Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
57383409 109378 0 None - 1 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccc(OC)c3)cc21 10.1021/jm500126s
CHEMBL3234238 109378 0 None - 1 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccc(OC)c3)cc21 10.1021/jm500126s
57383437 109404 0 None - 1 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 420 4 1 4 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)N(C)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
CHEMBL3234511 109404 0 None - 1 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 420 4 1 4 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)N(C)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
57383415 109417 0 None - 1 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 411 4 1 4 2.7 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCN3CCCCC3)cc21 10.1021/jm500126s
CHEMBL3234524 109417 0 None - 1 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 411 4 1 4 2.7 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCN3CCCCC3)cc21 10.1021/jm500126s
57383414 109425 0 None 9 2 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
CHEMBL3234537 109425 0 None 9 2 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
57383402 109413 0 None - 1 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccn3)cc21 10.1021/jm500126s
CHEMBL3234520 109413 0 None - 1 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccn3)cc21 10.1021/jm500126s
57377245 109395 0 None - 1 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 472 4 1 3 4.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C(F)(F)F)cc3)cc21 10.1021/jm500126s
CHEMBL3234502 109395 0 None - 1 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 472 4 1 3 4.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C(F)(F)F)cc3)cc21 10.1021/jm500126s
57377247 109396 0 None - 1 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
CHEMBL3234503 109396 0 None - 1 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
57383428 109401 0 None - 1 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 420 4 1 4 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234508 109401 0 None - 1 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 420 4 1 4 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383411 109410 0 None - 1 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
CHEMBL3234517 109410 0 None - 1 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
57383403 109420 1 None 7 2 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234527 109420 1 None 7 2 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383424 109406 0 None - 1 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 376 2 1 3 3.7 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccccc3)cc21 10.1021/jm500126s
CHEMBL3234513 109406 0 None - 1 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 376 2 1 3 3.7 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccccc3)cc21 10.1021/jm500126s
16007816 45374 5 None - 1 Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 4 1 3 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C)cc3)cc21 10.1021/jm500126s
CHEMBL1529544 45374 5 None - 1 Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 4 1 3 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C)cc3)cc21 10.1021/jm500126s
57383429 109398 0 None - 1 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 494 7 1 6 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cc(OC)c(OC)c(OC)c3)cc21 10.1021/jm500126s
CHEMBL3234505 109398 0 None - 1 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 494 7 1 6 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cc(OC)c(OC)c(OC)c3)cc21 10.1021/jm500126s
57383435 109393 0 None - 1 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 450 5 1 4 4.5 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(SC)cc3)cc21 10.1021/jm500126s
CHEMBL3234500 109393 0 None - 1 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 450 5 1 4 4.5 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(SC)cc3)cc21 10.1021/jm500126s
57383416 109408 0 None - 1 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 390 3 1 3 3.4 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3)cc21 10.1021/jm500126s
CHEMBL3234515 109408 0 None - 1 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 390 3 1 3 3.4 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3)cc21 10.1021/jm500126s
57383398 109423 0 None - 1 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 4.2 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(NC(=O)Cc3ccc(F)cc3)cc21 10.1021/jm500126s
CHEMBL3234535 109423 0 None - 1 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 4.2 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(NC(=O)Cc3ccc(F)cc3)cc21 10.1021/jm500126s
57383397 109426 0 None 16 2 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 496 4 1 3 5.1 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc(Br)cc3)cc21 10.1021/jm500126s
CHEMBL3234538 109426 0 None 16 2 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 496 4 1 3 5.1 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc(Br)cc3)cc21 10.1021/jm500126s
16007814 42639 3 None 6 2 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL1503220 42639 3 None 6 2 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383420 109429 0 None 11 2 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
CHEMBL3234540 109429 0 None 11 2 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
57383413 109411 0 None - 1 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccc(Cl)c3)cc21 10.1021/jm500126s
CHEMBL3234518 109411 0 None - 1 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccc(Cl)c3)cc21 10.1021/jm500126s
57383422 109414 0 None - 1 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
CHEMBL3234521 109414 0 None - 1 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
57383400 109394 0 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 460 4 1 3 5.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C(C)(C)C)cc3)cc21 10.1021/jm500126s
