccn3)[C@H]12 10.1016/j.bmcl.2007.06.002
58136821 132753 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 8 1 9 2.6 CCOc1nn2/c(=N/C)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704467 132753 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 8 1 9 2.6 CCOc1nn2/c(=N/C)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL4115741 211154 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL None None None None nan
11718309 70222 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 4 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(Cc4ccccc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL194920 70222 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 4 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(Cc4ccccc4)cn3)[C@H]12 10.1021/jm0502236
16100350 136239 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 491 3 0 3 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL374122 136239 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 491 3 0 3 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
23631279 142910 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 524 4 0 4 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL389835 142910 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 524 4 0 4 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
90663302 106148 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 9 7 1.1 CC(=O)N(C1CCCC1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143262 106148 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 9 7 1.1 CC(=O)N(C1CCCC1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143259 209390 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
23630915 92744 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 489 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[S+]([O-])CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244483 92744 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 489 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[S+]([O-])CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
44416717 80152 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 343 5 2 3 4.1 CCc1cccc(/C=C/[C@@H]2[C@H]([C@@H](C)O)[C@H](CO)C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
CHEMBL214956 80152 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 343 5 2 3 4.1 CCc1cccc(/C=C/[C@@H]2[C@H]([C@@H](C)O)[C@H](CO)C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
44418842 137344 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 437 3 1 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL376285 137344 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 437 3 1 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm061043e
127053952 159997 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 579 4 1 7 5.5 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C2(O)CN(C(=O)OC(C)(C)C)C2)CC1(F)F nan
CHEMBL4112571 159997 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 579 4 1 7 5.5 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C2(O)CN(C(=O)OC(C)(C)C)C2)CC1(F)F nan
44306500 167342 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL431369 167342 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
53245451 75523 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 394 5 2 2 5.1 CCCC(=O)Nc1cccc(NC(=O)c2cc(Cl)ccc2Br)c1 10.1021/ml2002696
CHEMBL2049115 75523 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 394 5 2 2 5.1 CCCC(=O)Nc1cccc(NC(=O)c2cc(Cl)ccc2Br)c1 10.1021/ml2002696
CHEMBL3143290 209408 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44408711 75050 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 375 2 0 3 5.6 Cc1cccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc12 10.1016/j.bmcl.2005.12.042
CHEMBL204064 75050 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 375 2 0 3 5.6 Cc1cccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc12 10.1016/j.bmcl.2005.12.042
53245435 75521 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 378 5 2 2 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccc(F)cc2Br)c1 10.1021/ml2002696
CHEMBL2049113 75521 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 378 5 2 2 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccc(F)cc2Br)c1 10.1021/ml2002696
72547554 103388 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091989 103388 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
56671606 62846 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 834 22 8 9 2.9 CC[C@@H](C)[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL1790240 62846 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 834 22 8 9 2.9 CC[C@@H](C)[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
90663313 106151 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 982 27 12 10 -0.3 C#CC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143273 106151 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 982 27 12 10 -0.3 C#CC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
127053969 152012 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 477 5 1 5 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NC2CCC2)CC1(F)F nan
CHEMBL3971706 152012 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 477 5 1 5 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NC2CCC2)CC1(F)F nan
117826532 149739 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 7 2 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC(O)CCl)CC1(F)F nan
CHEMBL3952681 149739 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 7 2 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC(O)CCl)CC1(F)F nan
127053968 150156 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 439 4 2 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NO)CC1(F)F nan
CHEMBL3956004 150156 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 439 4 2 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NO)CC1(F)F nan
127053977 153049 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 6 1 7 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cnccn2)CC1(F)F nan
CHEMBL3980605 153049 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 6 1 7 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cnccn2)CC1(F)F nan
127053944 151721 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 483 4 1 5 5.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3OC(F)(F)F)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
CHEMBL3969151 151721 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 483 4 1 5 5.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3OC(F)(F)F)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
57404484 72899 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 397 4 1 5 4.8 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccsc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012509 72899 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 397 4 1 5 4.8 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccsc2)cn1 10.1016/j.bmcl.2012.01.138
127053941 151281 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 467 4 0 4 6.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3OC(F)(F)F)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3965348 151281 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 467 4 0 4 6.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3OC(F)(F)F)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
127053970 159573 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2cccnc2)CC1(F)F nan
CHEMBL4108966 159573 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2cccnc2)CC1(F)F nan
127053989 150698 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 486 3 0 4 5.6 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(Br)CC1(F)F nan
CHEMBL3960140 150698 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 486 3 0 4 5.6 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(Br)CC1(F)F nan
127050971 140284 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 416 7 2 5 1.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCC2CC2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3819204 140284 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 416 7 2 5 1.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCC2CC2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
90663292 106142 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 857 22 9 9 1.4 COc1ccc(/C=C/C(=O)N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
CHEMBL3143251 106142 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 857 22 9 9 1.4 COc1ccc(/C=C/C(=O)N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
71735886 143545 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 479 4 2 6 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(C2(O)CNC2)CC1(F)F nan
CHEMBL3903446 143545 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 479 4 2 6 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(C2(O)CNC2)CC1(F)F nan
44403839 71050 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@H]3CCCC[C@@H]3C[C@@H]3C(=O)O[C@@H](C)[C@@H]32)n1 10.1021/jm0502236
CHEMBL195909 71050 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@H]3CCCC[C@@H]3C[C@@H]3C(=O)O[C@@H](C)[C@@H]32)n1 10.1021/jm0502236
11645276 71407 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 311 2 0 3 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccccn3)[C@H]12 10.1021/jm0502236
CHEMBL196683 71407 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 311 2 0 3 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccccn3)[C@H]12 10.1021/jm0502236
44280649 112147 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 743 19 8 9 1.3 COc1ccc(/C=C/C(=O)Nc2n[nH]c(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n2)cc1 10.1016/s0960-894x(99)00197-3
CHEMBL33033 112147 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 743 19 8 9 1.3 COc1ccc(/C=C/C(=O)Nc2n[nH]c(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n2)cc1 10.1016/s0960-894x(99)00197-3
44281172 99200 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 589 15 9 9 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1cccs1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284474 99200 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 589 15 9 9 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1cccs1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280955 118774 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 611 15 8 6 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc2[nH]cnc2c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34387 118774 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 611 15 8 6 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc2[nH]cnc2c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
10459564 514 34 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
4048 514 34 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
CHEMBL2103856 514 34 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
DB12046 514 34 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
90663298 106146 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143257 106146 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
16100342 82822 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3[C@@H](O)CCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218726 82822 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3[C@@H](O)CCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
72547552 103393 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3091994 103393 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
72547552 103393 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3091994 103393 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
44290166 169176 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 808 21 9 10 1.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL44387 169176 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 808 21 9 10 1.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
58046052 132764 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 457 9 1 8 3.9 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCF)cc(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704477 132764 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 457 9 1 8 3.9 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCF)cc(C(C)(C)C)c3)nc2c(C)c1C nan
90663563 106205 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 829 22 9 8 2.0 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143684 106205 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 829 22 9 8 2.0 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143288 209406 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@H](Cc1cccs1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44280585 116465 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 727 18 8 8 1.7 C/C(=C\c1ccccc1)C(=O)Nc1n[nH]c(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)n1 10.1016/s0960-894x(99)00197-3
CHEMBL33873 116465 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 727 18 8 8 1.7 C/C(=C\c1ccccc1)C(=O)Nc1n[nH]c(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)n1 10.1016/s0960-894x(99)00197-3
