Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
118727607 117003 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 117003 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 117555 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 117555 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 117002 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 117002 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 117001 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 117001 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 117548 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 117548 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 117004 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 117004 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 117553 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 117553 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 117554 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 117554 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 117550 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 117550 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 117006 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 117006 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 3359 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 3359 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 3359 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 117490 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 117490 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 117502 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 117502 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 133167 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 133167 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 133195 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 133195 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 133217 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 133217 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 133232 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 133232 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 133259 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 133259 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 133299 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 133299 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 133338 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 133338 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 133344 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 133344 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 133449 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 133449 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 133472 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 133472 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 133546 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 133546 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 133662 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 133662 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 133844 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 133844 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 133896 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 133896 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 133901 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 133901 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 133935 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 133935 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 133970 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 133970 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 133997 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 133997 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 134034 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 134034 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 134277 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 134277 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 134373 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 134373 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 117490 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 117490 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 117502 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 117502 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 133167 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 133167 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 133195 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 133195 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 133217 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 133217 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 133232 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 133232 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 133259 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 133259 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 133299 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 133299 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 133338 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 133338 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 133344 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 133344 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 133449 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 133449 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 133472 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 133472 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 133546 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 133546 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 133662 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 133662 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 133844 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 133844 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 133896 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 133896 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 133901 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 133901 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 133935 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 133935 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 133970 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 133970 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 133997 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 133997 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 134034 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 134034 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 134277 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 134277 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 134373 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 134373 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 180736 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 180736 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 117043 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 117043 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 190453 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 190453 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 190453 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 190453 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 117005 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 117005 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 117490 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 117490 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 117491 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 117491 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 117499 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 117499 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 117499 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 117078 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 117078 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 133517 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 133517 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 133517 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 133517 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 117055 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 117055 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 117076 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 117076 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 117026 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 117026 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 179608 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 179608 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 179608 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 179608 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 190150 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 190150 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 1047 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 1047 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 1047 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 190150 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 190150 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 179214 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 179214 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 117495 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 117495 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 117071 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 117071 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 179214 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 179214 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 117020 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 117020 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 117045 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 117045 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 117048 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 117048 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 117050 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 117050 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 117052 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 117052 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 117082 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 117082 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 117086 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 117086 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 117511 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 117511 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 117511 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 117511 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 1047 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 1047 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 1047 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 175925 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 175925 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 175925 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 175932 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 175932 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 175932 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 176027 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 176027 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 176027 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 1047 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 1047 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 1047 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 175925 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 175925 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 175925 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 175932 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 175932 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 175932 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 176027 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 176027 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 176027 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 181823 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 181823 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 181823 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 181823 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 189645 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 189645 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 117027 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 117027 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 117030 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 117030 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 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 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 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 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 117038 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 117038 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 117044 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 117044 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 191463 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 191463 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 191463 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 191463 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 141656 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 141656 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 141656 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 141656 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 183164 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 183164 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 183164 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 183186 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 183186 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 183186 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 183164 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 183164 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 183164 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 183186 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 183186 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 183186 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 189645 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 189645 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 133472 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 133472 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 141732 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 141732 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 141732 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 141732 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 133472 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 133472 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 180186 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 180186 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 180186 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 180186 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 180186 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 180186 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 180186 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 180186 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 117197 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 117197 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 117497 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 117497 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 117028 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 117028 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 117029 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 117029 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 117040 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 117040 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 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 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 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 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 133234 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 133234 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 133234 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 133234 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 175666 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 175666 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 175666 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 175666 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 175666 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 175666 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 117504 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 117504 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 117021 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 117021 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 117059 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 117059 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 189763 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 189763 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 190838 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 190838 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 189763 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 189763 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 190838 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 190838 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 117493 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 117493 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 117507 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 117507 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 117073 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 117073 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 117489 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 117489 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 117489 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 117489 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 191273 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 191273 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 191273 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 191273 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 181893 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 181893 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 189668 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 189668 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 190388 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 190388 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 181893 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 181893 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 189668 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 189668 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 190388 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 190388 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 117489 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 117489 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 117506 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 117506 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 117031 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 117031 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 117490 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 117490 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 117490 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 117490 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 117490 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 117490 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 117490 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 117490 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 190210 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 190210 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 190210 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 190210 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 117008 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 117008 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 117551 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 117551 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 117012 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 117012 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 117047 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 117047 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 180765 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 180765 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 180911 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 180911 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 180765 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 180765 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 180911 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 180911 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 117033 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 117033 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 117049 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 117049 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 117058 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 117058 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 180005 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 180005 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 180005 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 180005 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 180444 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 180444 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 180444 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 180444 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 117015 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 117015 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 117064 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 117064 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 117041 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 117041 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 180565 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 180565 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 180841 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 180841 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 180565 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 180565 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 180841 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 180841 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 180708 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 180708 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 180708 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 180708 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 117487 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 117487 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 181938 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 181938 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 182168 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 182168 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 189786 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 189786 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 181938 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 181938 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 182168 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 182168 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 189786 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 189786 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 3359 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 3359 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 3359 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 3359 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 3359 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 3359 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 