CHEMBL3234501 109394 0 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 460 4 1 3 5.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C(C)(C)C)cc3)cc21 10.1021/jm500126s
57383418 109397 0 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 482 5 1 5 3.2 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)cc21 10.1021/jm500126s
CHEMBL3234504 109397 0 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 482 5 1 5 3.2 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)cc21 10.1021/jm500126s
20861039 109399 3 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 4 1 5 3.5 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc4c(c3)OCO4)cc21 10.1021/jm500126s
CHEMBL3234506 109399 3 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 4 1 5 3.5 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc4c(c3)OCO4)cc21 10.1021/jm500126s
57383427 109402 0 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 6 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234509 109402 0 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 6 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383404 109407 0 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 406 3 1 4 3.7 COc1ccc(NC(=O)c2ccc3c(c2)N(C)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
CHEMBL3234514 109407 0 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 406 3 1 4 3.7 COc1ccc(NC(=O)c2ccc3c(c2)N(C)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
57383433 109409 0 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 408 3 1 3 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
CHEMBL3234516 109409 0 None - 1 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 408 3 1 3 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
57383434 109427 0 None 32 2 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 4 1 3 5.5 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc4ccccc4c3)cc21 10.1021/jm500126s
CHEMBL3234539 109427 0 None 32 2 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 4 1 3 5.5 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc4ccccc4c3)cc21 10.1021/jm500126s
57383399 109379 0 None - 1 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 404 4 1 3 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3)cc21 10.1021/jm500126s
CHEMBL3234239 109379 0 None - 1 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 404 4 1 3 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3)cc21 10.1021/jm500126s
57383436 109431 0 None 12 2 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
CHEMBL3234542 109431 0 None 12 2 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
16007818 59466 5 None - 1 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3OC)cc21 10.1021/jm500126s
CHEMBL1726600 59466 5 None - 1 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3OC)cc21 10.1021/jm500126s
16007812 59159 5 None - 1 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 438 4 1 3 4.4 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
CHEMBL1714249 59159 5 None - 1 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 438 4 1 3 4.4 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
57383430 109424 0 None 18 2 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
CHEMBL3234536 109424 0 None 18 2 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
20861041 109392 1 None - 1 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 4 1 3 4.3 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NC(C)c3ccccc3)cc21 10.1021/jm500126s
CHEMBL3234499 109392 1 None - 1 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 4 1 3 4.3 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NC(C)c3ccccc3)cc21 10.1021/jm500126s
57383406 109418 0 None - 1 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 385 5 1 4 2.1 CN(C)CCCNC(=O)c1ccc2c(c1)N(C)C(=O)c1ccccc1[S+]2[O-] 10.1021/jm500126s
CHEMBL3234525 109418 0 None - 1 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 385 5 1 4 2.1 CN(C)CCCNC(=O)c1ccc2c(c1)N(C)C(=O)c1ccccc1[S+]2[O-] 10.1021/jm500126s
57383417 109421 0 None - 1 Human 4.3 pAC50 = 4.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 432 5 0 3 4.5 CCN(Cc1ccccc1)C(=O)c1ccc2c(c1)N(CC)C(=O)c1ccccc1[S+]2[O-] 10.1021/jm500126s
CHEMBL3234532 109421 0 None - 1 Human 4.3 pAC50 = 4.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 432 5 0 3 4.5 CCN(Cc1ccccc1)C(=O)c1ccc2c(c1)N(CC)C(=O)c1ccccc1[S+]2[O-] 10.1021/jm500126s
57377246 2525 1 None 57 2 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 410 4 1 4 3.5 O=C(c1ccc2c(c1)N(C)C(=O)c1c([S@@]2=O)cccc1)NCCc1cccs1 10.1021/jm500126s
8368 2525 1 None 57 2 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 410 4 1 4 3.5 O=C(c1ccc2c(c1)N(C)C(=O)c1c([S@@]2=O)cccc1)NCCc1cccs1 10.1021/jm500126s
CHEMBL3234544 2525 1 None 57 2 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 410 4 1 4 3.5 O=C(c1ccc2c(c1)N(C)C(=O)c1c([S@@]2=O)cccc1)NCCc1cccs1 10.1021/jm500126s
57383401 109432 0 None 28 2 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
CHEMBL3234543 109432 0 None 28 2 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
57383423 109405 0 None - 1 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 6 1 4 4.2 CCCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234512 109405 0 None - 1 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 6 1 4 4.2 CCCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383432 109419 0 None - 1 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 5 1 4 4.8 CCN1C(=O)c2ccccc2Sc2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234526 109419 0 None - 1 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 5 1 4 4.8 CCN1C(=O)c2ccccc2Sc2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383419 109422 0 None - 1 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 4.0 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(NC(=O)Cc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234534 109422 0 None - 1 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 4.0 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(NC(=O)Cc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383421 109412 0 None - 1 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
