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
118727607 116990 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 410 6 1 2 5.8 NC1(CN(C(=O)[C@@H]2C[C@H]2c2ccccc2)c2ccc(-c3ccccc3)cc2)CCCC1 10.1016/j.bmcl.2015.02.038
CHEMBL3400199 116990 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 410 6 1 2 5.8 NC1(CN(C(=O)[C@@H]2C[C@H]2c2ccccc2)c2ccc(-c3ccccc3)cc2)CCCC1 10.1016/j.bmcl.2015.02.038
118730169 117542 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 438 7 1 2 6.4 N[C@H](CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1016/j.bmcl.2015.02.038
CHEMBL3404056 117542 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 438 7 1 2 6.4 N[C@H](CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1016/j.bmcl.2015.02.038
118727606 116989 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 414 8 1 3 4.9 CO[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400198 116989 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 414 8 1 3 4.9 CO[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727605 116988 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 398 7 1 2 5.5 CC(C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400197 116988 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 398 7 1 2 5.5 CC(C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118730162 117535 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 414 9 1 2 5.9 CC(C)C[C@H](N)CN(C(=O)C(C)Cc1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3404049 117535 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 414 9 1 2 5.9 CC(C)C[C@H](N)CN(C(=O)C(C)Cc1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727608 116991 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 384 6 1 2 5.2 CC(C)(N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400200 116991 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 384 6 1 2 5.2 CC(C)(N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118730167 117540 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC[C@@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3404054 117540 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC[C@@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118730168 117541 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 452 8 1 2 6.8 N[C@@H](CC1CCCCC1)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3404055 117541 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 452 8 1 2 6.8 N[C@@H](CC1CCCCC1)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118730164 117537 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC(C)C[C@@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3404051 117537 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC(C)C[C@@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727610 116993 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 410 6 1 2 5.5 O=C([C@@H]1C[C@H]1c1ccccc1)N(CC1CCCNC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400202 116993 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 410 6 1 2 5.5 O=C([C@@H]1C[C@H]1c1ccccc1)N(CC1CCCNC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
10031 3347 5 None 2 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
134813902 3347 5 None 2 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
CHEMBL4595209 3347 5 None 2 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
51356430 117477 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3403768 117477 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51356141 117489 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 438 11 1 4 4.8 CCCC(C)COc1ccc([C@H](CN2CCOCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3403783 117489 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 438 11 1 4 4.8 CCCC(C)COc1ccc([C@H](CN2CCOCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355601 133154 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 439 12 3 4 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3714989 133154 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 439 12 3 4 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355320 133182 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 438 14 2 3 6.1 CCCC(C)COc1ccc([C@H](CNCC(C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715058 133182 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 438 14 2 3 6.1 CCCC(C)COc1ccc([C@H](CNCC(C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51356142 133204 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 369 9 2 3 4.5 CC[C@H](C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)[C@@H](C)O)cc1 nan
CHEMBL3715126 133204 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 369 9 2 3 4.5 CC[C@H](C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)[C@@H](C)O)cc1 nan
51355319 133219 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 451 13 3 4 4.8 CCCC(C)COc1ccc([C@H](CNC[C@@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715177 133219 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 451 13 3 4 4.8 CCCC(C)COc1ccc([C@H](CNC[C@@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51356138 133246 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 425 13 3 4 4.4 CCCC(C)COc1ccc([C@H](CNC[C@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715294 133246 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 425 13 3 4 4.4 CCCC(C)COc1ccc([C@H](CNC[C@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
58466420 133286 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 385 11 3 4 3.4 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CO)c2ccccc2)cc1 nan
CHEMBL3715473 133286 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 385 11 3 4 3.4 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CO)c2ccccc2)cc1 nan
51356137 133325 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2cccnc2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715603 133325 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2cccnc2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355600 133331 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 467 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)CCC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715622 133331 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 467 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)CCC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51356431 133436 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 448 13 3 4 5.0 CCCC(C)COc1ccc([C@H](CNCc2cc[nH]n2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715982 133436 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 448 13 3 4 5.0 CCCC(C)COc1ccc([C@H](CNCc2cc[nH]n2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355324 133459 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 383 11 2 3 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CC)c2ccccc2)cc1 nan
CHEMBL3716055 133459 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 383 11 2 3 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CC)c2ccccc2)cc1 nan
51355879 133533 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 497 13 3 3 6.7 CCCC(C)COc1ccc([C@H](CNCc2c[nH]c3ccccc23)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716282 133533 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 497 13 3 3 6.7 CCCC(C)COc1ccc([C@H](CNCc2c[nH]c3ccccc23)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
58466410 133649 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 451 11 1 4 4.7 CCCC(C)COc1ccc(C(CN2CCN(C)CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716700 133649 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 451 11 1 4 4.7 CCCC(C)COc1ccc(C(CN2CCN(C)CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355602 133831 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 465 13 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)C2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717324 133831 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 465 13 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)C2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355878 133883 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 483 14 3 5 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@@H](C)OC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717488 133883 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 483 14 3 5 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@@H](C)OC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355882 133888 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 522 14 3 6 4.6 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)Cc2cscn2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717512 133888 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 522 14 3 6 4.6 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)Cc2cscn2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355321 133922 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717617 133922 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355881 133957 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)[C@@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717750 133957 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)[C@@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355322 133984 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2ccncc2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717835 133984 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2ccncc2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355597 134021 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 479 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CC2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717978 134021 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 479 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CC2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
58466403 134264 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 452 13 2 4 5.1 CCCC(C)COc1ccc([C@H](CNCC2CCOC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3718752 134264 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 452 13 2 4 5.1 CCCC(C)COc1ccc([C@H](CNCC2CCOC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355599 134360 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 396 12 2 3 5.1 CCCNC[C@H](NC(=O)[C@@H](C)c1ccccc1)c1ccc(OC[C@@H](C)CC)cc1 nan
CHEMBL3719078 134360 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 396 12 2 3 5.1 CCCNC[C@H](NC(=O)[C@@H](C)c1ccccc1)c1ccc(OC[C@@H](C)CC)cc1 nan
51356430 117477 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3403768 117477 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51356141 117489 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 438 11 1 4 4.8 CCCC(C)COc1ccc([C@H](CN2CCOCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3403783 117489 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 438 11 1 4 4.8 CCCC(C)COc1ccc([C@H](CN2CCOCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355601 133154 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 439 12 3 4 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3714989 133154 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 439 12 3 4 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355320 133182 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 438 14 2 3 6.1 CCCC(C)COc1ccc([C@H](CNCC(C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715058 133182 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 438 14 2 3 6.1 CCCC(C)COc1ccc([C@H](CNCC(C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51356142 133204 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 369 9 2 3 4.5 CC[C@H](C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)[C@@H](C)O)cc1 nan
CHEMBL3715126 133204 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 369 9 2 3 4.5 CC[C@H](C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)[C@@H](C)O)cc1 nan
51355319 133219 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 451 13 3 4 4.8 CCCC(C)COc1ccc([C@H](CNC[C@@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715177 133219 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 451 13 3 4 4.8 CCCC(C)COc1ccc([C@H](CNC[C@@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51356138 133246 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 425 13 3 4 4.4 CCCC(C)COc1ccc([C@H](CNC[C@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715294 133246 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 425 13 3 4 4.4 CCCC(C)COc1ccc([C@H](CNC[C@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
58466420 133286 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 385 11 3 4 3.4 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CO)c2ccccc2)cc1 nan
CHEMBL3715473 133286 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 385 11 3 4 3.4 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CO)c2ccccc2)cc1 nan
51356137 133325 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2cccnc2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715603 133325 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2cccnc2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355600 133331 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 467 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)CCC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715622 133331 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 467 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)CCC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51356431 133436 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 448 13 3 4 5.0 CCCC(C)COc1ccc([C@H](CNCc2cc[nH]n2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715982 133436 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 448 13 3 4 5.0 CCCC(C)COc1ccc([C@H](CNCc2cc[nH]n2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355324 133459 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 383 11 2 3 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CC)c2ccccc2)cc1 nan
CHEMBL3716055 133459 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 383 11 2 3 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CC)c2ccccc2)cc1 nan
51355879 133533 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 497 13 3 3 6.7 CCCC(C)COc1ccc([C@H](CNCc2c[nH]c3ccccc23)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716282 133533 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 497 13 3 3 6.7 CCCC(C)COc1ccc([C@H](CNCc2c[nH]c3ccccc23)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
58466410 133649 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 451 11 1 4 4.7 CCCC(C)COc1ccc(C(CN2CCN(C)CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716700 133649 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 451 11 1 4 4.7 CCCC(C)COc1ccc(C(CN2CCN(C)CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355602 133831 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 465 13 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)C2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717324 133831 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 465 13 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)C2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355878 133883 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 483 14 3 5 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@@H](C)OC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717488 133883 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 483 14 3 5 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@@H](C)OC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355882 133888 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 522 14 3 6 4.6 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)Cc2cscn2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717512 133888 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 522 14 3 6 4.6 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)Cc2cscn2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355321 133922 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717617 133922 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355881 133957 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)[C@@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717750 133957 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)[C@@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355322 133984 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2ccncc2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717835 133984 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2ccncc2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355597 134021 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 479 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CC2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717978 134021 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 479 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CC2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
58466403 134264 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 452 13 2 4 5.1 CCCC(C)COc1ccc([C@H](CNCC2CCOC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3718752 134264 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 452 13 2 4 5.1 CCCC(C)COc1ccc([C@H](CNCC2CCOC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355599 134360 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 396 12 2 3 5.1 CCCNC[C@H](NC(=O)[C@@H](C)c1ccccc1)c1ccc(OC[C@@H](C)CC)cc1 nan
CHEMBL3719078 134360 0 None - 1 Human 7.0 pEC50 = 7 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 396 12 2 3 5.1 CCCNC[C@H](NC(=O)[C@@H](C)c1ccccc1)c1ccc(OC[C@@H](C)CC)cc1 nan
162659346 180726 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 463 10 2 5 4.6 C[C@H](C(=O)N[C@@H](C(=O)NCc1nccs1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4762642 180726 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 463 10 2 5 4.6 C[C@H](C(=O)N[C@@H](C(=O)NCc1nccs1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
118727649 117030 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 413 8 1 3 5.3 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2cccnc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400240 117030 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 413 8 1 3 5.3 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2cccnc2)cc1 10.1016/j.bmcl.2015.02.038
168279298 190443 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 433 10 2 6 3.6 C[C@H](C(=O)N[C@@H](Cn1cc(CN)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5187140 190443 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 433 10 2 6 3.6 C[C@H](C(=O)N[C@@H](Cn1cc(CN)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168279298 190443 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 433 10 2 6 3.6 C[C@H](C(=O)N[C@@H](Cn1cc(CN)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5187140 190443 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 433 10 2 6 3.6 C[C@H](C(=O)N[C@@H](Cn1cc(CN)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
118727609 116992 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 6 1 2 5.9 CC(C)(C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400201 116992 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 6 1 2 5.9 CC(C)(C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
51356430 117477 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403768 117477 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
118730001 117478 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403772 117478 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
58466401 117486 0 None 6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403780 117486 0 None 6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3884102 117486 0 None 6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
118727684 117065 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 498 11 1 4 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(CCC(=O)OC)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400275 117065 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 498 11 1 4 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(CCC(=O)OC)cc2)cc1 10.1016/j.bmcl.2015.02.038
51355323 133504 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2ccccn2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716191 133504 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2ccccn2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355323 133504 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2ccccn2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716191 133504 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 459 13 2 4 5.6 CCCC(C)COc1ccc([C@H](CNCc2ccccn2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
118727661 117042 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 1 3 5.9 COc1cccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)c1 10.1016/j.bmcl.2015.02.038
CHEMBL3400252 117042 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 1 3 5.9 COc1cccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)c1 10.1016/j.bmcl.2015.02.038
118727682 117063 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 2 3 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(CO)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400273 117063 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 2 3 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(CO)cc2)cc1 10.1016/j.bmcl.2015.02.038
118727633 117013 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 448 8 1 2 6.1 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1c(F)cccc1F)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400224 117013 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 448 8 1 2 6.1 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1c(F)cccc1F)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
162651180 179598 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 421 11 1 5 5.1 CCCC(C)COc1ccc([C@H](Cc2nnco2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4749371 179598 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 421 11 1 5 5.1 CCCC(C)COc1ccc([C@H](Cc2nnco2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162651180 179598 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 421 11 1 5 5.1 CCCC(C)COc1ccc([C@H](Cc2nnco2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4749371 179598 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 421 11 1 5 5.1 CCCC(C)COc1ccc([C@H](Cc2nnco2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
168282483 190140 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 10 1 6 4.3 CC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5182820 190140 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 10 1 6 4.3 CC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
58466521 1044 3 None -29 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
7798 1044 3 None -29 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
CHEMBL3401461 1044 3 None -29 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
168282483 190140 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 10 1 6 4.3 CC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5182820 190140 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 10 1 6 4.3 CC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