44416466 140972 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 441 3 0 2 7.3 C[C@H]1OC[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL384562 140972 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 441 3 0 2 7.3 C[C@H]1OC[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL3143266 209394 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(C)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
72547555 103381 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 365 4 0 2 6.1 COC1(C)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091982 103381 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 365 4 0 2 6.1 COC1(C)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44432693 145156 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 385 3 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL391624 145156 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 385 3 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44309776 102642 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 754 16 6 7 5.3 NCCCNC(=O)[C@H](CCN)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL307831 102642 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 754 16 6 7 5.3 NCCCNC(=O)[C@H](CCN)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
90663337 106165 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 869 20 9 10 1.1 CC(=O)N(C(=O)c1cc2ccccc2oc1=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143301 106165 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 869 20 9 10 1.1 CC(=O)N(C(=O)c1cc2ccccc2oc1=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663294 106144 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 827 22 8 9 2.1 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143253 106144 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 827 22 8 9 2.1 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
9804049 133027 2 None - 1 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371069 133027 2 None - 1 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
11691128 140806 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 459 5 0 5 5.9 CCOC(=O)c1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
CHEMBL383606 140806 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 459 5 0 5 5.9 CCOC(=O)c1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
3525 3355 8 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10.1016/s0960-894x(03)00325-1
9853822 3355 8 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10.1016/s0960-894x(03)00325-1
CHEMBL311626 3355 8 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10.1016/s0960-894x(03)00325-1
44432756 86302 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 396 3 0 5 3.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCOCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231971 86302 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 396 3 0 5 3.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCOCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44306761 168332 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL438551 168332 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
9810477 98308 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 719 18 9 9 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccs2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL278216 98308 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 719 18 9 9 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccs2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280899 114274 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33394 114274 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
11284457 153976 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3939315 153976 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990814 153976 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
70693686 72886 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 389 4 0 3 5.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012495 72886 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 389 4 0 3 5.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C)c2)cn1 10.1016/j.bmcl.2012.01.138
44305939 201691 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 317 3 2 5 3.4 CCc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL65425 201691 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 317 3 2 5 3.4 CCc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
70695800 72897 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccc(OC)cc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012507 72897 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccc(OC)cc2)cn1 10.1016/j.bmcl.2012.01.138
90663291 106141 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 877 21 9 8 2.7 CC(=O)N(C(=O)c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143250 106141 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 877 21 9 8 2.7 CC(=O)N(C(=O)c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
11503433 135011 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4C(F)(F)F)cn3)[C@H]12 10.1021/jm0502236
CHEMBL372886 135011 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4C(F)(F)F)cn3)[C@H]12 10.1021/jm0502236
44432772 86502 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 437 3 0 3 5.8 O=C1OC[C@H]2[C@@H]1Cc1c(F)cc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232333 86502 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 437 3 0 3 5.8 O=C1OC[C@H]2[C@@H]1Cc1c(F)cc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
44280878 99587 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 501 13 8 8 -2.7 C[C@H](NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287156 99587 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 501 13 8 8 -2.7 C[C@H](NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
11682882 72171 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(F)cc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL199101 72171 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(F)cc4)cn3)[C@H]12 10.1021/jm0502236
44432715 86254 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 394 3 0 5 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4nccs4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231728 86254 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 394 3 0 5 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4nccs4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL3143260 209391 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44338791 9221 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111106 9221 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
76335370 103370 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3091971 103370 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3143318 209420 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44309730 202249 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 819 16 5 7 6.8 COc1ccc(CNC(=O)[C@H](CCN)NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)cc1 10.1016/s0960-894x(03)00325-1
CHEMBL69359 202249 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 819 16 5 7 6.8 COc1ccc(CNC(=O)[C@H](CCN)NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)cc1 10.1016/s0960-894x(03)00325-1
53245434 75520 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 374 5 2 2 4.7 CCCC(=O)Nc1cccc(NC(=O)c2cc(C)ccc2Br)c1 10.1021/ml2002696
CHEMBL2049112 75520 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 374 5 2 2 4.7 CCCC(=O)Nc1cccc(NC(=O)c2cc(C)ccc2Br)c1 10.1021/ml2002696
16100353 82625 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC[C@@H](O)C[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218168 82625 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC[C@@H](O)C[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
68058674 126737 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 420 6 1 3 4.2 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)C3(CC)COC3)C2)cc1 nan
CHEMBL3658403 126737 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 420 6 1 3 4.2 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)C3(CC)COC3)C2)cc1 nan
58046031 132768 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 10 2 10 3.1 CC(C)Oc1cc(OC(C)C)c2nn(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704481 132768 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 10 2 10 3.1 CC(C)Oc1cc(OC(C)C)c2nn(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)c(=N)n2n1 nan
70685282 72898 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 392 4 1 5 4.1 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccnc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012508 72898 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 392 4 1 5 4.1 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccnc2)cn1 10.1016/j.bmcl.2012.01.138
44305953 101616 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 375 6 3 6 3.7 CC(C)c1ccc(Cn2ccc3c4c(N)nc(NCCO)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL302226 101616 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 375 6 3 6 3.7 CC(C)c1ccc(Cn2ccc3c4c(N)nc(NCCO)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
127053939 153655 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 401 3 0 3 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3985900 153655 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 401 3 0 3 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
127053949 142215 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 447 4 0 5 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CC#N)CC1(F)F nan
CHEMBL3892564 142215 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 447 4 0 5 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CC#N)CC1(F)F nan
127053998 159317 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 0 5 4.8 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(N(C)C)CC1(F)F nan
CHEMBL4106780 159317 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 0 5 4.8 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(N(C)C)CC1(F)F nan
72547308 103390 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091991 103390 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
127053979 151715 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 6 1 7 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cncnc2)CC1(F)F nan
CHEMBL3969105 151715 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 6 1 7 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cncnc2)CC1(F)F nan
127053996 151992 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 423 3 2 4 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)NC(=O)[C@]2(O)CC1(F)F nan
CHEMBL3971586 151992 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 423 3 2 4 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)NC(=O)[C@]2(O)CC1(F)F nan
127050658 140226 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 458 7 2 5 2.3 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCCC(F)(F)F)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3818421 140226 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 458 7 2 5 2.3 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCCC(F)(F)F)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
11684648 140290 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 492 5 2 5 3.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3819237 140290 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 492 5 2 5 3.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
44409074 75063 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 443 3 0 4 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5ccsc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL204157 75063 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 443 3 0 4 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5ccsc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44409248 76780 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 4 0 5 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1OC 10.1016/j.bmcl.2005.12.042
CHEMBL207791 76780 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 4 0 5 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1OC 10.1016/j.bmcl.2005.12.042
72547554 103388 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091989 103388 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44309472 202543 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 804 16 5 7 6.2 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCc1ccccn1 10.1016/s0960-894x(03)00325-1
CHEMBL71140 202543 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 804 16 5 7 6.2 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCc1ccccn1 10.1016/s0960-894x(03)00325-1