CHEMBL3234519 109412 0 None - 1 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
57383426 109400 0 None - 1 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 390 3 1 3 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccccc3)cc21 10.1021/jm500126s
CHEMBL3234507 109400 0 None - 1 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 390 3 1 3 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccccc3)cc21 10.1021/jm500126s
57383425 109403 0 None - 1 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 406 4 2 4 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)NC(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
CHEMBL3234510 109403 0 None - 1 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 406 4 2 4 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)NC(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
16007752 58935 5 None - 1 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 496 6 1 4 5.0 COc1ccc(CNC(=O)c2ccc3c(c2)N(Cc2ccccc2)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
CHEMBL1703877 58935 5 None - 1 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 496 6 1 4 5.0 COc1ccc(CNC(=O)c2ccc3c(c2)N(Cc2ccccc2)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
16007820 67141 2 None - 1 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
CHEMBL1894173 67141 2 None - 1 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
57383431 109415 0 None 70 2 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 410 4 1 4 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3cccs3)cc21 10.1021/jm500126s
CHEMBL3234522 109415 0 None 70 2 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 410 4 1 4 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3cccs3)cc21 10.1021/jm500126s
57383412 109416 0 None - 1 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
CHEMBL3234523 109416 0 None - 1 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
57383405 109430 0 None 15 2 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
CHEMBL3234541 109430 0 None 15 2 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
10015731 206418 0 None - 1 Rat 10.9 pEC50 = 10.9 Functional
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from rat
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@H]21 10.1021/jm0000113
CHEMBL98305 206418 0 None - 1 Rat 10.9 pEC50 = 10.9 Functional
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from rat
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@H]21 10.1021/jm0000113
10378389 201545 1 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 201545 1 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 201545 1 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
76325150 105928 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 105928 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 105928 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
167715 2820 12 None 6 4 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2820 12 None 6 4 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2820 12 None 6 4 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
167715 2820 12 None 6 4 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2820 12 None 6 4 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2820 12 None 6 4 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
76325156 105896 1 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 105896 1 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 105896 1 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
137657882 159115 0 None 12589 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 159115 0 None 12589 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
137657882 159115 0 None 12589 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 159115 0 None 12589 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
56599011 145883 0 None - 1 Human 10.0 pEC50 = 10 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 449 9 1 5 4.7 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
CHEMBL3921903 145883 0 None - 1 Human 10.0 pEC50 = 10 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 449 9 1 5 4.7 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
44554472 105789 0 None 1071 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099226 105789 0 None 1071 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139040 105789 0 None 1071 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
76328715 105878 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115582 105878 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139265 105878 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
13851595 173923 2 None 489 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3098131 173923 2 None 489 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL455497 173923 2 None 489 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
66633659 152787 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 452 9 1 6 4.1 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
CHEMBL3978288 152787 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 452 9 1 6 4.1 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
17449900 138999 12 None -1 3 Human 9.7 pEC50 = 9.7 Functional
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 138999 12 None -1 3 Human 9.7 pEC50 = 9.7 Functional
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
137460109 190779 0 None 3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at dopamine D2 receptor (unknown origin) assessed as increase in GTPgammaS bindingAgonist activity at dopamine D2 receptor (unknown origin) assessed as increase in GTPgammaS binding
ChEMBL 482 7 2 4 5.4 CCCN(CCN1CCN(c2ccc3c(c2)[nH]c2ccccc23)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.ejmech.2022.114378