162647665 179204 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 410 11 2 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4744793 179204 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 410 11 2 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC)cc1 10.1021/acs.jmedchem.0c01581
118730004 117482 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 385 11 2 4 4.0 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](OC)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403776 117482 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 385 11 2 4 4.0 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](OC)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
118727677 117058 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 1 3 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400268 117058 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 1 3 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2015.02.038
162647665 179204 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 410 11 2 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4744793 179204 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 410 11 2 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC)cc1 10.1021/acs.jmedchem.0c01581
118727625 117007 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 8 1 2 6.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(C)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400216 117007 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 8 1 2 6.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(C)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727651 117032 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 418 8 1 3 5.9 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400242 117032 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 418 8 1 3 5.9 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2015.02.038
118727654 117035 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 402 8 1 2 5.8 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(C2=CCCC2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400245 117035 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 402 8 1 2 5.8 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(C2=CCCC2)cc1 10.1016/j.bmcl.2015.02.038
118727656 117037 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 416 8 1 2 6.2 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(C2=CCCCC2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400247 117037 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 416 8 1 2 6.2 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(C2=CCCCC2)cc1 10.1016/j.bmcl.2015.02.038
118727658 117039 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 8 1 2 6.2 Cc1cccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)c1 10.1016/j.bmcl.2015.02.038
CHEMBL3400249 117039 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 8 1 2 6.2 Cc1cccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)c1 10.1016/j.bmcl.2015.02.038
118727688 117069 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 505 10 2 4 5.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(NS(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400279 117069 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 505 10 2 4 5.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(NS(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2015.02.038
118727693 117073 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 457 10 1 4 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@H]1C[C@@H]1c1ccccn1)c1ccc(-c2ccc(COC)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400284 117073 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 457 10 1 4 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@H]1C[C@@H]1c1ccccn1)c1ccc(-c2ccc(COC)cc2)cc1 10.1016/j.bmcl.2015.02.038
51348369 117498 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 373 9 2 4 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3403792 117498 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 373 9 2 4 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
51348369 117498 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 373 9 2 4 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3403792 117498 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 373 9 2 4 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
58466521 1044 3 None 29 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
7798 1044 3 None 29 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
CHEMBL3401461 1044 3 None 29 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
155524266 175915 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4454851 175915 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4596750 175915 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
155555152 175922 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 445 9 1 5 4.3 COc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4550415 175922 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 445 9 1 5 4.3 COc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4596869 175922 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 445 9 1 5 4.3 COc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
155566460 176017 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 475 9 1 3 6.5 CCCc1ccc(-c2ccc(N(C[C@@H](N)c3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4587388 176017 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 475 9 1 3 6.5 CCCc1ccc(-c2ccc(N(C[C@@H](N)c3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4597686 176017 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 475 9 1 3 6.5 CCCc1ccc(-c2ccc(N(C[C@@H](N)c3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
58466521 1044 3 None 29 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
7798 1044 3 None 29 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
CHEMBL3401461 1044 3 None 29 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
155524266 175915 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4454851 175915 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4596750 175915 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
155555152 175922 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 445 9 1 5 4.3 COc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4550415 175922 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 445 9 1 5 4.3 COc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4596869 175922 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 445 9 1 5 4.3 COc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
155566460 176017 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 475 9 1 3 6.5 CCCc1ccc(-c2ccc(N(C[C@@H](N)c3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4587388 176017 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 475 9 1 3 6.5 CCCc1ccc(-c2ccc(N(C[C@@H](N)c3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4597686 176017 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 475 9 1 3 6.5 CCCc1ccc(-c2ccc(N(C[C@@H](N)c3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
162667879 181813 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 389 8 2 3 4.1 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CC(F)(F)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4785604 181813 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 389 8 2 3 4.1 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CC(F)(F)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162667879 181813 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 389 8 2 3 4.1 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CC(F)(F)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4785604 181813 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 389 8 2 3 4.1 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CC(F)(F)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
168275346 189635 0 None 549 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 477 12 2 6 4.1 CCC[C@H](C)COc1ccc([C@H](Cn2cc(C(=O)NC)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL5175064 189635 0 None 549 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 477 12 2 6 4.1 CCC[C@H](C)COc1ccc([C@H](Cn2cc(C(=O)NC)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
118727634 117014 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 413 8 1 3 5.3 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400225 117014 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 413 8 1 3 5.3 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727637 117017 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 414 8 1 4 4.7 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ncccn1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400228 117017 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 414 8 1 4 4.7 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ncccn1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727632 117012 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 448 8 1 2 6.1 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cc1F)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400223 117012 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 448 8 1 2 6.1 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cc1F)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727644 117025 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 433 8 1 4 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ncc(C)s1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400235 117025 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 433 8 1 4 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ncc(C)s1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727650 117031 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 413 8 1 3 5.3 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccncc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400241 117031 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 413 8 1 3 5.3 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccncc2)cc1 10.1016/j.bmcl.2015.02.038
168292704 191453 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nc(C)no2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL5202571 191453 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nc(C)no2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
168292704 191453 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nc(C)no2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL5202571 191453 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nc(C)no2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
86658399 141644 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 394 11 1 3 5.8 CCCC(C)COc1ccc([C@H](CN=[N+]=[N-])NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884002 141644 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 394 11 1 3 5.8 CCCC(C)COc1ccc([C@H](CN=[N+]=[N-])NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
86658399 141644 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 394 11 1 3 5.8 CCCC(C)COc1ccc([C@H](CN=[N+]=[N-])NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884002 141644 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 394 11 1 3 5.8 CCCC(C)COc1ccc([C@H](CN=[N+]=[N-])NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
162669690 183154 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 420 9 2 6 4.0 C[C@H](C(=O)N[C@@H](Cc1nnc(N)o1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4789484 183154 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 420 9 2 6 4.0 C[C@H](C(=O)N[C@@H](Cc1nnc(N)o1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4803720 183154 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 420 9 2 6 4.0 C[C@H](C(=O)N[C@@H](Cc1nnc(N)o1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162672689 183176 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4795623 183176 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4803902 183176 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162669690 183154 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 420 9 2 6 4.0 C[C@H](C(=O)N[C@@H](Cc1nnc(N)o1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4789484 183154 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 420 9 2 6 4.0 C[C@H](C(=O)N[C@@H](Cc1nnc(N)o1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4803720 183154 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 420 9 2 6 4.0 C[C@H](C(=O)N[C@@H](Cc1nnc(N)o1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162672689 183176 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4795623 183176 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4803902 183176 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
168275346 189635 0 None 549 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 477 12 2 6 4.1 CCC[C@H](C)COc1ccc([C@H](Cn2cc(C(=O)NC)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL5175064 189635 0 None 549 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 477 12 2 6 4.1 CCC[C@H](C)COc1ccc([C@H](Cn2cc(C(=O)NC)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
51355324 133459 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 11 2 3 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CC)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3716055 133459 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 11 2 3 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CC)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
134131592 141720 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 12 2 3 4.7 CCCC(C)COc1ccc([C@H](CO)NC(=O)CCCc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884899 141720 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 12 2 3 4.7 CCCC(C)COc1ccc([C@H](CO)NC(=O)CCCc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
134131592 141720 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 12 2 3 4.7 CCCC(C)COc1ccc([C@H](CO)NC(=O)CCCc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884899 141720 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 12 2 3 4.7 CCCC(C)COc1ccc([C@H](CO)NC(=O)CCCc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
51355324 133459 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 11 2 3 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CC)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3716055 133459 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 11 2 3 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CC)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
162656011 180176 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nnc(C)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4756228 180176 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nnc(C)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162656011 180176 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nnc(C)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL4756228 180176 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nnc(C)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
162656011 180176 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nnc(C)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4756228 180176 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nnc(C)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162656011 180176 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nnc(C)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL4756228 180176 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 435 11 1 5 5.4 CCCC(C)COc1ccc([C@H](Cc2nnc(C)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
51348956 117184 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 457 10 1 4 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(COC)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3401459 117184 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 457 10 1 4 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(COC)cc2)cc1 10.1016/j.bmcl.2015.02.038
118730006 117484 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 398 11 2 3 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)N(CC)Cc2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403778 117484 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 398 11 2 3 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)N(CC)Cc2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
118727635 117015 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 413 8 1 3 5.3 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccnc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400226 117015 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 413 8 1 3 5.3 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccnc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727636 117016 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 413 8 1 3 5.3 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccncc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400227 117016 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 413 8 1 3 5.3 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccncc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727646 117027 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 433 8 1 4 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1csc(C)n1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400237 117027 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 433 8 1 4 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1csc(C)n1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727652 117033 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 418 8 1 3 5.9 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400243 117033 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 418 8 1 3 5.9 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2015.02.038
51356139 133221 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 451 13 3 4 4.8 CCCC(C)COc1ccc([C@H](CNC[C@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715186 133221 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 451 13 3 4 4.8 CCCC(C)COc1ccc([C@H](CNC[C@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51356139 133221 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 451 13 3 4 4.8 CCCC(C)COc1ccc([C@H](CNC[C@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715186 133221 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 451 13 3 4 4.8 CCCC(C)COc1ccc([C@H](CNC[C@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
155516532 175656 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 441 9 1 3 5.8 CCCc1ccc(-c2ccc(N(C[C@@H](N)C(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4443664 175656 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 441 9 1 3 5.8 CCCc1ccc(-c2ccc(N(C[C@@H](N)C(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4594745 175656 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 441 9 1 3 5.8 CCCc1ccc(-c2ccc(N(C[C@@H](N)C(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
155516532 175656 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 441 9 1 3 5.8 CCCc1ccc(-c2ccc(N(C[C@@H](N)C(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4443664 175656 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 441 9 1 3 5.8 CCCc1ccc(-c2ccc(N(C[C@@H](N)C(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4594745 175656 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 441 9 1 3 5.8 CCCc1ccc(-c2ccc(N(C[C@@H](N)C(C)C)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
118730008 117491 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 369 9 2 3 4.4 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)c(C)c1 10.1016/j.bmcl.2015.01.036
CHEMBL3403785 117491 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 369 9 2 3 4.4 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)c(C)c1 10.1016/j.bmcl.2015.01.036
118727627 117008 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 437 8 1 3 5.7 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(C#N)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400218 117008 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 437 8 1 3 5.7 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(C#N)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727665 117046 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2F)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400256 117046 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2F)cc1 10.1016/j.bmcl.2015.02.038
168275843 189753 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 476 11 1 7 4.2 CC(=O)OCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5177010 189753 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 476 11 1 7 4.2 CC(=O)OCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
168288763 190828 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 476 11 1 7 4.3 CCOC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5192946 190828 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 476 11 1 7 4.3 CCOC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
168275843 189753 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 476 11 1 7 4.2 CC(=O)OCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5177010 189753 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 476 11 1 7 4.2 CC(=O)OCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
168288763 190828 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 476 11 1 7 4.3 CCOC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5192946 190828 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 476 11 1 7 4.3 CCOC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
118730003 117480 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 341 9 2 3 4.0 CCCC(C)COc1ccc([C@H](CO)NC(=O)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403774 117480 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 341 9 2 3 4.0 CCCC(C)COc1ccc([C@H](CO)NC(=O)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
118730011 117494 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 383 9 2 3 4.7 CC[C@H](C)COc1cc(C)c([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)c(C)c1 10.1016/j.bmcl.2015.01.036
CHEMBL3403788 117494 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 383 9 2 3 4.7 CC[C@H](C)COc1cc(C)c([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)c(C)c1 10.1016/j.bmcl.2015.01.036
118727679 117060 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 496 9 1 3 6.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400270 117060 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 496 9 1 3 6.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2015.02.038
67438968 117476 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 9 2 3 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL3403767 117476 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 9 2 3 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
67438968 117476 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 9 2 3 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL3403767 117476 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 9 2 3 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