90663299 106147 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 812 20 10 7 1.9 CC(=O)N(c1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143258 106147 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 812 20 10 7 1.9 CC(=O)N(c1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44409029 76122 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 504 5 0 6 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)N5CCOCC5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL205987 76122 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 504 5 0 6 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)N5CCOCC5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44409062 168414 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 538 6 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OC(C)(C)C(=O)Nc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL439157 168414 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 538 6 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OC(C)(C)C(=O)Nc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44306599 201949 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL67308 201949 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44416724 80125 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 379 3 1 3 4.7 C[C@H]1O[C@H](Cc2ccc3ccccc3n2)C2[C@H]1[C@H](C(=O)O)C[C@@H]1CCCC[C@@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL214862 80125 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 379 3 1 3 4.7 C[C@H]1O[C@H](Cc2ccc3ccccc3n2)C2[C@H]1[C@H](C(=O)O)C[C@@H]1CCCC[C@@H]21 10.1016/j.bmcl.2006.06.042
9831828 165836 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 733 19 7 8 2.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
CHEMBL42769 165836 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 733 19 7 8 2.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
44290181 172713 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 806 22 8 9 2.1 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL45259 172713 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 806 22 8 9 2.1 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
44281263 99367 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 603 16 7 5 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285685 99367 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 603 16 7 5 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
70687425 72889 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cc(Cl)ccc2Cl)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012498 72889 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cc(Cl)ccc2Cl)cn1 10.1016/j.bmcl.2012.01.138
10000177 201695 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometryAntagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometry
ChEMBL 385 5 1 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C5CC5)nc4ccc32)cc1 10.1039/c4md00485j
CHEMBL65476 201695 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometryAntagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometry
ChEMBL 385 5 1 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C5CC5)nc4ccc32)cc1 10.1039/c4md00485j
10000177 201695 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 385 5 1 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C5CC5)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL65476 201695 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 385 5 1 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C5CC5)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
44338929 5753 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107919 5753 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
49766539 59259 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 386 4 2 2 4.8 O=C(Nc1cccc(NC(=O)C2CCCC2)c1)c1ccccc1Br 10.1021/ml2002696
CHEMBL1718628 59259 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 386 4 2 2 4.8 O=C(Nc1cccc(NC(=O)C2CCCC2)c1)c1ccccc1Br 10.1021/ml2002696
50910534 75430 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 6 2 2 4.2 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2CC)c1 10.1021/ml2002696
CHEMBL2048423 75430 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 6 2 2 4.2 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2CC)c1 10.1021/ml2002696
44305897 102352 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 359 5 2 5 4.8 CCNc1nc(N)c2c(ccc3c2ccn3Cc2ccc(C(C)C)cc2)n1 10.1016/s0960-894x(99)00339-x
CHEMBL305557 102352 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 359 5 2 5 4.8 CCNc1nc(N)c2c(ccc3c2ccn3Cc2ccc(C(C)C)cc2)n1 10.1016/s0960-894x(99)00339-x
16100351 82365 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 491 3 0 3 7.0 C[C@H]1OC(=O)[C@@H]2C[C@H]3[C@@H](CCCC3(F)F)[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218000 82365 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 491 3 0 3 7.0 C[C@H]1OC(=O)[C@@H]2C[C@H]3[C@@H](CCCC3(F)F)[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
76328106 103378 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 378 4 1 2 5.2 CC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091979 103378 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 378 4 1 2 5.2 CC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
66761604 126997 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 474 3 2 3 2.8 O=C1CN(C(=O)N2CC(NC(=O)c3ccccc3)CC(c3ccc(C(F)(F)F)cc3)C2)CCN1 nan
CHEMBL3662511 126997 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 474 3 2 3 2.8 O=C1CN(C(=O)N2CC(NC(=O)c3ccccc3)CC(c3ccc(C(F)(F)F)cc3)C2)CCN1 nan
44306501 102205 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304683 102205 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44290276 164336 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 748 19 8 9 1.7 Cc1oc([C@H](Cc2ccc(F)cc2)NC(=O)C(N)CN)nc1C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc1ccccc1 10.1016/s0960-894x(98)00292-3
CHEMBL42224 164336 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 748 19 8 9 1.7 Cc1oc([C@H](Cc2ccc(F)cc2)NC(=O)C(N)CN)nc1C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc1ccccc1 10.1016/s0960-894x(98)00292-3
44290058 178409 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 705 18 7 8 2.1 NCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
CHEMBL47090 178409 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 705 18 7 8 2.1 NCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
9937578 99482 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 555 15 7 8 0.3 NCCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286430 99482 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 555 15 7 8 0.3 NCCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
23631278 92508 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 498 3 0 4 5.5 CC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
CHEMBL244108 92508 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 498 3 0 4 5.5 CC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
11639231 71977 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 367 4 0 3 5.3 CC(C)Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL198451 71977 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 367 4 0 3 5.3 CC(C)Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL33473 209644 18 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1016/s0960-894x(99)00197-3
44281237 116216 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 604 16 7 6 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33742 116216 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 604 16 7 6 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL4764659 212275 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Affinity Biochemical interaction (Binding assay (platelet membranes)) EUB0000291b F2RAffinity Biochemical interaction (Binding assay (platelet membranes)) EUB0000291b F2R
ChEMBL None None None O=C(N1CCS(=O)(=O)CC1)N1C[C@@](S)(c2ccc(OC(F)(F)F)cc2)C[C@@](S)(c2nc(C3CC3)no2)C1 nan
10971 3489 24 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometryAntagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometry
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1039/c4md00485j
4259181 3489 24 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometryAntagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometry
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1039/c4md00485j
CHEMBL63426 3489 24 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometryAntagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometry
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1039/c4md00485j
10971 3489 24 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1016/s0960-894x(99)00339-x
4259181 3489 24 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1016/s0960-894x(99)00339-x
CHEMBL63426 3489 24 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1016/s0960-894x(99)00339-x
90663354 106173 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccccc1F)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143319 106173 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccccc1F)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306612 101677 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL302603 101677 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
9831948 178340 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 749 20 7 8 2.9 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL47023 178340 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 749 20 7 8 2.9 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
44281264 114757 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 616 15 8 5 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33487 114757 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 616 15 8 5 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
11284457 153976 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3939315 153976 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990814 153976 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
44290231 99797 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 792 21 8 9 1.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL288976 99797 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 792 21 8 9 1.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
44432833 86243 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)O[C@H](C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL231695 86243 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)O[C@H](C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
72547553 103374 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 415 5 0 4 5.1 CS(=O)(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091975 103374 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 415 5 0 4 5.1 CS(=O)(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
121335735 152013 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 5 5.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)CC(C)(C)C)CC1(F)F nan
CHEMBL3971708 152013 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 5 5.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)CC(C)(C)C)CC1(F)F nan
9951647 140033 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 377 2 1 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL381265 140033 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 377 2 1 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
127053984 160209 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 522 5 2 5 4.9 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@@]2(NC(=S)NC2CC2)CC1(F)F nan
CHEMBL4114149 160209 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 522 5 2 5 4.9 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@@]2(NC(=S)NC2CC2)CC1(F)F nan
72547553 103374 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 415 5 0 4 5.1 CS(=O)(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091975 103374 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 415 5 0 4 5.1 CS(=O)(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
57404504 72891 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 391 4 1 4 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012500 72891 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 391 4 1 4 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2)cn1 10.1016/j.bmcl.2012.01.138
127053964 148897 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 476 4 0 8 3.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(n2cnnn2)CC1(F)F nan
CHEMBL3945945 148897 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 476 4 0 8 3.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(n2cnnn2)CC1(F)F nan
127053967 159639 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 490 4 0 8 4.2 Cc1nnnn1[C@@]12CC(F)(F)C(C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)C1[C@@H](C)OC2=O nan
CHEMBL4109515 159639 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 490 4 0 8 4.2 Cc1nnnn1[C@@]12CC(F)(F)C(C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)C1[C@@H](C)OC2=O nan
127053973 159598 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 504 6 1 7 5.0 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2ncco2)CC1(F)F nan
CHEMBL4109166 159598 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 504 6 1 7 5.0 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2ncco2)CC1(F)F nan