CHEMBL5192367 190779 0 None 3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at dopamine D2 receptor (unknown origin) assessed as increase in GTPgammaS bindingAgonist activity at dopamine D2 receptor (unknown origin) assessed as increase in GTPgammaS binding
ChEMBL 482 7 2 4 5.4 CCCN(CCN1CCN(c2ccc3c(c2)[nH]c2ccccc23)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.ejmech.2022.114378
132578416 173224 0 None 1 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human D2 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 383 9 3 4 4.8 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4538230 173224 0 None 1 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human D2 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 383 9 3 4 4.8 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2016.08.021
17449900 138999 12 None -1 3 Human 9.6 pEC50 = 9.6 Functional
Intrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 138999 12 None -1 3 Human 9.6 pEC50 = 9.6 Functional
Intrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
127046922 139169 0 None 5 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at dopamine D2 receptor (unknown origin) by cAMP accumulation assayAgonist activity at dopamine D2 receptor (unknown origin) by cAMP accumulation assay
ChEMBL 417 7 3 4 2.9 CN(CCCCNC(=O)c1cc2ccccc2[nH]1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.8b00435
CHEMBL3798179 139169 0 None 5 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at dopamine D2 receptor (unknown origin) by cAMP accumulation assayAgonist activity at dopamine D2 receptor (unknown origin) by cAMP accumulation assay
ChEMBL 417 7 3 4 2.9 CN(CCCCNC(=O)c1cc2ccccc2[nH]1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.8b00435
90645289 112001 3 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assayAgonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assay
ChEMBL 519 8 2 6 5.5 Cc1cc(C)c2c(N)c(C(=O)NCCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)sc2n1 10.1021/jm500457x
CHEMBL3298895 112001 3 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assayAgonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assay
ChEMBL 519 8 2 6 5.5 Cc1cc(C)c2c(N)c(C(=O)NCCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)sc2n1 10.1021/jm500457x
10715828 53759 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 397 7 1 4 3.7 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4F)CC3)cc2N1 10.1021/jm300603y
CHEMBL160630 53759 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 397 7 1 4 3.7 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4F)CC3)cc2N1 10.1021/jm300603y
127046922 139169 0 None 5 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 417 7 3 4 2.9 CN(CCCCNC(=O)c1cc2ccccc2[nH]1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.6b01875
CHEMBL3798179 139169 0 None 5 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 417 7 3 4 2.9 CN(CCCCNC(=O)c1cc2ccccc2[nH]1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.6b01875
219050 3309 21 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
52 3309 21 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
CHEMBL431367 3309 21 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
3033200 173945 5 None 616 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 173945 5 None 616 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
3033200 173945 5 None 616 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 173945 5 None 616 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
76325152 105877 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 105877 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 105877 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
12899503 53426 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 379 7 1 4 3.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm300603y
CHEMBL160357 53426 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 379 7 1 4 3.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm300603y
228 441 26 None -4 8 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 441 26 None -4 8 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 441 26 None -4 8 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 441 26 None -4 8 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 441 26 None -4 8 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
56597940 153405 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 450 7 2 6 2.9 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCC(=O)N5)CC3)cc2N1 nan
CHEMBL3983588 153405 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 450 7 2 6 2.9 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCC(=O)N5)CC3)cc2N1 nan
11154555 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
5037 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
7671 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
CHEMBL2028019 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
CHEMBL3085826 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
DB06016 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
21073553 144652 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 438 7 1 7 2.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)nc2N1 nan
CHEMBL3912435 144652 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 438 7 1 7 2.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)nc2N1 nan
137633863 156072 0 None -12 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 156072 0 None -12 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
137633863 156072 0 None -12 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 156072 0 None -12 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
71459660 83408 0 None 2 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 548 17 2 4 8.1 CCCN(CCCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
CHEMBL2206265 83408 0 None 2 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 548 17 2 4 8.1 CCCN(CCCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
11154555 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
5037 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
7671 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