168291461 191263 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 1 5 4.1 C[C@H](C(=O)N[C@@H](Cn1cncn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5199510 191263 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 1 5 4.1 C[C@H](C(=O)N[C@@H](Cn1cncn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168291461 191263 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 1 5 4.1 C[C@H](C(=O)N[C@@H](Cn1cncn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5199510 191263 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 1 5 4.1 C[C@H](C(=O)N[C@@H](Cn1cncn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
162667116 181883 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 424 11 2 3 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4786591 181883 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 424 11 2 3 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)C)cc1 10.1021/acs.jmedchem.0c01581
168274529 189658 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 480 10 1 5 5.8 C[C@H](C(=O)N[C@@H](Cn1cc(-c2ccccc2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5175440 189658 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 480 10 1 5 5.8 C[C@H](C(=O)N[C@@H](Cn1cc(-c2ccccc2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168281814 190378 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 11 1 5 5.1 CCCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5186221 190378 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 11 1 5 5.1 CCCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
162667116 181883 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 424 11 2 3 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4786591 181883 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 424 11 2 3 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)C)cc1 10.1021/acs.jmedchem.0c01581
168274529 189658 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 480 10 1 5 5.8 C[C@H](C(=O)N[C@@H](Cn1cc(-c2ccccc2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5175440 189658 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 480 10 1 5 5.8 C[C@H](C(=O)N[C@@H](Cn1cc(-c2ccccc2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168281814 190378 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 11 1 5 5.1 CCCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5186221 190378 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 11 1 5 5.1 CCCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
67438968 117476 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 355 9 2 3 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403767 117476 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 355 9 2 3 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
118730010 117493 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 385 10 2 4 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)c(OC)c1 10.1016/j.bmcl.2015.01.036
CHEMBL3403787 117493 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 385 10 2 4 4.1 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)c(OC)c1 10.1016/j.bmcl.2015.01.036
118727638 117018 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 414 8 1 4 4.7 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cncnc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400229 117018 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 414 8 1 4 4.7 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cncnc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
51356430 117477 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3403768 117477 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
51356430 117477 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL3403768 117477 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
51356430 117477 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3403768 117477 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
51356430 117477 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL3403768 117477 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
168281296 190200 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 447 11 2 6 3.8 CNCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5183784 190200 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 447 11 2 6 3.8 CNCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
168281296 190200 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 447 11 2 6 3.8 CNCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5183784 190200 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 447 11 2 6 3.8 CNCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
118727612 116995 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 440 10 1 2 6.6 CCC(CC)C(N)CCN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400204 116995 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 440 10 1 2 6.6 CCC(CC)C(N)CCN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118730165 117538 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 9 1 2 6.1 CN[C@@H](CC(C)C)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3404052 117538 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 9 1 2 6.1 CN[C@@H](CC(C)C)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727616 116999 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 438 9 1 2 6.3 O=C([C@@H]1C[C@H]1c1ccccc1)N(CCNCC1CCCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400208 116999 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 438 9 1 2 6.3 O=C([C@@H]1C[C@H]1c1ccccc1)N(CCNCC1CCCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727653 117034 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 402 8 1 3 5.5 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccoc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400244 117034 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 402 8 1 3 5.5 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccoc2)cc1 10.1016/j.bmcl.2015.02.038
162660471 180755 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 12 2 3 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4763023 180755 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 12 2 3 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CC2)cc1 10.1021/acs.jmedchem.0c01581
162661701 180901 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 450 11 2 3 5.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCCC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4764798 180901 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 450 11 2 3 5.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCCC2)cc1 10.1021/acs.jmedchem.0c01581
162660471 180755 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 12 2 3 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4763023 180755 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 12 2 3 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CC2)cc1 10.1021/acs.jmedchem.0c01581
162661701 180901 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 450 11 2 3 5.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCCC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4764798 180901 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 450 11 2 3 5.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCCC2)cc1 10.1021/acs.jmedchem.0c01581
118727639 117020 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 419 8 1 4 5.3 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1nccs1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400230 117020 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 419 8 1 4 5.3 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1nccs1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727655 117036 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.5 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(C2=CCCCCC2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400246 117036 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.5 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(C2=CCCCCC2)cc1 10.1016/j.bmcl.2015.02.038
118727664 117045 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2cccc(F)c2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400255 117045 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2cccc(F)c2)cc1 10.1016/j.bmcl.2015.02.038
162654782 179995 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 452 12 2 3 5.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)C(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4754332 179995 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 452 12 2 3 5.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)C(C)C)cc1 10.1021/acs.jmedchem.0c01581
162654782 179995 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 452 12 2 3 5.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)C(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4754332 179995 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 452 12 2 3 5.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)C(C)C)cc1 10.1021/acs.jmedchem.0c01581
162657753 180434 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 472 12 2 3 5.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4759273 180434 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 472 12 2 3 5.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162657753 180434 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 472 12 2 3 5.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4759273 180434 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 472 12 2 3 5.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
118727618 117002 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 446 8 1 2 6.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(Cl)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400210 117002 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 446 8 1 2 6.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(Cl)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727670 117051 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400261 117051 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727647 117028 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2015.02.038
CHEMBL3400238 117028 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2015.02.038
162658043 180555 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 450 11 2 3 5.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2(C)CCC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4760733 180555 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 450 11 2 3 5.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2(C)CCC2)cc1 10.1021/acs.jmedchem.0c01581
162661453 180831 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 353 8 2 3 3.8 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4763920 180831 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 353 8 2 3 3.8 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162658043 180555 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 450 11 2 3 5.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2(C)CCC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4760733 180555 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 450 11 2 3 5.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2(C)CCC2)cc1 10.1021/acs.jmedchem.0c01581
162661453 180831 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 353 8 2 3 3.8 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4763920 180831 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 353 8 2 3 3.8 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162659288 180698 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 11 2 3 4.7 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4762227 180698 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 11 2 3 4.7 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CC2)cc1 10.1021/acs.jmedchem.0c01581
162659288 180698 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 11 2 3 4.7 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4762227 180698 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 11 2 3 4.7 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CC2)cc1 10.1021/acs.jmedchem.0c01581
51348522 117474 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as [35S]GTPgammaS binding after 60 mins by trilux scintillation counting analysis relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as [35S]GTPgammaS binding after 60 mins by trilux scintillation counting analysis relative to control
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403765 117474 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as [35S]GTPgammaS binding after 60 mins by trilux scintillation counting analysis relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as [35S]GTPgammaS binding after 60 mins by trilux scintillation counting analysis relative to control
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 10.1016/j.bmcl.2015.01.036
162666891 181928 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 438 12 2 3 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)CC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4787141 181928 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 438 12 2 3 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)CC)cc1 10.1021/acs.jmedchem.0c01581
162670172 182158 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 458 11 2 3 6.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4790074 182158 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 458 11 2 3 6.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
168276612 189776 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 444 10 1 5 5.0 C[C@H](C(=O)N[C@@H](Cn1cc(C2CC2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5177434 189776 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 444 10 1 5 5.0 C[C@H](C(=O)N[C@@H](Cn1cc(C2CC2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
162666891 181928 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 438 12 2 3 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)CC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4787141 181928 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 438 12 2 3 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)CC)cc1 10.1021/acs.jmedchem.0c01581
162670172 182158 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 458 11 2 3 6.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4790074 182158 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 458 11 2 3 6.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)Nc2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
168276612 189776 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 444 10 1 5 5.0 C[C@H](C(=O)N[C@@H](Cn1cc(C2CC2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5177434 189776 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 444 10 1 5 5.0 C[C@H](C(=O)N[C@@H](Cn1cc(C2CC2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
10031 3347 5 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
134813902 3347 5 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
CHEMBL4595209 3347 5 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
10031 3347 5 None -2 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation countingAgonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation counting
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.0c01581
134813902 3347 5 None -2 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation countingAgonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation counting
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.0c01581
CHEMBL4595209 3347 5 None -2 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation countingAgonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation counting
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.0c01581
10031 3347 5 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
134813902 3347 5 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
CHEMBL4595209 3347 5 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
118730018 117500 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 331 5 2 2 3.8 O=C(N[C@@H](CO)c1ccc2ccccc2c1)[C@H]1C[C@@H]1c1ccccc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403797 117500 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 331 5 2 2 3.8 O=C(N[C@@H](CO)c1ccc2ccccc2c1)[C@H]1C[C@@H]1c1ccccc1 10.1016/j.bmcl.2015.01.036
162657060 180307 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 9 2 3 4.1 CCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4757666 180307 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 9 2 3 4.1 CCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162657060 180307 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 9 2 3 4.1 CCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4757666 180307 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 9 2 3 4.1 CCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
58466412 133773 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 380 8 2 3 4.4 CC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)[C@H]2CCCN2)cc1 nan
CHEMBL3717100 133773 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 380 8 2 3 4.4 CC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)[C@H]2CCCN2)cc1 nan
58466412 133773 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 380 8 2 3 4.4 CC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)[C@H]2CCCN2)cc1 nan
CHEMBL3717100 133773 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 380 8 2 3 4.4 CC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)[C@H]2CCCN2)cc1 nan
162646899 178983 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 367 8 2 3 4.2 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CCCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4741911 178983 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 367 8 2 3 4.2 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CCCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162646899 178983 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 367 8 2 3 4.2 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CCCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4741911 178983 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 367 8 2 3 4.2 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CCCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
118730012 117495 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 370 9 2 4 3.8 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)c(C)n1 10.1016/j.bmcl.2015.01.036
CHEMBL3403789 117495 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 370 9 2 4 3.8 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)c(C)n1 10.1016/j.bmcl.2015.01.036
118727685 117066 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 484 10 1 4 6.0 CCOC(=O)c1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400276 117066 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 484 10 1 4 6.0 CCOC(=O)c1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
168289890 190796 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 10 1 5 4.7 CCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5192533 190796 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 10 1 5 4.7 CCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
168289890 190796 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 10 1 5 4.7 CCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5192533 190796 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 10 1 5 4.7 CCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
134131464 141750 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 10 1 4 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3885190 141750 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 10 1 4 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
134131464 141750 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 10 1 4 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3885190 141750 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 383 10 1 4 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
162643661 181098 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 12 2 4 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccco2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4776570 181098 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 12 2 4 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccco2)cc1 10.1021/acs.jmedchem.0c01581
162643661 181098 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 12 2 4 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccco2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4776570 181098 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 12 2 4 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccco2)cc1 10.1021/acs.jmedchem.0c01581
51354469 117485 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 397 10 2 3 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(C)(C)O)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403779 117485 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 397 10 2 3 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(C)(C)O)cc1 10.1016/j.bmcl.2015.01.036
118727681 117062 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 498 10 1 3 7.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(COC(C)(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400272 117062 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 498 10 1 3 7.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(COC(C)(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
162661800 180862 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CC(C)CCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4764409 180862 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CC(C)CCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162674526 182846 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 3 5.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4798774 182846 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 3 5.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCC2)cc1 10.1021/acs.jmedchem.0c01581
168279345 190516 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 448 11 1 6 4.3 COCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5188019 190516 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 448 11 1 6 4.3 COCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
162661800 180862 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CC(C)CCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4764409 180862 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.5 CC(C)CCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162674526 182846 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 3 5.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4798774 182846 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 3 5.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCC2)cc1 10.1021/acs.jmedchem.0c01581
168279345 190516 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 448 11 1 6 4.3 COCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5188019 190516 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 448 11 1 6 4.3 COCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
51355032 117487 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 396 11 1 3 5.0 CCCC(C)COc1ccc([C@H](CN(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403781 117487 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 396 11 1 3 5.0 CCCC(C)COc1ccc([C@H](CN(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