CHEMBL3143275 209400 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm960455s
44310308 167313 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 759 15 5 7 5.5 CSC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN 10.1016/s0960-894x(03)00325-1
CHEMBL431164 167313 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 759 15 5 7 5.5 CSC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN 10.1016/s0960-894x(03)00325-1
127051545 140189 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 476 5 2 5 3.3 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(F)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3817930 140189 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 476 5 2 5 3.3 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(F)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
127050656 140297 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 490 7 2 6 3.1 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(OC(F)F)cc2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3819343 140297 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 490 7 2 6 3.1 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(OC(F)F)cc2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
44408851 75042 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL204009 75042 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
44408851 75042 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL204009 75042 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
10161572 5461 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107667 5461 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
23631809 92747 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 456 3 1 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CNCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244487 92747 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 456 3 1 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CNCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
23631900 142369 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 5 5.5 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4ccccc4C)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
CHEMBL389382 142369 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 5 5.5 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4ccccc4C)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
53245432 75522 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 378 5 2 2 4.6 CCCC(=O)Nc1cccc(NC(=O)c2cc(F)ccc2Br)c1 10.1021/ml2002696
CHEMBL2049114 75522 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 378 5 2 2 4.6 CCCC(=O)Nc1cccc(NC(=O)c2cc(F)ccc2Br)c1 10.1021/ml2002696
44281289 118044 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 599 15 10 9 -0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34156 118044 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 599 15 10 9 -0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44290110 100762 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 715 19 7 8 2.5 CNCC(=O)N[C@@H](Cc1ccccc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
CHEMBL296147 100762 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 715 19 7 8 2.5 CNCC(=O)N[C@@H](Cc1ccccc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
44187102 124608 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 404 8 1 7 2.7 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(Cl)cc(OC)c1 nan
CHEMBL3644437 124608 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 404 8 1 7 2.7 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(Cl)cc(OC)c1 nan
CHEMBL3143299 209410 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(N)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143321 209422 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(O)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44416691 80930 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 393 3 1 4 5.1 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)O[C@@H](O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL215924 80930 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 393 3 1 4 5.1 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)O[C@@H](O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
44408873 76342 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL206502 76342 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
44290059 100968 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 615 16 7 8 0.3 NCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)co1 10.1016/s0960-894x(98)00292-3
CHEMBL297640 100968 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 615 16 7 8 0.3 NCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)co1 10.1016/s0960-894x(98)00292-3
44416567 138098 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 377 3 0 3 5.7 COc1ccc2nc(/C=C/[C@@H]3[C@H]4[C@H](CO[C@@H]4C)C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL377594 138098 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 377 3 0 3 5.7 COc1ccc2nc(/C=C/[C@@H]3[C@H]4[C@H](CO[C@@H]4C)C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
66760951 127001 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 476 3 1 3 4.5 N#CC1CCN(C(=O)N2CC(NC(=O)C3CCCC3)CC(c3ccc(C(F)(F)F)cc3)C2)CC1 nan
CHEMBL3662515 127001 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 476 3 1 3 4.5 N#CC1CCN(C(=O)N2CC(NC(=O)C3CCCC3)CC(c3ccc(C(F)(F)F)cc3)C2)CC1 nan
44432795 86300 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL231957 86300 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL3143300 209411 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44183746 132744 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 469 11 1 9 3.8 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(OCCOC)cc(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704457 132744 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 469 11 1 9 3.8 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(OCCOC)cc(C(C)(C)C)c3)c(=N)n2n1 nan
70683207 72901 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 384 4 1 5 3.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(N2CCCC2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012511 72901 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 384 4 1 5 3.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(N2CCCC2)cn1 10.1016/j.bmcl.2012.01.138
44306336 201844 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL66585 201844 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
9875040 113912 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 713 18 9 8 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33318 113912 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 713 18 9 8 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44432763 86353 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 453 3 0 3 6.0 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232171 86353 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 453 3 0 3 6.0 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
2858875 206504 10 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 469 5 2 5 6.2 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(Cc3ccccc3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
CHEMBL98805 206504 10 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 469 5 2 5 6.2 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(Cc3ccccc3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
137661486 158917 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4101591 158917 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
10204371 205162 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 451 6 3 3 4.9 CN(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL90864 205162 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 451 6 3 3 4.9 CN(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
76313664 103383 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 351 4 0 2 5.7 COC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091984 103383 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 351 4 0 2 5.7 COC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
76335372 103384 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 4 0 3 5.7 CC(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091985 103384 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 4 0 3 5.7 CC(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
9810475 101055 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 719 19 7 8 2.5 NCCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
CHEMBL298273 101055 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 719 19 7 8 2.5 NCCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
44409259 140150 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 432 4 1 4 5.6 CCC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL381569 140150 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 432 4 1 4 5.6 CCC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
90663331 106160 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 773 20 9 7 1.4 CC(=O)N(c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143294 106160 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 773 20 9 7 1.4 CC(=O)N(c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306076 201331 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 335 3 2 6 3.5 CSc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL63381 201331 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 335 3 2 6 3.5 CSc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
44432803 144465 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 421 3 0 3 5.3 O=C1OC[C@H]2[C@@H]1Cc1c(ccc(F)c1F)[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL391098 144465 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 421 3 0 3 5.3 O=C1OC[C@H]2[C@@H]1Cc1c(ccc(F)c1F)[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
127053987 143265 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 501 5 1 6 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NS(C)(=O)=O)CC1(F)F nan
CHEMBL3901289 143265 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 501 5 1 6 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NS(C)(=O)=O)CC1(F)F nan
66761456 126748 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 500 4 1 4 4.5 N#CC1CCN(C(=O)N2CC(NC(=O)c3ccccc3)CC(c3ccc(OC(F)(F)F)cc3)C2)CC1 nan
CHEMBL3658413 126748 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 500 4 1 4 4.5 N#CC1CCN(C(=O)N2CC(NC(=O)c3ccccc3)CC(c3ccc(OC(F)(F)F)cc3)C2)CC1 nan
127053983 148219 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 5 2 5 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NC(=O)NC2CCC2)CC1(F)F nan
CHEMBL3940503 148219 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 5 2 5 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NC(=O)NC2CCC2)CC1(F)F nan
72547551 103380 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
CHEMBL3091981 103380 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
127053942 142884 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 423 3 1 5 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(N)CC1(F)F nan
CHEMBL3898141 142884 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 423 3 1 5 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(N)CC1(F)F nan
CHEMBL3143291 209409 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44432814 87574 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 3 5.0 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL234397 87574 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 3 5.0 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
127053961 151167 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 499 5 1 6 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nn[nH]n2)CC1(F)F nan
CHEMBL3964337 151167 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 499 5 1 6 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nn[nH]n2)CC1(F)F nan
10350886 178169 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 942 27 13 9 -0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1016/s0960-894x(98)00292-3
CHEMBL46869 178169 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 942 27 13 9 -0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1016/s0960-894x(98)00292-3
23628249 86803 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1cc(F)ccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232955 86803 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1cc(F)ccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL3143272 209399 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44309471 101675 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
CHEMBL302594 101675 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
44309959 168633 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 772 15 5 7 5.7 NCCNC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](Cc1ccccc1F)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL440808 168633 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 772 15 5 7 5.7 NCCNC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](Cc1ccccc1F)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