3359 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 3359 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 3359 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 117513 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 117513 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 180317 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 180317 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 180317 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 180317 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 133786 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 133786 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 133786 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 133786 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 178993 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 178993 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 178993 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 178993 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 117508 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 117508 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 117079 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 117079 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 190806 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 190806 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 190806 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 190806 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 141762 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 141762 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 141762 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 141762 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 181108 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 181108 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 181108 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 181108 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 117498 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 117498 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 117075 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 117075 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 180872 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 180872 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 182856 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 182856 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 190526 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 190526 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 180872 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 180872 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 182856 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 182856 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 190526 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 190526 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 117500 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 117500 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 180033 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 180033 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 182131 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 182131 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 182780 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 182780 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 180033 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 180033 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 180033 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 180033 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 182131 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 182131 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 182780 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 182780 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 1047 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 1047 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 1047 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 117197 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 117197 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 117198 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 117198 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 133914 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 133914 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 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 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 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 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 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 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 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 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 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 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 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 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 134639 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 134639 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 134639 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 134640 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 134640 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 134640 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 134641 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 134641 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 134641 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 134642 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 134642 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 134642 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 134643 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 134643 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 134643 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 134644 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 134644 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 134644 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 134645 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 134645 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 134645 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 134647 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 134647 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 134647 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 134648 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 134648 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 134648 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 134649 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 134649 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 134649 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 134650 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 134650 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 134650 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 134651 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 134651 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 134651 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 1047 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 1047 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 1047 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 117197 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 117197 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 117198 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 117198 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 133914 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 133914 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 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 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 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 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 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 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 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 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 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 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 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 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 134639 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 134639 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 134639 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 134640 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 134640 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 134640 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 134641 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 134641 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 134641 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 134642 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 134642 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 134642 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 134643 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 134643 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 134643 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 134644 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 134644 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 134644 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 134645 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 134645 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 134645 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 134647 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 134647 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 134647 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 134648 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 134648 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 134648 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 134649 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 134649 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 134649 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 134650 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 134650 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 134650 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 134651 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 134651 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 134651 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 117007 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 117007 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 1047 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 1047 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 1047 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 117198 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 117198 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 117016 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 117016 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 181760 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 181760 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 181760 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 181760 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 182750 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 182750 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 175797 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 175797 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 175797 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 182750 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 182750 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 175797 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 175797 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 175797 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 117081 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 117081 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 117056 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 117056 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 189643 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 189643 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 189643 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 189643 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 117054 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 117054 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 190265 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 190265 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 180821 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 180821 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 180821 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 180821 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 190265 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 190265 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 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 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 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 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 117053 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 117053 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 141688 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 141688 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 141688 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 141688 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 117074 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 117074 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 190216 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 190216 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 190216 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 190216 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 117034 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 117034 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 117051 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 117051 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 117039 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 117039 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 189704 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 189704 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 189704 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 189704 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 179611 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 179611 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 179611 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 179611 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 141708 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 141708 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 182945 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 182945 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 189986 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 189986 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 141708 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 141708 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 182945 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 182945 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 189986 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 189986 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 180454 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 180454 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 181088 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 181088 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 180454 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 180454 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 181088 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 181088 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 117063 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 117063 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 191213 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 191213 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 191213 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 191213 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 141794 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 141794 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 117498 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 117498 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 117500 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 117500 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 117512 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 117512 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 133185 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 133185 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 133415 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 133415 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 133473 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 133473 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 133481 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 133481 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 133571 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 133571 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 133840 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 133840 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 134070 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 134070 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 134139 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 134139 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 134195 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 134195 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 117498 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 117498 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 117500 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 117500 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 117512 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 117512 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 133185 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 133185 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 133415 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 133415 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 133473 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 133473 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 133481 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 133481 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 133571 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 133571 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 133840 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 133840 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 134070 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 134070 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 134139 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 134139 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 134195 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 134195 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 191504 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 191504 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 141794 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 141794 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 180343 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 180343 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 175863 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 175863 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 175863 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 180343 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 180343 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 175863 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 175863 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 175863 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 117000 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 117000 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 117010 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 117010 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 191504 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 191504 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 191632 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 191632 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 191632 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 191632 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 117509 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 117509 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 117499 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 117499 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 117499 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 117499 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 117499 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 117499 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 117499 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 117499 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 117499 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 180894 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 180894 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 180894 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 180894 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 117013 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 117013 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 117065 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 117065 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 3359 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 3359 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 3359 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 3359 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 3359 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 3359 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 117035 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 117035 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 117061 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 117061 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 179125 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 179125 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 189651 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 189651 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 179125 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 179125 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 189651 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 189651 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 3359 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 3359 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 3359 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 117505 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 117505 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 117084 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 117084 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 182263 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 182263 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 182900 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 182900 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 181556 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 181556 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 181556 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 181556 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 182263 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 182263 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 182900 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 182900 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 3359 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 3359 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 3359 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 180697 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 180697 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 180697 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 180697 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 189498 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 