162654604 180023 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 396 10 2 3 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4754668 180023 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 396 10 2 3 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC)cc1 10.1021/acs.jmedchem.0c01581
162669183 182121 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 10 2 3 4.2 CCCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4789594 182121 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 10 2 3 4.2 CCCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162676113 182770 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 405 9 1 5 4.5 C[C@H](C(=O)N[C@@H](Cc1nnco1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4797747 182770 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 405 9 1 5 4.5 C[C@H](C(=O)N[C@@H](Cc1nnco1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162654604 180023 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 396 10 2 3 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL4754668 180023 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 396 10 2 3 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC)cc1 10.1021/acs.jmedchem.1c01075
162654604 180023 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 396 10 2 3 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4754668 180023 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 396 10 2 3 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC)cc1 10.1021/acs.jmedchem.0c01581
162669183 182121 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 10 2 3 4.2 CCCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4789594 182121 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 355 10 2 3 4.2 CCCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162676113 182770 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 405 9 1 5 4.5 C[C@H](C(=O)N[C@@H](Cc1nnco1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4797747 182770 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 405 9 1 5 4.5 C[C@H](C(=O)N[C@@H](Cc1nnco1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
58466521 1044 3 None 29 2 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N nan
7798 1044 3 None 29 2 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N nan
CHEMBL3401461 1044 3 None 29 2 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N nan
51348956 117184 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 457 10 1 4 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(COC)cc2)cc1 nan
CHEMBL3401459 117184 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 457 10 1 4 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(COC)cc2)cc1 nan
51348672 117185 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 471 10 1 4 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 nan
CHEMBL3401460 117185 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 471 10 1 4 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 nan
58466519 133901 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 421 10 1 4 4.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(OCC2CCC2)cc1 nan
CHEMBL3717562 133901 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 421 10 1 4 4.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(OCC2CCC2)cc1 nan
51348816 134624 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(-c2ccc(COC)cc2)cc1 nan
CHEMBL3715838 134624 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(-c2ccc(COC)cc2)cc1 nan
CHEMBL3719573 134624 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(-c2ccc(COC)cc2)cc1 nan
51348952 134625 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 451 8 1 3 5.6 CC#Cc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
CHEMBL3719007 134625 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 451 8 1 3 5.6 CC#Cc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
CHEMBL3719574 134625 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 451 8 1 3 5.6 CC#Cc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
58466522 134626 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 471 8 1 3 6.2 CCCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3718084 134626 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 471 8 1 3 6.2 CCCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3719575 134626 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 471 8 1 3 6.2 CCCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
58466530 134627 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 487 8 1 4 6.1 CC(C)Oc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3714801 134627 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 487 8 1 4 6.1 CC(C)Oc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3719576 134627 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 487 8 1 4 6.1 CC(C)Oc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
58466532 134628 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 473 8 1 4 5.4 COCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3718807 134628 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 473 8 1 4 5.4 COCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3719577 134628 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 473 8 1 4 5.4 COCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
58466518 134629 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 469 8 1 4 5.3 CCCc1ccc(-c2ccc(N(CC3(N)CCOCC3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
CHEMBL3716013 134629 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 469 8 1 4 5.3 CCCc1ccc(-c2ccc(N(CC3(N)CCOCC3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
CHEMBL3719578 134629 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 469 8 1 4 5.3 CCCc1ccc(-c2ccc(N(CC3(N)CCOCC3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
127024356 134630 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ncccc3F)cc2)cc1 nan
CHEMBL3718515 134630 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ncccc3F)cc2)cc1 nan
CHEMBL3719579 134630 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ncccc3F)cc2)cc1 nan
67114108 134631 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 456 10 1 4 5.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
CHEMBL3715829 134631 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 456 10 1 4 5.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
CHEMBL3719580 134631 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 456 10 1 4 5.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
58466524 134632 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3715807 134632 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3719581 134632 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
58466514 134634 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(COC)cc2)cc1 nan
CHEMBL3717656 134634 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(COC)cc2)cc1 nan
CHEMBL3719583 134634 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(COC)cc2)cc1 nan
58466535 134635 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 439 10 1 4 4.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(OCC2CCC2)cc1 nan
CHEMBL3716470 134635 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 439 10 1 4 4.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(OCC2CCC2)cc1 nan
CHEMBL3719584 134635 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 439 10 1 4 4.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(OCC2CCC2)cc1 nan
58466528 134636 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 458 10 1 5 4.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
CHEMBL3718875 134636 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 458 10 1 5 4.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
CHEMBL3719585 134636 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 458 10 1 5 4.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
86658431 134637 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 421 8 1 3 4.9 CCCC#Cc1ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]2C[C@@H]2c2cccc(F)n2)cc1 nan
CHEMBL3718945 134637 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 421 8 1 3 4.9 CCCC#Cc1ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]2C[C@@H]2c2cccc(F)n2)cc1 nan
CHEMBL3719586 134637 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 421 8 1 3 4.9 CCCC#Cc1ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]2C[C@@H]2c2cccc(F)n2)cc1 nan
51349088 134638 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 445 8 1 3 5.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc2cc(C3CC3)ccc2c1 nan
CHEMBL3718796 134638 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 445 8 1 3 5.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc2cc(C3CC3)ccc2c1 nan
CHEMBL3719587 134638 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 445 8 1 3 5.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc2cc(C3CC3)ccc2c1 nan
58466521 1044 3 None 29 2 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N nan
7798 1044 3 None 29 2 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N nan
CHEMBL3401461 1044 3 None 29 2 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N nan
51348956 117184 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 457 10 1 4 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(COC)cc2)cc1 nan
CHEMBL3401459 117184 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 457 10 1 4 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(COC)cc2)cc1 nan
51348672 117185 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 471 10 1 4 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 nan
CHEMBL3401460 117185 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 471 10 1 4 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 nan
58466519 133901 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 421 10 1 4 4.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(OCC2CCC2)cc1 nan
CHEMBL3717562 133901 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 421 10 1 4 4.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(OCC2CCC2)cc1 nan
51348816 134624 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(-c2ccc(COC)cc2)cc1 nan
CHEMBL3715838 134624 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(-c2ccc(COC)cc2)cc1 nan
CHEMBL3719573 134624 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(-c2ccc(COC)cc2)cc1 nan
51348952 134625 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 451 8 1 3 5.6 CC#Cc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
CHEMBL3719007 134625 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 451 8 1 3 5.6 CC#Cc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
CHEMBL3719574 134625 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 451 8 1 3 5.6 CC#Cc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
58466522 134626 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 471 8 1 3 6.2 CCCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3718084 134626 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 471 8 1 3 6.2 CCCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3719575 134626 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 471 8 1 3 6.2 CCCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
58466530 134627 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 487 8 1 4 6.1 CC(C)Oc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3714801 134627 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 487 8 1 4 6.1 CC(C)Oc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3719576 134627 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 487 8 1 4 6.1 CC(C)Oc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
58466532 134628 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 473 8 1 4 5.4 COCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3718807 134628 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 473 8 1 4 5.4 COCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3719577 134628 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 473 8 1 4 5.4 COCc1ccc(-c2ccc(N(CC3(N)CCCC3)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
58466518 134629 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 469 8 1 4 5.3 CCCc1ccc(-c2ccc(N(CC3(N)CCOCC3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
CHEMBL3716013 134629 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 469 8 1 4 5.3 CCCc1ccc(-c2ccc(N(CC3(N)CCOCC3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
CHEMBL3719578 134629 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 469 8 1 4 5.3 CCCc1ccc(-c2ccc(N(CC3(N)CCOCC3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 nan
127024356 134630 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ncccc3F)cc2)cc1 nan
CHEMBL3718515 134630 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ncccc3F)cc2)cc1 nan
CHEMBL3719579 134630 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ncccc3F)cc2)cc1 nan
67114108 134631 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 456 10 1 4 5.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
CHEMBL3715829 134631 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 456 10 1 4 5.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
CHEMBL3719580 134631 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 456 10 1 4 5.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
58466524 134632 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3715807 134632 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
CHEMBL3719581 134632 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 473 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3cccc(F)n3)cc2)cc1 nan
58466514 134634 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(COC)cc2)cc1 nan
CHEMBL3717656 134634 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(COC)cc2)cc1 nan
CHEMBL3719583 134634 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 475 10 1 4 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(COC)cc2)cc1 nan
58466535 134635 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 439 10 1 4 4.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(OCC2CCC2)cc1 nan
CHEMBL3716470 134635 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 439 10 1 4 4.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(OCC2CCC2)cc1 nan
CHEMBL3719584 134635 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 439 10 1 4 4.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(OCC2CCC2)cc1 nan
58466528 134636 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 458 10 1 5 4.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
CHEMBL3718875 134636 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 458 10 1 5 4.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
CHEMBL3719585 134636 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 458 10 1 5 4.6 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3cnccn3)cc2)cc1 nan
86658431 134637 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 421 8 1 3 4.9 CCCC#Cc1ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]2C[C@@H]2c2cccc(F)n2)cc1 nan
CHEMBL3718945 134637 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 421 8 1 3 4.9 CCCC#Cc1ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]2C[C@@H]2c2cccc(F)n2)cc1 nan
CHEMBL3719586 134637 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 421 8 1 3 4.9 CCCC#Cc1ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]2C[C@@H]2c2cccc(F)n2)cc1 nan
51349088 134638 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 445 8 1 3 5.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc2cc(C3CC3)ccc2c1 nan
CHEMBL3718796 134638 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 445 8 1 3 5.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc2cc(C3CC3)ccc2c1 nan
CHEMBL3719587 134638 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 445 8 1 3 5.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc2cc(C3CC3)ccc2c1 nan
118727611 116994 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 9 1 2 6.3 CC(C)C[C@H](N)CCN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400203 116994 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 9 1 2 6.3 CC(C)C[C@H](N)CCN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
58466521 1044 3 None 29 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1016/j.bmcl.2015.02.038
7798 1044 3 None 29 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1016/j.bmcl.2015.02.038
CHEMBL3401461 1044 3 None 29 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1016/j.bmcl.2015.02.038
51348672 117185 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 471 10 1 4 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3401460 117185 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 471 10 1 4 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
118727621 117003 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 1 3 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(OC)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400212 117003 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 1 3 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(OC)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
162665770 181750 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 367 8 2 3 4.1 CC1CC(COc2ccc([C@H](CO)NC(=O)[C@@H](C)c3ccccc3)cc2)C1 10.1021/acs.jmedchem.0c01581
CHEMBL4784512 181750 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 367 8 2 3 4.1 CC1CC(COc2ccc([C@H](CO)NC(=O)[C@@H](C)c3ccccc3)cc2)C1 10.1021/acs.jmedchem.0c01581
162665770 181750 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 367 8 2 3 4.1 CC1CC(COc2ccc([C@H](CO)NC(=O)[C@@H](C)c3ccccc3)cc2)C1 10.1021/acs.jmedchem.0c01581
CHEMBL4784512 181750 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 367 8 2 3 4.1 CC1CC(COc2ccc([C@H](CO)NC(=O)[C@@H](C)c3ccccc3)cc2)C1 10.1021/acs.jmedchem.0c01581
162674462 182740 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 438 10 2 3 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4797419 182740 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 438 10 2 3 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
155524122 175787 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 427 8 1 3 5.6 CCCc1ccc(-c2ccc(N(CC(C)(C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4453972 175787 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 427 8 1 3 5.6 CCCc1ccc(-c2ccc(N(CC(C)(C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4595791 175787 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 427 8 1 3 5.6 CCCc1ccc(-c2ccc(N(CC(C)(C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
162674462 182740 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 438 10 2 3 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4797419 182740 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 438 10 2 3 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
155524122 175787 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 427 8 1 3 5.6 CCCc1ccc(-c2ccc(N(CC(C)(C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4453972 175787 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 427 8 1 3 5.6 CCCc1ccc(-c2ccc(N(CC(C)(C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4595791 175787 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 427 8 1 3 5.6 CCCc1ccc(-c2ccc(N(CC(C)(C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
118727687 117068 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 427 8 2 3 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(N)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400278 117068 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 427 8 2 3 5.4 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(N)cc2)cc1 10.1016/j.bmcl.2015.02.038
118727662 117043 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 1 3 5.9 COc1ccccc1-c1ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]2C[C@H]2c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400253 117043 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 1 3 5.9 COc1ccccc1-c1ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]2C[C@H]2c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
168274022 189633 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 419 9 1 5 4.8 Cc1noc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)n1 10.1021/acs.jmedchem.1c01075
CHEMBL5175026 189633 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 419 9 1 5 4.8 Cc1noc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)n1 10.1021/acs.jmedchem.1c01075
168274022 189633 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 419 9 1 5 4.8 Cc1noc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)n1 10.1021/acs.jmedchem.1c01075
CHEMBL5175026 189633 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 419 9 1 5 4.8 Cc1noc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)n1 10.1021/acs.jmedchem.1c01075
118727660 117041 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 1 3 5.9 COc1ccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400251 117041 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 442 9 1 3 5.9 COc1ccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
168279556 190255 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 486 10 1 5 6.2 C[C@H](C(=O)N[C@@H](Cn1cc(C2CCCCC2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5184589 190255 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 486 10 1 5 6.2 C[C@H](C(=O)N[C@@H](Cn1cc(C2CCCCC2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
162661550 180811 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 465 12 3 4 4.3 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CCCN2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4763624 180811 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 465 12 3 4 4.3 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CCCN2)cc1 10.1021/acs.jmedchem.0c01581
162661550 180811 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 465 12 3 4 4.3 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CCCN2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4763624 180811 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 465 12 3 4 4.3 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CCCN2)cc1 10.1021/acs.jmedchem.0c01581
168279556 190255 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 486 10 1 5 6.2 C[C@H](C(=O)N[C@@H](Cn1cc(C2CCCCC2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5184589 190255 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 486 10 1 5 6.2 C[C@H](C(=O)N[C@@H](Cn1cc(C2CCCCC2)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
118727674 117055 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 480 8 1 2 6.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400265 117055 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 480 8 1 2 6.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2015.02.038
118727659 117040 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 8 1 2 6.2 Cc1ccccc1-c1ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]2C[C@H]2c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400250 117040 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 8 1 2 6.2 Cc1ccccc1-c1ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]2C[C@H]2c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
134130396 141676 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 369 11 2 3 4.3 CCCC(C)COc1ccc([C@H](CO)NC(=O)CCc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884316 141676 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 369 11 2 3 4.3 CCCC(C)COc1ccc([C@H](CO)NC(=O)CCc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