127051546 140292 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 490 7 2 6 3.1 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2cccc(OC(F)F)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3819277 140292 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 490 7 2 6 3.1 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2cccc(OC(F)F)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
44418846 82809 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3C[C@H](O)CC[C@H]32)nc1 10.1021/jm061043e
CHEMBL218670 82809 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3C[C@H](O)CC[C@H]32)nc1 10.1021/jm061043e
10246587 71747 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197791 71747 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44324193 105662 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 479 7 3 3 5.6 CC(C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL313645 105662 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 479 7 3 3 5.6 CC(C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
44408709 140834 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1cccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc12 10.1016/j.bmcl.2005.12.042
CHEMBL383832 140834 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1cccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc12 10.1016/j.bmcl.2005.12.042
44416634 80658 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 377 3 0 3 5.7 CO[C@@H]1O[C@H](C)[C@H]2[C@@H](/C=C/c3ccc4ccccc4n3)[C@@H]3CCCC[C@H]3C[C@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL215524 80658 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 377 3 0 3 5.7 CO[C@@H]1O[C@H](C)[C@H]2[C@@H](/C=C/c3ccc4ccccc4n3)[C@@H]3CCCC[C@H]3C[C@H]21 10.1016/j.bmcl.2006.06.042
44416487 165445 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 321 3 0 2 5.9 COc1ccc2nc(/C=C/[C@@H]3CCC[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL425437 165445 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 321 3 0 2 5.9 COc1ccc2nc(/C=C/[C@@H]3CCC[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
44280703 116283 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33781 116283 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280768 116659 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 569 14 9 8 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(99)00197-3
CHEMBL33940 116659 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 569 14 9 8 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(99)00197-3
50910535 75431 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 366 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2OC(F)(F)F)c1 10.1021/ml2002696
CHEMBL2048425 75431 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 366 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2OC(F)(F)F)c1 10.1021/ml2002696
44418839 82999 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm061043e
CHEMBL219698 82999 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm061043e
11674764 71920 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 353 3 0 3 5.2 CC(C)c1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL198273 71920 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 353 3 0 3 5.2 CC(C)c1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44408615 74065 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 379 2 0 3 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(F)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL202677 74065 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 379 2 0 3 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(F)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44306402 167634 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL433499 167634 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL33473 209644 18 None - 0 Human 4.1 pIC50 = 4.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1016/s0960-894x(98)00292-3
44328647 112287 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 525 5 2 5 7.5 CC(C)(C)c1ccc(Cn2c(=N)n(CC(=O)c3cc(C(C)(C)C)c(O)c(C(C)(C)C)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00555-8
CHEMBL330643 112287 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 525 5 2 5 7.5 CC(C)(C)c1ccc(Cn2c(=N)n(CC(=O)c3cc(C(C)(C)C)c(O)c(C(C)(C)C)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00555-8
44416740 141450 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 395 5 2 4 4.7 COc1ccc2nc(/C=C/[C@@H]3[C@H]([C@@H](C)O)[C@H](CO)C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL387441 141450 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 395 5 2 4 4.7 COc1ccc2nc(/C=C/[C@@H]3[C@H]([C@@H](C)O)[C@H](CO)C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL3143316 209418 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44280522 98731 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL281443 98731 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
23631277 142905 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 470 3 0 4 5.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL389834 142905 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 470 3 0 4 5.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
12018762 109133 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL322282 109133 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
17187522 59322 2 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 296 5 2 2 4.0 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2C)c1 10.1021/ml2002696
CHEMBL1721173 59322 2 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 296 5 2 2 4.0 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2C)c1 10.1021/ml2002696
90663305 106149 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 558 11 5 5 2.3 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(N)=O 10.1021/jm960455s
CHEMBL3143265 106149 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 558 11 5 5 2.3 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(N)=O 10.1021/jm960455s
76331783 103377 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 436 4 1 3 6.6 CC(C)(C)OC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091978 103377 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 436 4 1 3 6.6 CC(C)(C)OC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
66761321 126992 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 435 4 1 3 3.9 CC(C)c1cccc(C2CC(NC(=O)c3ccccc3)CN(C(=O)N3CCOCC3)C2)c1 nan
CHEMBL3662506 126992 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 435 4 1 3 3.9 CC(C)c1cccc(C2CC(NC(=O)c3ccccc3)CN(C(=O)N3CCOCC3)C2)c1 nan
23631188 92506 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3ccccc3F)cn2)C1 10.1021/jm070704k
CHEMBL244105 92506 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3ccccc3F)cn2)C1 10.1021/jm070704k
23631811 92669 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244299 92669 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm070704k
127053951 148997 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 480 4 1 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C2(O)COC2)CC1(F)F nan
CHEMBL3946656 148997 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 480 4 1 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C2(O)COC2)CC1(F)F nan
57404483 72895 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012505 72895 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2012.01.138
127053945 143962 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 417 3 1 4 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
CHEMBL3906979 143962 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 417 3 1 4 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
72547551 103380 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
CHEMBL3091981 103380 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
70683205 72900 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 381 4 1 5 4.3 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccoc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012510 72900 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 381 4 1 5 4.3 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccoc2)cn1 10.1016/j.bmcl.2012.01.138
70681077 72880 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 375 4 0 3 5.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012489 72880 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 375 4 0 3 5.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2)cn1 10.1016/j.bmcl.2012.01.138
127051547 140249 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 504 5 2 7 2.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc3c(c2)OC(F)(F)O3)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3818750 140249 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 504 5 2 7 2.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc3c(c2)OC(F)(F)O3)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
23630915 92744 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 489 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[S+]([O-])CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244483 92744 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 489 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[S+]([O-])CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
44418837 141038 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 437 3 0 3 6.3 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CC(F)(F)CC[C@H]43)nc2)c1 10.1021/jm061043e
CHEMBL384982 141038 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 437 3 0 3 6.3 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CC(F)(F)CC[C@H]43)nc2)c1 10.1021/jm061043e
44409289 74281 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 425 3 0 4 5.9 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1Cl 10.1016/j.bmcl.2005.12.042
CHEMBL203012 74281 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 425 3 0 4 5.9 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1Cl 10.1016/j.bmcl.2005.12.042
44409050 140536 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 462 5 1 5 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OC(C)(C)C(N)=O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL382581 140536 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 462 5 1 5 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OC(C)(C)C(N)=O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44306337 96376 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL265227 96376 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
44416672 165890 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 347 2 0 2 5.7 C[C@H]1OC[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL427783 165890 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 347 2 0 2 5.7 C[C@H]1OC[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@@H]21 10.1016/j.bmcl.2006.06.042
44289954 100888 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 721 18 7 8 2.3 NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csc([C@@H](N)Cc2ccc(F)cc2)n1 10.1016/s0960-894x(98)00292-3
CHEMBL297091 100888 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 721 18 7 8 2.3 NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csc([C@@H](N)Cc2ccc(F)cc2)n1 10.1016/s0960-894x(98)00292-3
10077130 3932 49 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4047 3932 49 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4870 3932 49 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
CHEMBL493982 3932 49 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
DB09030 3932 49 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
46931416 127000 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 467 3 2 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)C1CCCC1 nan
CHEMBL3662514 127000 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 467 3 2 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)C1CCCC1 nan
9919038 166164 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL428311 166164 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44290234 177930 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 832 22 8 10 2.4 COc1ccc(C[C@H](NC(=O)C(N)C(C)C)c2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)cs2)cc1 10.1016/s0960-894x(98)00292-3
CHEMBL46670 177930 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 832 22 8 10 2.4 COc1ccc(C[C@H](NC(=O)C(N)C(C)C)c2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)cs2)cc1 10.1016/s0960-894x(98)00292-3
58045917 132752 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 496 8 1 10 3.0 CCOc1nn2c(=N)n(CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)nc2cc1CC nan
CHEMBL3704465 132752 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 496 8 1 10 3.0 CCOc1nn2c(=N)n(CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)nc2cc1CC nan
44418840 83000 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(F)cc4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL219699 83000 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(F)cc4)cn3)[C@H]12 10.1021/jm061043e