189498 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 117494 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 117494 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 117494 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 117494 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 179995 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 179995 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 179995 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 179995 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 117009 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 117009 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 117552 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 117552 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 1047 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 1047 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 1047 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 117488 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 117488 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 189420 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 189420 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 175745 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 175745 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 175745 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 175930 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 175930 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 175930 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 189420 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 189420 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 175745 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 175745 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 175745 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 175930 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 175930 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 175930 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 179872 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 179872 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 181217 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 181217 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 181217 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 181217 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 179872 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 179872 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 181586 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 181586 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 181586 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 181586 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 181586 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 181586 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 3359 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 3359 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 3359 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 181423 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 181423 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 181968 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 181968 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 181423 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 181423 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 181968 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 181968 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 141594 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 141594 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 141594 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 141594 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 117499 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 117499 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 117499 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 117499 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 117499 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 117499 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 179653 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 179653 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 179867 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 179867 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 181231 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 181231 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 181302 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 181302 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 181231 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 181231 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 181302 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 181302 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 179653 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 179653 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 179867 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 179867 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 117083 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 117083 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 1047 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 1047 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 1047 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 117018 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 117018 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 179597 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 179597 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 181392 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 181392 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 179597 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 179597 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 181392 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 181392 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 117503 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 117503 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 180764 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 180764 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 180764 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 180764 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 182216 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 182216 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 182216 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 117036 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 117036 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 141754 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 141754 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 141714 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 141714 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 182943 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 182943 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 141754 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 141754 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 181972 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 181972 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 181972 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 181972 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 141714 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 141714 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 182943 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 182943 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 182216 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 182216 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 182216 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 182216 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 182216 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 182216 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 117011 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 117011 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 190232 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 190232 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 190232 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 190232 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 117017 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 117017 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 117486 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 117486 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 191501 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 191501 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 191501 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 191501 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 117066 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 117066 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 141785 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 141785 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 141785 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 141785 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 141785 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 141785 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 178902 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 178902 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 141785 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 141785 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 178902 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 178902 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 117487 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 117487 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 133129 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 133129 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 133170 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 133170 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 133225 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 133225 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 133275 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 133275 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 133418 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 133418 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 133526 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 133526 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 133567 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 133567 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 133703 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 133703 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 133971 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 133971 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 134005 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 134005 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 134169 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 134169 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 134291 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 134291 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 134307 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 134307 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 134396 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 134396 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 117487 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 117487 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 133129 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 133129 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 133170 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 133170 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 133225 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 133225 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 133275 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 133275 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 133418 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 133418 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 133526 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 133526 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 133567 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 133567 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 133703 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 133703 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 133971 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 133971 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 134005 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 134005 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 134169 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 134169 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 134291 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 134291 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 134307 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 134307 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 134396 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 134396 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 117042 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 117042 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 175920 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 175920 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 175920 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 175920 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 175920 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 175920 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 179870 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 179870 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 179870 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 179870 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 117062 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 117062 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 117085 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 117085 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 117019 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 117019 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 189645 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 189645 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 117077 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 117077 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 117060 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 117060 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 181373 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 181373 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 181373 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 181373 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 117510 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 117510 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 183082 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 183082 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 183082 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 190225 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 190225 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 190225 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 190225 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 183082 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 183082 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 183082 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 117069 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 117069 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 1047 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 1047 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 1047 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 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 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 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 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 182136 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 182136 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 182136 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 182136 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 1047 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 1047 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 1047 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 1047 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 1047 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 1047 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 117492 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 117492 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 117037 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 117037 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 183107 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 183107 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 183107 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 189456 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 189456 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 134196 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 134196 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 134196 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 134196 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 183107 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 183107 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 183107 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 189456 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 189456 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 179884 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 179884 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 179884 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 179884 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 117067 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 117067 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 189498 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 189498 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 183148 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 183148 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 183148 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 117022 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 117022 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 183148 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 183148 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 183148 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 141788 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 141788 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 178873 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 178873 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 178873 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 178873 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 141788 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 141788 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 134646 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 134646 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 134646 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 134646 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 134646 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 134646 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 117064 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 117064 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 134247 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 134247 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 134247 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 134247 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 116993 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 116993 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 117496 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 117496 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 182451 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 182451 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 182451 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 182451 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 117547 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 117547 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 190586 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 190586 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 133179 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 133179 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 133179 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 133179 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 190586 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 190586 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 189645 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 189645 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 180495 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 180495 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 180495 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 180495 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 117501 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 117501 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 117070 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 117070 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 117057 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 117057 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 189422 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 189422 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 191623 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 191623 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 117502 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 117502 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 189422 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 189422 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 191623 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 191623 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 190828 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 190828 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 190828 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 190828 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 117487 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 117487 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 117072 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 117072 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 182216 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 182216 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 182216 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 190058 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 190058 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 190058 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 190058 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 141737 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 141737 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 141737 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 141737 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 170460 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 170460 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 117023 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 117023 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 117080 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 117080 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 3358 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
167993640 3358 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 3359 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 3359 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 3359 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 1047 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 1047 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 1047 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




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 117499 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 117499 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 117499 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