134130396 141676 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 369 11 2 3 4.3 CCCC(C)COc1ccc([C@H](CO)NC(=O)CCc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884316 141676 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 369 11 2 3 4.3 CCCC(C)COc1ccc([C@H](CO)NC(=O)CCc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
118727680 117061 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 456 10 1 3 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(COC)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400271 117061 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 456 10 1 3 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(COC)cc2)cc1 10.1016/j.bmcl.2015.02.038
168282137 190206 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 2 4 4.2 C[C@H](C(=O)N[C@@H](Cc1c[nH]nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5183838 190206 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 2 4 4.2 C[C@H](C(=O)N[C@@H](Cc1c[nH]nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168282137 190206 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 2 4 4.2 C[C@H](C(=O)N[C@@H](Cc1c[nH]nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5183838 190206 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 2 4 4.2 C[C@H](C(=O)N[C@@H](Cc1c[nH]nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
118727640 117021 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 418 8 1 3 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccs1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400231 117021 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 418 8 1 3 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccs1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727657 117038 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 8 1 2 6.2 Cc1ccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400248 117038 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 8 1 2 6.2 Cc1ccc(-c2ccc(N(C[C@@H](N)CC(C)C)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
118727645 117026 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 447 8 1 4 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1nc(C)c(C)s1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400236 117026 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 447 8 1 4 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1nc(C)c(C)s1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
168277341 189694 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 10 1 5 5.2 CC(C)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5175963 189694 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 10 1 5 5.2 CC(C)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
168277341 189694 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 10 1 5 5.2 CC(C)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5175963 189694 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 446 10 1 5 5.2 CC(C)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
162651966 179601 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 446 10 3 4 3.9 C[C@H](C(=O)N[C@@H](C(=O)NCc1ncc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4749480 179601 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 446 10 3 4 3.9 C[C@H](C(=O)N[C@@H](C(=O)NCc1ncc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162651966 179601 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 446 10 3 4 3.9 C[C@H](C(=O)N[C@@H](C(=O)NCc1ncc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4749480 179601 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 446 10 3 4 3.9 C[C@H](C(=O)N[C@@H](C(=O)NCc1ncc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
134131577 141696 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 397 10 1 4 4.4 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(C)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884700 141696 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 397 10 1 4 4.4 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(C)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
162677103 182935 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 419 9 1 5 4.8 Cc1nnc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
CHEMBL4799883 182935 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 419 9 1 5 4.8 Cc1nnc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
168275929 189976 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 1 5 4.2 C[C@H](C(=O)N[C@@H](Cc1cnn(C)n1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5180324 189976 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 1 5 4.2 C[C@H](C(=O)N[C@@H](Cc1cnn(C)n1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
134131577 141696 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 397 10 1 4 4.4 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(C)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884700 141696 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 397 10 1 4 4.4 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(C)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
162677103 182935 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 419 9 1 5 4.8 Cc1nnc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
CHEMBL4799883 182935 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 419 9 1 5 4.8 Cc1nnc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
168275929 189976 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 1 5 4.2 C[C@H](C(=O)N[C@@H](Cc1cnn(C)n1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5180324 189976 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 1 5 4.2 C[C@H](C(=O)N[C@@H](Cc1cnn(C)n1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
162658387 180444 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.6 CCCCC(C)Oc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4759345 180444 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.6 CCCCC(C)Oc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162643654 181078 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 341 9 2 3 3.8 CCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4776381 181078 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 341 9 2 3 3.8 CCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162658387 180444 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.6 CCCCC(C)Oc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4759345 180444 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 369 10 2 3 4.6 CCCCC(C)Oc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162643654 181078 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 341 9 2 3 3.8 CCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4776381 181078 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 341 9 2 3 3.8 CCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
118727669 117050 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 446 8 1 2 6.5 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2Cl)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400260 117050 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 446 8 1 2 6.5 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2Cl)cc1 10.1016/j.bmcl.2015.02.038
168287256 191203 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 475 10 1 6 3.8 C[C@H](C(=O)N[C@@H](Cn1cc(C(=O)N(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5198398 191203 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 475 10 1 6 3.8 C[C@H](C(=O)N[C@@H](Cn1cc(C(=O)N(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168287256 191203 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 475 10 1 6 3.8 C[C@H](C(=O)N[C@@H](Cn1cc(C(=O)N(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5198398 191203 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 475 10 1 6 3.8 C[C@H](C(=O)N[C@@H](Cn1cc(C(=O)N(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
134130479 141782 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2cccc(F)c2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3885494 141782 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2cccc(F)c2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
51354469 117485 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 397 10 2 3 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(C)(C)O)cc1 nan
CHEMBL3403779 117485 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 397 10 2 3 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(C)(C)O)cc1 nan
51355032 117487 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 396 11 1 3 5.0 CCCC(C)COc1ccc([C@H](CN(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3403781 117487 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 396 11 1 3 5.0 CCCC(C)COc1ccc([C@H](CN(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354470 117499 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 354 9 2 3 4.0 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3403793 117499 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 354 9 2 3 4.0 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355031 133172 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 453 13 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715029 133172 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 453 13 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354737 133402 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 422 13 2 3 5.5 CCCC(C)COc1ccc([C@H](CNCC2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715862 133402 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 422 13 2 3 5.5 CCCC(C)COc1ccc([C@H](CNCC2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354739 133460 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)CC(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716058 133460 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)CC(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355033 133468 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 467 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CCC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716078 133468 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 467 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CCC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355030 133558 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 467 13 3 4 4.6 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)C(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716360 133558 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 467 13 3 4 4.6 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)C(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354738 133827 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717315 133827 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355028 134057 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)[C@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3718100 134057 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)[C@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354736 134126 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 465 13 3 4 5.3 CCCC(C)COc1ccc([C@H](CNCC2(N)CCCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3718302 134126 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 465 13 3 4 5.3 CCCC(C)COc1ccc([C@H](CNCC2(N)CCCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355029 134182 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 439 12 3 4 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3718503 134182 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 439 12 3 4 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354469 117485 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 397 10 2 3 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(C)(C)O)cc1 nan
CHEMBL3403779 117485 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 397 10 2 3 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(C)(C)O)cc1 nan
51355032 117487 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 396 11 1 3 5.0 CCCC(C)COc1ccc([C@H](CN(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3403781 117487 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 396 11 1 3 5.0 CCCC(C)COc1ccc([C@H](CN(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354470 117499 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 354 9 2 3 4.0 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3403793 117499 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 354 9 2 3 4.0 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355031 133172 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 453 13 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715029 133172 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 453 13 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354737 133402 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 422 13 2 3 5.5 CCCC(C)COc1ccc([C@H](CNCC2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715862 133402 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 422 13 2 3 5.5 CCCC(C)COc1ccc([C@H](CNCC2CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354739 133460 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)CC(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716058 133460 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)CC(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355033 133468 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 467 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CCC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716078 133468 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 467 14 3 4 4.7 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)CCC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355030 133558 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 467 13 3 4 4.6 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)C(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3716360 133558 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 467 13 3 4 4.6 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)C(C)C)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354738 133827 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3717315 133827 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](N)[C@@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355028 134057 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)[C@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3718100 134057 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 481 14 3 4 5.0 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)[C@H](C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354736 134126 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 465 13 3 4 5.3 CCCC(C)COc1ccc([C@H](CNCC2(N)CCCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3718302 134126 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 465 13 3 4 5.3 CCCC(C)COc1ccc([C@H](CNCC2(N)CCCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51355029 134182 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 439 12 3 4 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3718503 134182 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 439 12 3 4 3.9 CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
168293070 191494 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 461 10 2 6 3.5 CNC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5203114 191494 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 461 10 2 6 3.5 CNC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
134130479 141782 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2cccc(F)c2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3885494 141782 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2cccc(F)c2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
162656522 180333 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 424 12 2 3 5.0 CCCNC(=O)[C@H](NC(=O)[C@@H](C)c1ccccc1)c1ccc(OCC(C)CCC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4758007 180333 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 424 12 2 3 5.0 CCCNC(=O)[C@H](NC(=O)[C@@H](C)c1ccccc1)c1ccc(OCC(C)CCC)cc1 10.1021/acs.jmedchem.0c01581
155524318 175853 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 413 8 1 3 5.2 CCCc1ccc(-c2ccc(N(C[C@H](C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4454531 175853 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 413 8 1 3 5.2 CCCc1ccc(-c2ccc(N(C[C@H](C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4596277 175853 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 413 8 1 3 5.2 CCCc1ccc(-c2ccc(N(C[C@H](C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
162656522 180333 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 424 12 2 3 5.0 CCCNC(=O)[C@H](NC(=O)[C@@H](C)c1ccccc1)c1ccc(OCC(C)CCC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4758007 180333 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 424 12 2 3 5.0 CCCNC(=O)[C@H](NC(=O)[C@@H](C)c1ccccc1)c1ccc(OCC(C)CCC)cc1 10.1021/acs.jmedchem.0c01581
155524318 175853 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 413 8 1 3 5.2 CCCc1ccc(-c2ccc(N(C[C@H](C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4454531 175853 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 413 8 1 3 5.2 CCCc1ccc(-c2ccc(N(C[C@H](C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4596277 175853 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 413 8 1 3 5.2 CCCc1ccc(-c2ccc(N(C[C@H](C)N)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
118727604 116987 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 432 7 1 2 6.2 N[C@H](CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1)c1ccccc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400196 116987 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 432 7 1 2 6.2 N[C@H](CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1)c1ccccc1 10.1016/j.bmcl.2015.02.038
118727614 116997 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 10 1 2 6.1 CCC(C)CNCCN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400206 116997 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 10 1 2 6.1 CCC(C)CNCCN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
168293070 191494 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 461 10 2 6 3.5 CNC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5203114 191494 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 461 10 2 6 3.5 CNC(=O)c1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
168294517 191622 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 448 11 1 6 4.5 CCOc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5205098 191622 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 448 11 1 6 4.5 CCOc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
168294517 191622 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 448 11 1 6 4.5 CCOc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5205098 191622 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 448 11 1 6 4.5 CCOc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
118730013 117496 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 299 6 2 3 2.6 COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403790 117496 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 299 6 2 3 2.6 COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
58466401 117486 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL3403780 117486 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL3884102 117486 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
58466401 117486 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3403780 117486 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884102 117486 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
58466401 117486 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3403780 117486 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884102 117486 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
162661210 180884 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 426 12 3 4 3.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCO)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4764623 180884 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 426 12 3 4 3.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCO)cc1 10.1021/acs.jmedchem.0c01581
162661210 180884 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 426 12 3 4 3.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCO)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4764623 180884 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 426 12 3 4 3.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCO)cc1 10.1021/acs.jmedchem.0c01581
118727617 117000 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 446 8 1 2 6.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(Cl)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400209 117000 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 446 8 1 2 6.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(Cl)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727671 117052 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 440 9 1 2 6.4 CCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400262 117052 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 440 9 1 2 6.4 CCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
10031 3347 5 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.1c01075
134813902 3347 5 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.1c01075
CHEMBL4595209 3347 5 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.1c01075
10031 3347 5 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.1c01075
134813902 3347 5 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.1c01075
CHEMBL4595209 3347 5 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.1c01075
118727641 117022 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 418 8 1 3 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccsc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400232 117022 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 418 8 1 3 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccsc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727667 117048 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 437 8 1 3 5.7 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400258 117048 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 437 8 1 3 5.7 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2015.02.038
162645574 179115 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 445 10 3 3 4.5 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4743847 179115 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 445 10 3 3 4.5 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
168271605 189641 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 9 1 5 4.7 Cc1nnn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)c1C 10.1021/acs.jmedchem.1c01075
CHEMBL5175154 189641 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 9 1 5 4.7 Cc1nnn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)c1C 10.1021/acs.jmedchem.1c01075
162645574 179115 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 445 10 3 3 4.5 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4743847 179115 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 445 10 3 3 4.5 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