11249717 153890 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3903962 153890 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990074 153890 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
58137009 124615 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 486 11 2 9 2.5 CCOc1nn2c(N)n[n+](CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c2cc1CC nan
CHEMBL3644444 124615 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 486 11 2 9 2.5 CCOc1nn2c(N)n[n+](CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c2cc1CC nan
16100343 137616 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC[C@H](O)C[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL376890 137616 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC[C@H](O)C[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
44187647 124611 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 470 11 1 8 3.4 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OCCOC)cc(C(C)(C)C)c1 nan
CHEMBL3644440 124611 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 470 11 1 8 3.4 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OCCOC)cc(C(C)(C)C)c1 nan
10246587 71747 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
CHEMBL197791 71747 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
10246587 71747 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197791 71747 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44432806 86843 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1cccc(F)c1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL233163 86843 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1cccc(F)c1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
11508687 71536 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 355 4 0 4 4.2 COCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197133 71536 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 355 4 0 4 4.2 COCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44826172 99513 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc([N+](=O)[O-])c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286648 99513 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc([N+](=O)[O-])c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280822 116032 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 594 15 8 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1nccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33629 116032 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 594 15 8 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1nccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL3143255 209389 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm960455s
44305896 102311 3 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 345 4 2 5 4.4 CNc1nc(N)c2c(ccc3c2ccn3Cc2ccc(C(C)C)cc2)n1 10.1016/s0960-894x(99)00339-x
CHEMBL305329 102311 3 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 345 4 2 5 4.4 CNc1nc(N)c2c(ccc3c2ccn3Cc2ccc(C(C)C)cc2)n1 10.1016/s0960-894x(99)00339-x
127053991 143127 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 466 4 2 7 3.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3-c3nnn[nH]3)cn2)C2[C@@H](C)OC(=O)[C@]2(N)CC1(F)F nan
CHEMBL3900057 143127 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 466 4 2 7 3.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3-c3nnn[nH]3)cn2)C2[C@@H](C)OC(=O)[C@]2(N)CC1(F)F nan
44432721 86341 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 389 3 0 5 4.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cnccn4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL232140 86341 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 389 3 0 5 4.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cnccn4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44339029 109191 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 447 8 0 6 5.7 Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL322763 109191 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 447 8 0 6 5.7 Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
72547308 103390 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091991 103390 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3143305 209412 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NS(=O)(=O)c1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663318 106156 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 986 28 12 10 0.5 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143280 106156 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 986 28 12 10 0.5 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
127053966 160375 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 580 6 1 8 6.2 CNc1ccc(-c2cn([C@@]34CC(F)(F)C(C)[C@H](/C=C/c5ccc(-c6ccccc6C#N)cn5)C3[C@@H](C)OC4=O)nn2)cc1 nan
CHEMBL4115431 160375 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 580 6 1 8 6.2 CNc1ccc(-c2cn([C@@]34CC(F)(F)C(C)[C@H](/C=C/c5ccc(-c6ccccc6C#N)cn5)C3[C@@H](C)OC4=O)nn2)cc1 nan
44310191 202829 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 770 17 6 7 5.2 CCNCCNC(=O)[C@H](CCN)NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL72854 202829 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 770 17 6 7 5.2 CCNCCNC(=O)[C@H](CCN)NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
44432836 87597 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@H]3c4ccccc4C[C@@H]4C(=O)O[C@H](C)[C@@H]43)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL234483 87597 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@H]3c4ccccc4C[C@@H]4C(=O)O[C@H](C)[C@@H]43)ccc2c1 10.1016/j.bmcl.2007.04.061
11516923 71575 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 4 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(Cc4ccccc4)n3)[C@H]12 10.1021/jm0502236
CHEMBL197248 71575 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 4 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(Cc4ccccc4)n3)[C@H]12 10.1021/jm0502236
1047175 206324 12 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 393 3 2 5 4.6 Cn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
CHEMBL97706 206324 12 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 393 3 2 5 4.6 Cn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
44281173 114761 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 544 16 7 6 -0.5 NCCC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33489 114761 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 544 16 7 6 -0.5 NCCC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44432839 144765 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@H]3c4ccccc4C[C@@H]4C(=O)O[C@@H](C)[C@@H]43)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL391323 144765 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@H]3c4ccccc4C[C@@H]4C(=O)O[C@@H](C)[C@@H]43)ccc2c1 10.1016/j.bmcl.2007.04.061
44306732 102118 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304128 102118 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL3143289 209407 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44280685 99277 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 585 15 7 8 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csnn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285018 99277 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 585 15 7 8 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csnn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44290251 100725 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 792 21 8 9 1.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL295849 100725 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 792 21 8 9 1.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
90663329 106158 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 774 20 9 8 0.8 CC(=O)N(c1cccnc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143292 106158 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 774 20 9 8 0.8 CC(=O)N(c1cccnc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
58045928 132746 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 439 8 1 8 4.1 CCC(CC)Oc1nn2c(=N)n(CC(=O)c3cc(OC)cc(C(C)(C)C)c3)nc2cc1C nan
CHEMBL3704459 132746 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 439 8 1 8 4.1 CCC(CC)Oc1nn2c(=N)n(CC(=O)c3cc(OC)cc(C(C)(C)C)c3)nc2cc1C nan
44305955 100545 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 315 3 2 5 3.4 C=Cc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL294544 100545 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 315 3 2 5 3.4 C=Cc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
4314709 205926 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 477 9 2 5 7.1 CCCCCCCn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
CHEMBL95359 205926 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 477 9 2 5 7.1 CCCCCCCn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
72547307 103379 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
CHEMBL3091980 103379 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
44418848 82767 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 6.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cc(Cl)ccc4Cl)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218449 82767 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 6.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cc(Cl)ccc4Cl)cn3)[C@H]12 10.1021/jm061043e
17187609 59546 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 300 5 2 2 3.8 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2F)c1 10.1021/ml2002696
CHEMBL1729550 59546 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 300 5 2 2 3.8 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2F)c1 10.1021/ml2002696
58046023 132750 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 499 11 2 10 3.4 CCC(CC)Oc1cc(C)c2nn(CC(=O)c3cc(OCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704463 132750 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 499 11 2 10 3.4 CCC(CC)Oc1cc(C)c2nn(CC(=O)c3cc(OCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
1047179 205972 5 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 492 6 2 7 4.4 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(CCN3CCOCC3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
CHEMBL95632 205972 5 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 492 6 2 7 4.4 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(CCN3CCOCC3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
68058705 126738 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 433 5 1 4 4.9 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)c3scnc3C)C2)cc1 nan
CHEMBL3658404 126738 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 433 5 1 4 4.9 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)c3scnc3C)C2)cc1 nan
76335371 103376 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 394 4 1 3 5.5 COC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091977 103376 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 394 4 1 3 5.5 COC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL4115732 211149 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL None None None None nan
90663307 106150 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1ccc(Cl)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143267 106150 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1ccc(Cl)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
12018759 110698 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL326456 110698 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
44264856 96594 0 None - 1 Human 10.4 pKd = 10.4 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 846 17 7 7 6.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccncc1 10.1021/jm000506s
CHEMBL267059 96594 0 None - 1 Human 10.4 pKd = 10.4 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 846 17 7 7 6.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccncc1 10.1021/jm000506s
9832212 203231 4 None - 1 Human 9.8 pKd = 9.8 Binding
Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
CHEMBL4226137 203231 4 None - 1 Human 9.8 pKd = 9.8 Binding
Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
CHEMBL7642 203231 4 None - 1 Human 9.8 pKd = 9.8 Binding
Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
10509332 98019 0 None - 1 Human 9.2 pKd = 9.2 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 759 17 7 6 5.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
CHEMBL275946 98019 0 None - 1 Human 9.2 pKd = 9.2 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 759 17 7 6 5.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
9919038 166164 0 None - 1 Human 9.1 pKd = 9.1 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
CHEMBL428311 166164 0 None - 1 Human 9.1 pKd = 9.1 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
10819322 203195 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
CHEMBL7610 203195 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