168271605 189641 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 9 1 5 4.7 Cc1nnn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)c1C 10.1021/acs.jmedchem.1c01075
CHEMBL5175154 189641 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 9 1 5 4.7 Cc1nnn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)c1C 10.1021/acs.jmedchem.1c01075
10031 3347 5 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.0c01581
134813902 3347 5 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.0c01581
CHEMBL4595209 3347 5 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.0c01581
118730009 117492 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 373 9 2 3 4.2 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)c(F)c1 10.1016/j.bmcl.2015.01.036
CHEMBL3403786 117492 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 373 9 2 3 4.2 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)c(F)c1 10.1016/j.bmcl.2015.01.036
118727690 117071 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 469 10 1 3 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(CN(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400281 117071 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 469 10 1 3 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(CN(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
162671884 182253 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 466 12 2 4 4.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CCCO2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4791411 182253 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 466 12 2 4 4.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CCCO2)cc1 10.1021/acs.jmedchem.0c01581
162676440 182890 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 454 12 2 5 3.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC(=O)OC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4799403 182890 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 454 12 2 5 3.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC(=O)OC)cc1 10.1021/acs.jmedchem.0c01581
162665250 181546 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 371 11 2 4 3.4 COCCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4782249 181546 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 371 11 2 4 3.4 COCCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162665250 181546 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 371 11 2 4 3.4 COCCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4782249 181546 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 371 11 2 4 3.4 COCCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162671884 182253 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 466 12 2 4 4.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CCCO2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4791411 182253 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 466 12 2 4 4.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC2CCCO2)cc1 10.1021/acs.jmedchem.0c01581
162676440 182890 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 454 12 2 5 3.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC(=O)OC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4799403 182890 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 454 12 2 5 3.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCC(=O)OC)cc1 10.1021/acs.jmedchem.0c01581
10031 3347 5 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.0c01581
134813902 3347 5 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.0c01581
CHEMBL4595209 3347 5 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.0c01581
162660648 180687 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 391 8 1 5 4.3 C[C@H](C(=O)N[C@H](c1ccc(OCC2CCC2)cc1)c1nnco1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4762163 180687 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 391 8 1 5 4.3 C[C@H](C(=O)N[C@H](c1ccc(OCC2CCC2)cc1)c1nnco1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162660648 180687 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 391 8 1 5 4.3 C[C@H](C(=O)N[C@H](c1ccc(OCC2CCC2)cc1)c1nnco1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4762163 180687 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 391 8 1 5 4.3 C[C@H](C(=O)N[C@H](c1ccc(OCC2CCC2)cc1)c1nnco1)c1ccccc1 10.1021/acs.jmedchem.0c01581
168274798 189488 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 450 12 2 6 4.2 CCC[C@H](C)COc1ccc([C@H](Cn2cc(CO)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL5172809 189488 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 450 12 2 6 4.2 CCC[C@H](C)COc1ccc([C@H](Cn2cc(CO)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
69925894 117481 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 355 10 2 3 3.9 CCCC(C)COc1ccc([C@H](CO)NC(=O)Cc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3403775 117481 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 355 10 2 3 3.9 CCCC(C)COc1ccc([C@H](CO)NC(=O)Cc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
69925894 117481 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 355 10 2 3 3.9 CCCC(C)COc1ccc([C@H](CO)NC(=O)Cc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3403775 117481 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 355 10 2 3 3.9 CCCC(C)COc1ccc([C@H](CO)NC(=O)Cc2ccccc2)cc1 10.1016/j.bmc.2016.11.058
162654926 179985 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 10 2 6 3.8 Cc1nnc(CNC(=O)[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
CHEMBL4754124 179985 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 10 2 6 3.8 Cc1nnc(CNC(=O)[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
162654926 179985 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 10 2 6 3.8 Cc1nnc(CNC(=O)[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
CHEMBL4754124 179985 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 10 2 6 3.8 Cc1nnc(CNC(=O)[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
118727613 116996 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 10 1 2 6.1 CC(C)CCNCCN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400205 116996 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 426 10 1 2 6.1 CC(C)CCNCCN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118730166 117539 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 454 9 1 2 6.0 CC[C@H](C)[C@@H](CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1)NC(C)=O 10.1016/j.bmcl.2015.02.038
CHEMBL3404053 117539 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 454 9 1 2 6.0 CC[C@H](C)[C@@H](CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1)NC(C)=O 10.1016/j.bmcl.2015.02.038
58466521 1044 3 None 29 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human PPLS-HA-tagged-GPR88 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET based LANCE assayAgonist activity at human PPLS-HA-tagged-GPR88 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET based LANCE assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1016/j.bmc.2016.11.058
7798 1044 3 None 29 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human PPLS-HA-tagged-GPR88 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET based LANCE assayAgonist activity at human PPLS-HA-tagged-GPR88 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET based LANCE assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1016/j.bmc.2016.11.058
CHEMBL3401461 1044 3 None 29 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human PPLS-HA-tagged-GPR88 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET based LANCE assayAgonist activity at human PPLS-HA-tagged-GPR88 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET based LANCE assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1016/j.bmc.2016.11.058
118729997 117475 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 341 8 2 3 3.7 CC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403766 117475 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 341 8 2 3 3.7 CC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
168269611 189410 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 2 4 4.5 Cc1nnc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)[nH]1 10.1021/acs.jmedchem.1c01075
CHEMBL5171511 189410 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 2 4 4.5 Cc1nnc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)[nH]1 10.1021/acs.jmedchem.1c01075
155530523 175735 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 399 8 1 3 4.8 CCCc1ccc(-c2ccc(N(CCN)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4464331 175735 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 399 8 1 3 4.8 CCCc1ccc(-c2ccc(N(CCN)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4595321 175735 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 399 8 1 3 4.8 CCCc1ccc(-c2ccc(N(CCN)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
155538984 175920 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 489 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)Cc3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4513479 175920 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 489 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)Cc3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4596842 175920 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 489 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)Cc3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
168269611 189410 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 2 4 4.5 Cc1nnc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)[nH]1 10.1021/acs.jmedchem.1c01075
CHEMBL5171511 189410 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 2 4 4.5 Cc1nnc(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)[nH]1 10.1021/acs.jmedchem.1c01075
155530523 175735 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 399 8 1 3 4.8 CCCc1ccc(-c2ccc(N(CCN)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4464331 175735 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 399 8 1 3 4.8 CCCc1ccc(-c2ccc(N(CCN)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4595321 175735 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 399 8 1 3 4.8 CCCc1ccc(-c2ccc(N(CCN)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
155538984 175920 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 489 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)Cc3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4513479 175920 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 489 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)Cc3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4596842 175920 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 489 10 1 3 6.4 CCCc1ccc(-c2ccc(N(C[C@@H](N)Cc3ccccc3)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
162652578 179862 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 539 13 2 5 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN(C)C(=O)OC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4752733 179862 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 539 13 2 5 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN(C)C(=O)OC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
162644183 181207 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 447 10 3 5 3.3 C[C@H](C(=O)N[C@@H](C(=O)NCc1nnc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4778038 181207 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 447 10 3 5 3.3 C[C@H](C(=O)N[C@@H](C(=O)NCc1nnc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162644183 181207 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 447 10 3 5 3.3 C[C@H](C(=O)N[C@@H](C(=O)NCc1nnc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4778038 181207 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 447 10 3 5 3.3 C[C@H](C(=O)N[C@@H](C(=O)NCc1nnc[nH]1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162652578 179862 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 539 13 2 5 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN(C)C(=O)OC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4752733 179862 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 539 13 2 5 5.4 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN(C)C(=O)OC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
162664171 181576 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 421 10 1 5 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)c2nnc(C)o2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4782571 181576 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 421 10 1 5 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)c2nnc(C)o2)cc1 10.1021/acs.jmedchem.0c01581
162664171 181576 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 421 10 1 5 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)c2nnc(C)o2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4782571 181576 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 421 10 1 5 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)c2nnc(C)o2)cc1 10.1021/acs.jmedchem.0c01581
162664171 181576 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 421 10 1 5 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)c2nnc(C)o2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL4782571 181576 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 421 10 1 5 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)c2nnc(C)o2)cc1 10.1021/acs.jmedchem.1c01075
10031 3347 5 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
134813902 3347 5 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
CHEMBL4595209 3347 5 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at GPR88 in wild type mouse striatal membranes assessed as increase in [35S]-GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 10.1021/acs.jmedchem.8b00566
162663886 181413 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 440 13 2 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCOC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4780568 181413 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 440 13 2 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCOC)cc1 10.1021/acs.jmedchem.0c01581
162668147 181958 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 407 10 1 5 4.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)c2nnco2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4787512 181958 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 407 10 1 5 4.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)c2nnco2)cc1 10.1021/acs.jmedchem.0c01581
162663886 181413 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 440 13 2 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCOC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4780568 181413 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 440 13 2 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCOC)cc1 10.1021/acs.jmedchem.0c01581
162668147 181958 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 407 10 1 5 4.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)c2nnco2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4787512 181958 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 407 10 1 5 4.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)c2nnco2)cc1 10.1021/acs.jmedchem.0c01581
134130337 141582 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 397 10 1 4 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3883403 141582 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 397 10 1 4 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
134130337 141582 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 397 10 1 4 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3883403 141582 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 397 10 1 4 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
58466401 117486 0 None 6 2 Human 7.3 pEC50 = 7.3 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3403780 117486 0 None 6 2 Human 7.3 pEC50 = 7.3 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3884102 117486 0 None 6 2 Human 7.3 pEC50 = 7.3 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
58466401 117486 0 None 6 2 Human 7.3 pEC50 = 7.3 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3403780 117486 0 None 6 2 Human 7.3 pEC50 = 7.3 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3884102 117486 0 None 6 2 Human 7.3 pEC50 = 7.3 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
162651096 179643 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 446 10 2 4 4.7 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccco1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4750015 179643 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 446 10 2 4 4.7 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccco1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162653235 179857 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 405 8 1 5 4.6 Cc1nnc([C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
CHEMBL4752677 179857 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 405 8 1 5 4.6 Cc1nnc([C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
162644207 181221 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 439 13 3 4 3.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCNC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4778149 181221 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 439 13 3 4 3.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCNC)cc1 10.1021/acs.jmedchem.0c01581
162660875 181292 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 453 13 2 4 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4779002 181292 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 453 13 2 4 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN(C)C)cc1 10.1021/acs.jmedchem.0c01581
162644207 181221 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 439 13 3 4 3.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCNC)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4778149 181221 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 439 13 3 4 3.8 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCNC)cc1 10.1021/acs.jmedchem.0c01581
162660875 181292 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 453 13 2 4 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4779002 181292 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 453 13 2 4 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN(C)C)cc1 10.1021/acs.jmedchem.0c01581
162651096 179643 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 446 10 2 4 4.7 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccco1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4750015 179643 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 446 10 2 4 4.7 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccco1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162653235 179857 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 405 8 1 5 4.6 Cc1nnc([C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
CHEMBL4752677 179857 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 405 8 1 5 4.6 Cc1nnc([C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
118727689 117070 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 469 9 2 3 5.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(NC(C)=O)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400280 117070 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 469 9 2 3 5.8 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(NC(C)=O)cc2)cc1 10.1016/j.bmcl.2015.02.038
58466521 1044 3 None 29 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
7798 1044 3 None 29 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
CHEMBL3401461 1044 3 None 29 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.8b00566
118727623 117005 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400214 117005 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
162651638 179587 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 327 8 2 3 3.4 CCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4749174 179587 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 327 8 2 3 3.4 CCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162662433 181382 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 464 11 2 3 5.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4780227 181382 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 464 11 2 3 5.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.0c01581
162651638 179587 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 327 8 2 3 3.4 CCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4749174 179587 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 327 8 2 3 3.4 CCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162662433 181382 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 464 11 2 3 5.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4780227 181382 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 464 11 2 3 5.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.0c01581
118730007 117490 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 422 11 1 3 5.6 CCCC(C)COc1ccc([C@H](CN2CCCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403784 117490 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 422 11 1 3 5.6 CCCC(C)COc1ccc([C@H](CN2CCCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
162660464 180754 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 382 10 2 3 3.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(N)=O)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4763017 180754 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 382 10 2 3 3.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(N)=O)cc1 10.1021/acs.jmedchem.0c01581
162660464 180754 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 382 10 2 3 3.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(N)=O)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4763017 180754 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 382 10 2 3 3.9 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(N)=O)cc1 10.1021/acs.jmedchem.0c01581
162665470 182206 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4784623 182206 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4790638 182206 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
118727642 117023 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 402 8 1 3 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccoc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400233 117023 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 402 8 1 3 5.5 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccoc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
134129964 141742 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 411 11 1 4 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](CC)c2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3885146 141742 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 411 11 1 4 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](CC)c2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
134130956 141702 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(F)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884736 141702 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(F)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
162677099 182933 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2cccnc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4799879 182933 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2cccnc2)cc1 10.1021/acs.jmedchem.0c01581
134129964 141742 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 411 11 1 4 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](CC)c2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3885146 141742 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 411 11 1 4 5.0 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](CC)c2ccccc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
162667290 181962 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 357 10 2 4 3.1 COCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4787574 181962 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 357 10 2 4 3.1 COCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162667290 181962 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 357 10 2 4 3.1 COCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4787574 181962 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 357 10 2 4 3.1 COCCCOc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
134130956 141702 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(F)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884736 141702 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(F)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
162677099 182933 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2cccnc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4799879 182933 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2cccnc2)cc1 10.1021/acs.jmedchem.0c01581
162665470 182206 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4784623 182206 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4790638 182206 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
162665470 182206 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL4784623 182206 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL4790638 182206 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
118727615 116998 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 452 9 1 2 6.7 O=C([C@@H]1C[C@H]1c1ccccc1)N(CCNCC1CCCCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400207 116998 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 452 9 1 2 6.7 O=C([C@@H]1C[C@H]1c1ccccc1)N(CCNCC1CCCCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
168283746 190222 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 420 11 1 5 4.8 CCCC(C)COc1ccc([C@H](Cn2ccnn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL5184001 190222 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 420 11 1 5 4.8 CCCC(C)COc1ccc([C@H](Cn2ccnn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
168283746 190222 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 420 11 1 5 4.8 CCCC(C)COc1ccc([C@H](Cn2ccnn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL5184001 190222 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 420 11 1 5 4.8 CCCC(C)COc1ccc([C@H](Cn2ccnn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
118727622 117004 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400213 117004 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118729996 117473 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 331 5 2 2 3.8 O=C(NC(CO)c1ccc2ccccc2c1)[C@@H]1C[C@H]1c1ccccc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403764 117473 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 331 5 2 2 3.8 O=C(NC(CO)c1ccc2ccccc2c1)[C@@H]1C[C@H]1c1ccccc1 10.1016/j.bmcl.2015.01.036
168292918 191491 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 460 9 1 5 5.4 C[C@H](C(=O)N[C@@H](Cn1cc(C(C)(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5203098 191491 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 460 9 1 5 5.4 C[C@H](C(=O)N[C@@H](Cn1cc(C(C)(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168292918 191491 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 460 9 1 5 5.4 C[C@H](C(=O)N[C@@H](Cn1cc(C(C)(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5203098 191491 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 460 9 1 5 5.4 C[C@H](C(=O)N[C@@H](Cn1cc(C(C)(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
118727672 117053 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 454 10 1 2 6.8 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400263 117053 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 454 10 1 2 6.8 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
134130466 141773 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 410 10 1 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)N(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL3885410 141773 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 410 10 1 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)N(C)C)cc1 10.1021/acs.jmedchem.0c01581
134130466 141773 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 410 10 1 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)N(C)C)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3885410 141773 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 410 10 1 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)N(C)C)cc1 10.1016/j.bmc.2016.11.058
134130466 141773 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 410 10 1 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)N(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL3885410 141773 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 410 10 1 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)N(C)C)cc1 10.1021/acs.jmedchem.0c01581
162646652 178892 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccccn2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4740926 178892 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccccn2)cc1 10.1021/acs.jmedchem.0c01581
134130466 141773 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 410 10 1 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)N(C)C)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3885410 141773 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 410 10 1 3 4.6 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)N(C)C)cc1 10.1016/j.bmc.2016.11.058
162646652 178892 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccccn2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4740926 178892 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccccn2)cc1 10.1021/acs.jmedchem.0c01581
51348522 117474 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 nan
CHEMBL3403765 117474 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 nan
67430825 133116 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 455 10 1 5 4.4 CC[C@H](C)COc1ccc([C@H](CN2CCN(C)CC2)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3714859 133116 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 455 10 1 5 4.4 CC[C@H](C)COc1ccc([C@H](CN2CCN(C)CC2)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
58459797 133157 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 411 11 2 4 4.5 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2ccccc2)c(OC)c1 nan
CHEMBL3714993 133157 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 411 11 2 4 4.5 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2ccccc2)c(OC)c1 nan
51348523 133212 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 372 9 2 4 4.1 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3715159 133212 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 372 9 2 4 4.1 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
51348668 133262 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 407 7 2 4 4.7 COc1cc(-c2ccc(C)cc2)ccc1[C@H](CO)NC(=O)[C@H]1C[C@@H]1c1cccs1 nan
CHEMBL3715370 133262 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 407 7 2 4 4.7 COc1cc(-c2ccc(C)cc2)ccc1[C@H](CO)NC(=O)[C@H]1C[C@@H]1c1cccs1 nan
51348520 133405 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 401 10 2 4 4.8 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
CHEMBL3715868 133405 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 401 10 2 4 4.8 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
51348524 133513 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 387 9 2 4 4.4 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
CHEMBL3716229 133513 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 387 9 2 4 4.4 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
51348521 133554 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 387 10 2 4 4.5 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3716350 133554 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 387 10 2 4 4.5 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
51348525 133690 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 469 11 1 5 4.8 CCCC(C)COc1ccc([C@H](CN2CCN(C)CC2)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3716842 133690 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 469 11 1 5 4.8 CCCC(C)COc1ccc([C@H](CN2CCN(C)CC2)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
58459803 133958 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 386 9 2 4 4.4 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
CHEMBL3717751 133958 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 386 9 2 4 4.4 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
51348365 133992 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 391 7 2 3 4.9 CCc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 nan
CHEMBL3717862 133992 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 391 7 2 3 4.9 CCc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 nan
51348223 134156 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 421 8 2 4 4.9 CCc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)c(OC)c2)cc1 nan
CHEMBL3718412 134156 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 421 8 2 4 4.9 CCc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)c(OC)c2)cc1 nan
51348667 134278 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 401 10 2 4 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
CHEMBL3718798 134278 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 401 10 2 4 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
58459793 134294 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 383 7 2 4 3.9 CCCC#Cc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(OC)c1 nan
CHEMBL3718836 134294 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 383 7 2 4 3.9 CCCC#Cc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(OC)c1 nan
58459808 134383 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 385 7 1 2 5.7 CC[C@H](NC(=O)[C@H]1C[C@@H]1c1ccccc1)c1ccc(-c2ccc(OC)cc2)cc1 nan
CHEMBL3719161 134383 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 385 7 1 2 5.7 CC[C@H](NC(=O)[C@H]1C[C@@H]1c1ccccc1)c1ccc(-c2ccc(OC)cc2)cc1 nan
51348522 117474 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 nan
CHEMBL3403765 117474 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 nan
67430825 133116 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 455 10 1 5 4.4 CC[C@H](C)COc1ccc([C@H](CN2CCN(C)CC2)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3714859 133116 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 455 10 1 5 4.4 CC[C@H](C)COc1ccc([C@H](CN2CCN(C)CC2)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
58459797 133157 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 411 11 2 4 4.5 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2ccccc2)c(OC)c1 nan
CHEMBL3714993 133157 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 411 11 2 4 4.5 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2ccccc2)c(OC)c1 nan
51348523 133212 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 372 9 2 4 4.1 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3715159 133212 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 372 9 2 4 4.1 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
51348668 133262 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 407 7 2 4 4.7 COc1cc(-c2ccc(C)cc2)ccc1[C@H](CO)NC(=O)[C@H]1C[C@@H]1c1cccs1 nan
CHEMBL3715370 133262 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 407 7 2 4 4.7 COc1cc(-c2ccc(C)cc2)ccc1[C@H](CO)NC(=O)[C@H]1C[C@@H]1c1cccs1 nan
51348520 133405 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 401 10 2 4 4.8 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
CHEMBL3715868 133405 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 401 10 2 4 4.8 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
51348524 133513 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 387 9 2 4 4.4 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
CHEMBL3716229 133513 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 387 9 2 4 4.4 CC[C@H](C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
51348521 133554 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 387 10 2 4 4.5 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3716350 133554 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 387 10 2 4 4.5 CCC(CC)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
51348525 133690 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 469 11 1 5 4.8 CCCC(C)COc1ccc([C@H](CN2CCN(C)CC2)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3716842 133690 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 469 11 1 5 4.8 CCCC(C)COc1ccc([C@H](CN2CCN(C)CC2)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
58459803 133958 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 386 9 2 4 4.4 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
CHEMBL3717751 133958 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 386 9 2 4 4.4 CC[C@H](C)COc1ccc([C@H](CN)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
51348365 133992 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 391 7 2 3 4.9 CCc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 nan
CHEMBL3717862 133992 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 391 7 2 3 4.9 CCc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 nan
51348223 134156 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 421 8 2 4 4.9 CCc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)c(OC)c2)cc1 nan
CHEMBL3718412 134156 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 421 8 2 4 4.9 CCc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)c(OC)c2)cc1 nan
51348667 134278 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 401 10 2 4 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
CHEMBL3718798 134278 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 401 10 2 4 4.8 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(C)c1 nan
58459793 134294 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 383 7 2 4 3.9 CCCC#Cc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(OC)c1 nan
CHEMBL3718836 134294 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 383 7 2 4 3.9 CCCC#Cc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)c(OC)c1 nan
58459808 134383 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 385 7 1 2 5.7 CC[C@H](NC(=O)[C@H]1C[C@@H]1c1ccccc1)c1ccc(-c2ccc(OC)cc2)cc1 nan
CHEMBL3719161 134383 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 385 7 1 2 5.7 CC[C@H](NC(=O)[C@H]1C[C@@H]1c1ccccc1)c1ccc(-c2ccc(OC)cc2)cc1 nan
118727648 117029 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400239 117029 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2015.02.038
155561860 175910 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 457 10 1 4 5.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4583504 175910 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 457 10 1 4 5.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4596729 175910 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 457 10 1 4 5.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
155561860 175910 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 457 10 1 4 5.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4583504 175910 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 457 10 1 4 5.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4596729 175910 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 457 10 1 4 5.2 CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1 10.1021/acs.jmedchem.8b00566
162652475 179860 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 339 8 2 3 3.4 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4752713 179860 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 339 8 2 3 3.4 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162652475 179860 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 339 8 2 3 3.4 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4752713 179860 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 339 8 2 3 3.4 C[C@H](C(=O)N[C@@H](CO)c1ccc(OCC2CC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
118727668 117049 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 446 8 1 2 6.5 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400259 117049 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 446 8 1 2 6.5 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.02.038
118727691 117072 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 455 10 2 3 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(CNC)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400282 117072 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 455 10 2 3 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(CNC)cc2)cc1 10.1016/j.bmcl.2015.02.038
118727624 117006 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1F)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400215 117006 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1F)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
168275346 189635 0 None -549 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at wild type GPR88 expressed in C57BL/6J mouse striatal membrane assessed as [35S] GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at wild type GPR88 expressed in C57BL/6J mouse striatal membrane assessed as [35S] GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 477 12 2 6 4.1 CCC[C@H](C)COc1ccc([C@H](Cn2cc(C(=O)NC)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL5175064 189635 0 None -549 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at wild type GPR88 expressed in C57BL/6J mouse striatal membrane assessed as [35S] GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at wild type GPR88 expressed in C57BL/6J mouse striatal membrane assessed as [35S] GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 477 12 2 6 4.1 CCC[C@H](C)COc1ccc([C@H](Cn2cc(C(=O)NC)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
118727683 117064 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 484 10 1 4 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(CC(=O)OC)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400274 117064 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 484 10 1 4 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(CC(=O)OC)cc2)cc1 10.1016/j.bmcl.2015.02.038
118727666 117047 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 437 8 1 3 5.7 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(C#N)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400257 117047 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 437 8 1 3 5.7 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(C#N)cc2)cc1 10.1016/j.bmcl.2015.02.038
162663827 181363 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 461 10 2 5 4.4 Cc1cnc(CNC(=O)[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
CHEMBL4779964 181363 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 461 10 2 5 4.4 Cc1cnc(CNC(=O)[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
162663827 181363 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 461 10 2 5 4.4 Cc1cnc(CNC(=O)[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
CHEMBL4779964 181363 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 461 10 2 5 4.4 Cc1cnc(CNC(=O)[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)o1 10.1021/acs.jmedchem.0c01581
118730014 117497 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 359 8 2 4 3.7 CC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403791 117497 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 359 8 2 4 3.7 CC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 10.1016/j.bmcl.2015.01.036
162653251 183072 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4751633 183072 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4802826 183072 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
168281316 190215 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 461 11 1 6 4.2 C[C@H](C(=O)N[C@@H](Cn1cc(CN(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5183956 190215 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 461 11 1 6 4.2 C[C@H](C(=O)N[C@@H](Cn1cc(CN(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168281316 190215 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 461 11 1 6 4.2 C[C@H](C(=O)N[C@@H](Cn1cc(CN(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5183956 190215 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 461 11 1 6 4.2 C[C@H](C(=O)N[C@@H](Cn1cc(CN(C)C)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
162653251 183072 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4751633 183072 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4802826 183072 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 422 10 2 6 4.3 CC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
118727675 117056 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 470 10 1 3 6.7 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400266 117056 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 470 10 1 3 6.7 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
58466521 1044 3 None 29 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.0c01581
7798 1044 3 None 29 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.0c01581
CHEMBL3401461 1044 3 None 29 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.0c01581
118727631 117011 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 448 8 1 2 6.1 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)c(F)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400222 117011 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 448 8 1 2 6.1 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)c(F)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
162669578 182126 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 10 2 4 5.2 C[C@H](C(=O)N[C@@H](C(=O)NCc1cccs1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4789643 182126 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 10 2 4 5.2 C[C@H](C(=O)N[C@@H](C(=O)NCc1cccs1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162669578 182126 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 10 2 4 5.2 C[C@H](C(=O)N[C@@H](C(=O)NCc1cccs1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4789643 182126 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 462 10 2 4 5.2 C[C@H](C(=O)N[C@@H](C(=O)NCc1cccs1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
58466521 1044 3 None 29 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.0c01581