10747940 203211 0 None - 1 Human 8.0 pKd = 8.0 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 803 19 7 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CNC4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
CHEMBL7627 203211 0 None - 1 Human 8.0 pKd = 8.0 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 803 19 7 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CNC4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
9853816 96875 0 None - 1 Human 8.7 pKd = 8.7 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
CHEMBL269345 96875 0 None - 1 Human 8.7 pKd = 8.7 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
10724264 96730 0 None - 1 Human 8.6 pKd = 8.6 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 855 19 6 8 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
CHEMBL268328 96730 0 None - 1 Human 8.6 pKd = 8.6 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 855 19 6 8 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
24879036 168862 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 499 5 1 6 5.4 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1021/jm800180e
CHEMBL442649 168862 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 499 5 1 6 5.4 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1021/jm800180e
24878928 171877 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 548 5 1 5 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm800180e
CHEMBL447996 171877 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 548 5 1 5 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm800180e
9890926 82861 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218933 82861 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
24878927 186865 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 498 5 1 5 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
CHEMBL493975 186865 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 498 5 1 5 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
24878984 187139 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2F)cn1 10.1021/jm800180e
CHEMBL495422 187139 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2F)cn1 10.1021/jm800180e
24879079 188311 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 5 1 5 5.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C)c2F)cn1 10.1021/jm800180e
CHEMBL507697 188311 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 5 1 5 5.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C)c2F)cn1 10.1021/jm800180e
24879037 191995 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 508 5 1 5 6.1 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1021/jm800180e
CHEMBL521531 191995 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 508 5 1 5 6.1 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1021/jm800180e
76310288 104317 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 476 5 1 4 5.3 CC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109583 104317 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 476 5 1 4 5.3 CC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
52947767 18104 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 504 6 1 6 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270636 18104 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 504 6 1 6 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2010.09.009
10246587 71747 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against Protease-activated receptor 1Inhibitory constant against Protease-activated receptor 1
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197791 71747 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against Protease-activated receptor 1Inhibitory constant against Protease-activated receptor 1
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
76317514 104318 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 490 6 1 4 5.7 CCC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109584 104318 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 490 6 1 4 5.7 CCC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
76335713 104324 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 505 6 2 4 5.5 CCNC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109590 104324 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 505 6 2 4 5.5 CCNC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
24878827 172053 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 542 5 1 5 6.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/jm800180e
CHEMBL449425 172053 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 542 5 1 5 6.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/jm800180e
76324857 104321 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 545 6 2 5 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNC(=O)C4CCNCC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109587 104321 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 545 6 2 5 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNC(=O)C4CCNCC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
58939091 104316 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 506 6 1 5 5.9 CCOC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109582 104316 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 506 6 1 5 5.9 CCOC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
76328415 104323 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 526 7 1 5 5.1 CCS(=O)(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109589 104323 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 526 7 1 5 5.1 CCS(=O)(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
76335711 104308 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 575 5 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)Nc4ccncc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109574 104308 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 575 5 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)Nc4ccncc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
44264660 203374 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 519 8 2 5 4.4 CNc1ccc(C#CC[C@H](NS(=O)(=O)c2ccc3cc(OC)ccc3c2)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
CHEMBL7758 203374 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 519 8 2 5 4.4 CNc1ccc(C#CC[C@H](NS(=O)(=O)c2ccc3cc(OC)ccc3c2)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
52940892 18169 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 489 5 1 6 5.2 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccc(C)cn2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1271149 18169 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 489 5 1 6 5.2 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccc(C)cn2)cn1 10.1016/j.bmcl.2010.09.009
76332097 104322 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 512 6 1 5 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109588 104322 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 512 6 1 5 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
52949514 18092 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 499 5 1 6 5.4 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2C#N)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270537 18092 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 499 5 1 6 5.4 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2C#N)cn1 10.1016/j.bmcl.2010.09.009
90644637 111470 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288436 111470 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
24830436 187022 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 6 1 5 6.0 CCCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL494816 187022 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 6 1 5 6.0 CCCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
76335712 104310 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 568 4 1 5 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)N4CC[C@@H](O)C4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109576 104310 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 568 4 1 5 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)N4CC[C@@H](O)C4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
16214871 18119 3 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270738 18119 3 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cn1 10.1016/j.bmcl.2010.09.009
59016155 104312 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 508 5 2 6 4.7 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@]1(O)C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109578 104312 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 508 5 2 6 4.7 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@]1(O)C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
10345602 203169 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 493 7 2 4 4.1 CNc1ccc(C#CC[C@H](NS(=O)(=O)c2ccc3c(c2)CCCC3)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
CHEMBL7587 203169 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 493 7 2 4 4.1 CNc1ccc(C#CC[C@H](NS(=O)(=O)c2ccc3c(c2)CCCC3)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
9804049 133027 2 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against Protease-activated receptor 1Inhibitory constant against Protease-activated receptor 1
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371069 133027 2 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against Protease-activated receptor 1Inhibitory constant against Protease-activated receptor 1
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
59016136 104314 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 434 4 1 4 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CN)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109580 104314 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 434 4 1 4 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CN)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
24878828 187590 3 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 420 3 1 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](N)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
CHEMBL498785 187590 3 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 420 3 1 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](N)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
90644636 111469 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288435 111469 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
90644643 111479 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 459 3 1 6 4.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccn5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288444 111479 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 459 3 1 6 4.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccn5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
76310287 104309 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 575 5 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)Nc4cccnc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109575 104309 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 575 5 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)Nc4cccnc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
76310289 104320 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 531 6 2 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNC(=O)[C@@H]4CCCN4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109586 104320 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 531 6 2 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNC(=O)[C@@H]4CCCN4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
52942074 18134 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccnc2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270840 18134 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccnc2)cn1 10.1016/j.bmcl.2010.09.009
76310290 104325 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 512 4 1 4 5.8 CNC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
CHEMBL3109591 104325 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 512 4 1 4 5.8 CNC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
90644642 111478 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5F)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288443 111478 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5F)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
52946929 18148 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccncc2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270942 18148 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccncc2)cn1 10.1016/j.bmcl.2010.09.009
90644639 111473 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288439 111473 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
90644638 111472 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C#N)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288438 111472 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C#N)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