7798 1044 3 None 29 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.0c01581
CHEMBL3401461 1044 3 None 29 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.0c01581
58466521 1044 3 None 29 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR88 expressed in HEK293T cells assessed as reduction in cAMP production incubated for 15 mins measured after 1 hr by by FLIPR assayAgonist activity at human GPR88 expressed in HEK293T cells assessed as reduction in cAMP production incubated for 15 mins measured after 1 hr by by FLIPR assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.1c01075
7798 1044 3 None 29 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR88 expressed in HEK293T cells assessed as reduction in cAMP production incubated for 15 mins measured after 1 hr by by FLIPR assayAgonist activity at human GPR88 expressed in HEK293T cells assessed as reduction in cAMP production incubated for 15 mins measured after 1 hr by by FLIPR assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.1c01075
CHEMBL3401461 1044 3 None 29 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR88 expressed in HEK293T cells assessed as reduction in cAMP production incubated for 15 mins measured after 1 hr by by FLIPR assayAgonist activity at human GPR88 expressed in HEK293T cells assessed as reduction in cAMP production incubated for 15 mins measured after 1 hr by by FLIPR assay
ChEMBL 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 10.1021/acs.jmedchem.1c01075
118730002 117479 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 381 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403773 117479 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 381 10 2 3 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
118727643 117024 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 433 8 1 4 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1nc(C)cs1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400234 117024 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 433 8 1 4 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1nc(C)cs1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
162658645 183097 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4760182 183097 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4803101 183097 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
168270814 189446 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 10 1 6 3.9 C[C@H](C(=O)N[C@@H](Cn1cc(C=O)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5172064 189446 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 10 1 6 3.9 C[C@H](C(=O)N[C@@H](Cn1cc(C=O)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
58459796 134183 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 387 10 2 4 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3718508 134183 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 387 10 2 4 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
58459796 134183 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 387 10 2 4 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
CHEMBL3718508 134183 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 387 10 2 4 4.5 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@H]2C[C@@H]2c2cccs2)cc1 nan
162658645 183097 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4760182 183097 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4803101 183097 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
168270814 189446 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 10 1 6 3.9 C[C@H](C(=O)N[C@@H](Cn1cc(C=O)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5172064 189446 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 432 10 1 6 3.9 C[C@H](C(=O)N[C@@H](Cn1cc(C=O)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
162652798 179874 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 447 10 2 5 4.1 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccon1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4752868 179874 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 447 10 2 5 4.1 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccon1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
162652798 179874 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 447 10 2 5 4.1 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccon1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
CHEMBL4752868 179874 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 447 10 2 5 4.1 C[C@H](C(=O)N[C@@H](C(=O)NCc1ccon1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.0c01581
118727673 117054 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 468 8 1 2 7.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400264 117054 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 468 8 1 2 7.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
168274798 189488 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 450 12 2 6 4.2 CCC[C@H](C)COc1ccc([C@H](Cn2cc(CO)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL5172809 189488 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 450 12 2 6 4.2 CCC[C@H](C)COc1ccc([C@H](Cn2cc(CO)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
162665334 183138 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4783876 183138 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4803469 183138 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
118727629 117009 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 448 8 1 2 6.1 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cc(F)ccc1F)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400220 117009 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 448 8 1 2 6.1 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cc(F)ccc1F)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
162665334 183138 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4783876 183138 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4803469 183138 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 436 11 2 6 4.7 CCC[C@H](C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
134131406 141776 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccccc2F)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3885445 141776 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccccc2F)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
162644557 178863 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 425 12 3 4 3.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4740613 178863 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 425 12 3 4 3.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN)cc1 10.1021/acs.jmedchem.0c01581
162644557 178863 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 425 12 3 4 3.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4740613 178863 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 425 12 3 4 3.5 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCN)cc1 10.1021/acs.jmedchem.0c01581
134131406 141776 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccccc2F)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3885445 141776 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 401 10 1 4 4.2 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccccc2F)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
58466533 134633 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 489 10 1 4 6.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 nan
CHEMBL3714828 134633 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 489 10 1 4 6.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 nan
CHEMBL3719582 134633 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayActivity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 489 10 1 4 6.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 nan
58466533 134633 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 489 10 1 4 6.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 nan
CHEMBL3714828 134633 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 489 10 1 4 6.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 nan
CHEMBL3719582 134633 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayActivity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 489 10 1 4 6.2 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cccc(F)n1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 nan
118727670 117051 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400261 117051 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
51348370 134234 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@@H]3C[C@H]3c3cccs3)cc2)cc1 nan
CHEMBL3718649 134234 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assayModulator activity at GPR88 (unknown origin) expressed in cell membranes incubated for 1 hr by liquid scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@@H]3C[C@H]3c3cccs3)cc2)cc1 nan
51348370 134234 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@@H]3C[C@H]3c3cccs3)cc2)cc1 nan
CHEMBL3718649 134234 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at GPR88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@@H]3C[C@H]3c3cccs3)cc2)cc1 nan
51355598 116980 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 385 11 3 4 3.4 CCCC(C)COc1ccc([C@H](CO)NC(=O)C(CO)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3400186 116980 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 385 11 3 4 3.4 CCCC(C)COc1ccc([C@H](CO)NC(=O)C(CO)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
118730005 117483 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 384 11 3 4 3.6 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](NC)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403777 117483 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 384 11 3 4 3.6 CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](NC)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
162673915 182441 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccncc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4793946 182441 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccncc2)cc1 10.1021/acs.jmedchem.0c01581
162673915 182441 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccncc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4793946 182441 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 473 12 2 4 5.2 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCc2ccncc2)cc1 10.1021/acs.jmedchem.0c01581
118730161 117534 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3404048 117534 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 412 8 1 2 5.9 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
168278367 190576 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 1 5 4.4 Cc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5189064 190576 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 1 5 4.4 Cc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
51354740 133166 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 465 12 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715014 133166 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 465 12 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
51354740 133166 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 465 12 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
CHEMBL3715014 133166 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 30 mins by cell based cAMP HTRF assay
ChEMBL 465 12 3 4 4.3 CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 nan
168278367 190576 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 1 5 4.4 Cc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5189064 190576 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 418 9 1 5 4.4 Cc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
168275346 189635 0 None -549 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at wild type GPR88 expressed in mouse striatal membrane assessed as [35S] GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at wild type GPR88 expressed in mouse striatal membrane assessed as [35S] GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 477 12 2 6 4.1 CCC[C@H](C)COc1ccc([C@H](Cn2cc(C(=O)NC)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
CHEMBL5175064 189635 0 None -549 2 Mouse 5.1 pEC50 = 5.1 Functional
Agonist activity at wild type GPR88 expressed in mouse striatal membrane assessed as [35S] GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at wild type GPR88 expressed in mouse striatal membrane assessed as [35S] GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 477 12 2 6 4.1 CCC[C@H](C)COc1ccc([C@H](Cn2cc(C(=O)NC)nn2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.1c01075
162657387 180485 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 525 13 3 5 5.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCNC(=O)OC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4759904 180485 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 525 13 3 5 5.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCNC(=O)OC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
162657387 180485 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 525 13 3 5 5.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCNC(=O)OC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4759904 180485 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production by TR-FRET assay
ChEMBL 525 13 3 5 5.1 CCCC(C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)C(=O)NCCNC(=O)OC(C)(C)C)cc1 10.1021/acs.jmedchem.0c01581
51355880 117488 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 451 11 1 4 4.7 CCCC(C)COc1ccc([C@H](CN2CCN(C)CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403782 117488 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 451 11 1 4 4.7 CCCC(C)COc1ccc([C@H](CN2CCN(C)CC2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
118727676 117057 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 456 10 1 3 6.3 CCOc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400267 117057 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 456 10 1 3 6.3 CCOc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
118727663 117044 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400254 117044 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 430 8 1 2 6.0 CC(C)C[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2015.02.038
168269202 189412 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 434 10 2 6 3.6 C[C@H](C(=O)N[C@@H](Cn1cc(CO)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5171567 189412 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 434 10 2 6 3.6 C[C@H](C(=O)N[C@@H](Cn1cc(CO)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168296691 191613 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 447 10 2 6 3.2 C[C@H](C(=O)N[C@@H](Cn1cc(C(N)=O)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5204827 191613 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 447 10 2 6 3.2 C[C@H](C(=O)N[C@@H](Cn1cc(C(N)=O)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
51356141 117489 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 438 11 1 4 4.8 CCCC(C)COc1ccc([C@H](CN2CCOCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403783 117489 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 438 11 1 4 4.8 CCCC(C)COc1ccc([C@H](CN2CCOCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmcl.2015.01.036
168269202 189412 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 434 10 2 6 3.6 C[C@H](C(=O)N[C@@H](Cn1cc(CO)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5171567 189412 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 434 10 2 6 3.6 C[C@H](C(=O)N[C@@H](Cn1cc(CO)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168296691 191613 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 447 10 2 6 3.2 C[C@H](C(=O)N[C@@H](Cn1cc(C(N)=O)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5204827 191613 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 447 10 2 6 3.2 C[C@H](C(=O)N[C@@H](Cn1cc(C(N)=O)nn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168288752 190818 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 488 14 1 5 6.2 CCCCCCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5192812 190818 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 488 14 1 5 6.2 CCCCCCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
168288752 190818 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 488 14 1 5 6.2 CCCCCCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
CHEMBL5192812 190818 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 488 14 1 5 6.2 CCCCCCc1cn(C[C@H](NC(=O)[C@@H](C)c2ccccc2)c2ccc(OCC3CCC3)cc2)nn1 10.1021/acs.jmedchem.1c01075
51348522 117474 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 10.1016/j.bmcl.2015.01.036
CHEMBL3403765 117474 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to controlAgonist activity at GPR88 (unknown origin) transfected in forskolin-stimulated HEK cells assessed as inhibition of cAMP production after 30 mins by HTRF method relative to control
ChEMBL 377 6 2 3 4.7 Cc1ccc(-c2ccc([C@H](CO)NC(=O)[C@H]3C[C@@H]3c3cccs3)cc2)cc1 10.1016/j.bmcl.2015.01.036
118727678 117059 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 504 10 1 3 7.7 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400269 117059 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 504 10 1 3 7.7 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2015.02.038
162665470 182206 0 None -15 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation countingAgonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation counting
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4784623 182206 0 None -15 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation countingAgonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation counting
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
CHEMBL4790638 182206 0 None -15 2 Mouse 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation countingAgonist activity at GPR88 in mouse striatal membrane assessed as [35S]-GTPgammaS-binding by liquid scintillation counting
ChEMBL 436 11 2 6 4.7 CCCC(C)COc1ccc([C@H](Cc2nnc(N)o2)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1021/acs.jmedchem.0c01581
168275176 190048 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 1 5 4.1 C[C@H](C(=O)N[C@@H](Cn1ccnn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5181466 190048 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 1 5 4.1 C[C@H](C(=O)N[C@@H](Cn1ccnn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
168275176 190048 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 1 5 4.1 C[C@H](C(=O)N[C@@H](Cn1ccnn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
CHEMBL5181466 190048 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assayAgonist activity at GPR88 (unknown origin) expressed in CHO cells coexpressing PPLS-HA assessed as reduction in forskolin-stimulated cAMP production and measured after 90 mins by Lance TR-FRET cAMP assay
ChEMBL 404 9 1 5 4.1 C[C@H](C(=O)N[C@@H](Cn1ccnn1)c1ccc(OCC2CCC2)cc1)c1ccccc1 10.1021/acs.jmedchem.1c01075
134130076 141725 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 413 11 1 5 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(OC)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884939 141725 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 413 11 1 5 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(OC)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
134130076 141725 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 413 11 1 5 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(OC)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884939 141725 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assayAgonist activity at PPLS-HA-tagged-GPR88 (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins by TR-FRET assay
ChEMBL 413 11 1 5 4.1 CCCC(C)COc1ccc([C@@H](NC(=O)Cc2ccc(OC)cc2)C(=O)OC)cc1 10.1016/j.bmc.2016.11.058
155525986 170450 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 443 9 1 4 5.3 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.8b00566
CHEMBL4456708 170450 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay
ChEMBL 443 9 1 4 5.3 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccn1)c1ccc(-c2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.8b00566
118727630 117010 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 448 8 1 2 6.1 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cc(F)cc(F)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400221 117010 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 448 8 1 2 6.1 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1cc(F)cc(F)c1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2015.02.038
118727686 117067 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 483 9 1 3 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(C(=O)N(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
CHEMBL3400277 117067 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay
ChEMBL 483 9 1 3 5.6 CC[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccc(C(=O)N(C)C)cc2)cc1 10.1016/j.bmcl.2015.02.038
12395 3346 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist potency determined in a TR-FRET cAMP assay using CHO cells expressing hGPR88Agonist potency determined in a TR-FRET cAMP assay using CHO cells expressing hGPR88
Guide to Pharmacology 491 10 1 5 5.2 N[C@@H]([C@@H](C)OC)CN(C(=O)[C@H]1[C@H](c2ccc(F)cn2)C1)c1ccc(c2ccc(OC(C)C)cc2)cc1 36749855
10031 3347 5 None 2 2 Human 7.6 pEC50 = 7.6 Functional
In an <i>in vitro</i> cAMP functional assay.In an <i>in vitro</i> cAMP functional assay.
Guide to Pharmacology 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 30011199
134813902 3347 5 None 2 2 Human 7.6 pEC50 = 7.6 Functional
In an <i>in vitro</i> cAMP functional assay.In an <i>in vitro</i> cAMP functional assay.
Guide to Pharmacology 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 30011199
CHEMBL4595209 3347 5 None 2 2 Human 7.6 pEC50 = 7.6 Functional
In an <i>in vitro</i> cAMP functional assay.In an <i>in vitro</i> cAMP functional assay.
Guide to Pharmacology 459 10 1 5 4.4 COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N 30011199
58466521 1044 3 None 29 2 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 24793972
7798 1044 3 None 29 2 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 24793972
CHEMBL3401461 1044 3 None 29 2 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 10 1 3 6.2 CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N 24793972


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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
58466401 117486 0 None - 0 Mouse 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS bindingAgonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS binding
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3403780 117486 0 None - 0 Mouse 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS bindingAgonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS binding
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058
CHEMBL3884102 117486 0 None - 0 Mouse 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS bindingAgonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS binding
ChEMBL 368 10 2 3 4.4 CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 10.1016/j.bmc.2016.11.058