90644640 111475 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288440 111475 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
127053945 143962 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 417 3 1 4 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
CHEMBL3906979 143962 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 417 3 1 4 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
127053948 146294 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 488 6 2 5 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NCCO)CC1(F)F nan
CHEMBL3925032 146294 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 488 6 2 5 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NCCO)CC1(F)F nan
127053939 153655 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 401 3 0 3 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3985900 153655 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 401 3 0 3 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
24878982 172992 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 556 5 0 5 6.9 CCOC(=O)N(C)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm800180e
CHEMBL453277 172992 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 556 5 0 5 6.9 CCOC(=O)N(C)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm800180e
24878829 171870 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 512 4 1 4 5.9 CC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/jm800180e
CHEMBL447913 171870 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 512 4 1 4 5.9 CC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/jm800180e
76317512 104306 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 540 5 1 4 6.5 CC(C)NC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
CHEMBL3109572 104306 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 540 5 1 4 6.5 CC(C)NC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
90644644 111480 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)CNC(=O)O4 10.1021/ml500008w
CHEMBL3288445 111480 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)CNC(=O)O4 10.1021/ml500008w
76332096 104319 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 505 6 2 5 4.6 C[C@H](N)C(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109585 104319 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 505 6 2 5 4.6 C[C@H](N)C(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
52940897 18181 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 476 5 1 7 4.3 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cncnc2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1271252 18181 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 476 5 1 7 4.3 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cncnc2)cn1 10.1016/j.bmcl.2010.09.009
58187662 104305 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 526 5 1 4 6.1 CCNC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
CHEMBL3109571 104305 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 526 5 1 4 6.1 CCNC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
24879035 176197 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 517 6 2 6 4.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(N)=O)c2)cn1 10.1021/jm800180e
CHEMBL460583 176197 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 517 6 2 6 4.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(N)=O)c2)cn1 10.1021/jm800180e
76317513 104311 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 568 4 1 5 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)N4CC[C@H](O)C4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109577 104311 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 568 4 1 5 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)N4CC[C@H](O)C4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
90644645 111481 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)CNC(=O)O4 10.1021/ml500008w
CHEMBL3288446 111481 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)CNC(=O)O4 10.1021/ml500008w
24878930 187717 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 5 0 5 6.0 CCOC(=O)N(C)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm800180e
CHEMBL500551 187717 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 5 0 5 6.0 CCOC(=O)N(C)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm800180e
44428104 143878 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
CHEMBL390630 143878 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
24878874 186806 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 477 4 2 4 4.8 CNC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL493633 186806 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 477 4 2 4 4.8 CNC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
24878875 192651 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 491 5 2 4 5.2 CCNC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL523854 192651 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 491 5 2 4 5.2 CCNC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
52942093 18158 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 489 5 1 6 5.2 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cc(C)ccn2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1271045 18158 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 489 5 1 6 5.2 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cc(C)ccn2)cn1 10.1016/j.bmcl.2010.09.009
90644641 111477 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C#N)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288442 111477 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C#N)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
24878929 173723 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 527 4 1 6 6.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NC(=O)OC(C)(C)C)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@H]12 10.1021/jm800180e
CHEMBL455020 173723 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 527 4 1 6 6.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NC(=O)OC(C)(C)C)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@H]12 10.1021/jm800180e
52946957 18190 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 505 6 1 7 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccc(OC)cn2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1271353 18190 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 505 6 1 7 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccc(OC)cn2)cn1 10.1016/j.bmcl.2010.09.009
76285459 104315 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.5 COC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109581 104315 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.5 COC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
86302495 111471 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5C#N)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288437 111471 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5C#N)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
24878983 170890 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 504 6 1 6 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(OC)c2)cn1 10.1021/jm800180e
CHEMBL446344 170890 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 504 6 1 6 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(OC)c2)cn1 10.1021/jm800180e
24879038 175141 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 510 5 1 5 5.8 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cc(F)cc(F)c2)cn1 10.1021/jm800180e
CHEMBL458264 175141 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 510 5 1 5 5.8 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cc(F)cc(F)c2)cn1 10.1021/jm800180e
24830595 186868 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 478 4 1 5 5.2 COC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL493983 186868 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 478 4 1 5 5.2 COC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
24878873 186805 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 462 4 1 4 5.0 CC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL493632 186805 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 462 4 1 4 5.0 CC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
24878871 186836 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 476 5 1 4 5.4 CCC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL493792 186836 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 476 5 1 4 5.4 CCC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
24878872 186981 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 488 5 1 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NC(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
CHEMBL494618 186981 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 488 5 1 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NC(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
52949425 18197 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 464 5 1 6 5.1 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccoc2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1271461 18197 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 464 5 1 6 5.1 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccoc2)cn1 10.1016/j.bmcl.2010.09.009
10390481 193806 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 481 9 2 4 4.2 CCCc1ccc(S(=O)(=O)N[C@@H](CC#Cc2ccc(NC)cc2)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
CHEMBL553108 193806 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 481 9 2 4 4.2 CCCc1ccc(S(=O)(=O)N[C@@H](CC#Cc2ccc(NC)cc2)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
52948306 17983 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 481 5 1 7 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2nccs2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1269815 17983 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 481 5 1 7 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2nccs2)cn1 10.1016/j.bmcl.2010.09.009
59016133 104313 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 435 4 1 4 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CO)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109579 104313 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 435 4 1 4 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CO)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
10077130 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2010.09.009
4047 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2010.09.009
4870 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2010.09.009
CHEMBL493982 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2010.09.009
DB09030 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2010.09.009
10077130 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4047 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4870 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL493982 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
DB09030 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
10077130 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400452v
4047 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400452v
4870 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400452v
CHEMBL493982 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400452v
DB09030 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400452v
86302515 111476 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5C#N)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288441 111476 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5C#N)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
24878981 188258 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 534 7 0 5 6.8 CCCN(C(=O)OCC)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm800180e
CHEMBL506808 188258 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 534 7 0 5 6.8 CCCN(C(=O)OCC)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm800180e
76332095 104307 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 542 6 2 5 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)NCCO)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109573 104307 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 542 6 2 5 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)NCCO)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
10077130 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C None
4047 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C None
4870 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C None
CHEMBL493982 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C None
DB09030 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C None
10077130 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 18447380
4047 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 18447380
4870 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 18447380
CHEMBL493982 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 18447380
DB09030 3932 49 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 18447380