CHEMBL2028019 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
CHEMBL3085826 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
DB06016 786 57 None 1 4 Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
44554649 103777 0 None 457 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099235 103777 0 None 457 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
10692886 53357 2 None - 1 Human 9.3 pEC50 = 9.3 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
CHEMBL160296 53357 2 None - 1 Human 9.3 pEC50 = 9.3 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
CHEMBL1813590 53357 2 None - 1 Human 9.3 pEC50 = 9.3 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
52937876 60831 0 None -489 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrsAgonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrs
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765633 60831 0 None -489 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrsAgonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrs
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
44554820 105792 0 None 31 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099222 105792 0 None 31 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139044 105792 0 None 31 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
21073553 144652 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 438 7 1 7 2.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)nc2N1 nan
CHEMBL3912435 144652 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 438 7 1 7 2.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)nc2N1 nan
10692886 53357 2 None - 1 Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL160296 53357 2 None - 1 Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL1813590 53357 2 None - 1 Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
681 1432 65 None -17 12 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
940 1432 65 None -17 12 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
947 1432 65 None -17 12 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
CHEMBL59 1432 65 None -17 12 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
DB00988 1432 65 None -17 12 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
76321554 105909 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 105909 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 105909 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
46882052 6147 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 287 4 0 2 2.8 O=C1N(CCN2CCCCCC2)CCN1c1ccccc1 10.1016/j.bmcl.2010.01.090
CHEMBL1081489 6147 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 287 4 0 2 2.8 O=C1N(CCN2CCCCCC2)CCN1c1ccccc1 10.1016/j.bmcl.2010.01.090
46881463 7124 0 None 794 3 Human 9.2 pEC50 = 9.2 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 293 3 1 2 2.7 O=C1N(CC2CCCCN2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1085672 7124 0 None 794 3 Human 9.2 pEC50 = 9.2 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 293 3 1 2 2.7 O=C1N(CC2CCCCN2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
44621617 172737 8 None - 1 Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 355 4 1 3 4.0 N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4526364 172737 8 None - 1 Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 355 4 1 3 4.0 N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.9b00508
21786101 155179 0 None 38 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 261 2 2 3 2.7 CCCN1CCC[C@@H]2Cc3c(ccc(O)c3O)C[C@H]21 10.1016/j.bmc.2007.06.036
CHEMBL405519 155179 0 None 38 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 261 2 2 3 2.7 CCCN1CCC[C@@H]2Cc3c(ccc(O)c3O)C[C@H]21 10.1016/j.bmc.2007.06.036
2407 3308 73 None 11 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
59227 3308 73 None 11 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
941 3308 73 None 11 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
CHEMBL1303 3308 73 None 11 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
DB05271 3308 73 None 11 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
44621617 172737 8 None - 1 Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 355 4 1 3 4.0 N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4526364 172737 8 None - 1 Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 355 4 1 3 4.0 N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.9b00508
25093832 155327 0 None 2 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155327 0 None 2 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
25093832 155327 0 None 2 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155327 0 None 2 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
46882053 6148 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 305 4 0 2 2.9 O=C1N(CCN2CCCCCC2)CCN1c1cccc(F)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1081490 6148 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 305 4 0 2 2.9 O=C1N(CCN2CCCCCC2)CCN1c1cccc(F)c1 10.1016/j.bmcl.2010.01.090
10715828 53759 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 397 7 1 4 3.7 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4F)CC3)cc2N1 10.1021/jm300603y
CHEMBL160630 53759 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 397 7 1 4 3.7 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4F)CC3)cc2N1 10.1021/jm300603y
10763756 54125 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 404 7 1 5 3.4 N#Cc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL160921 54125 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 404 7 1 5 3.4 N#Cc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
10502413 168904 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 423 9 1 5 4.0 CCOc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL443034 168904 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 423 9 1 5 4.0 CCOc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
681 1432 65 None -17 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
940 1432 65 None -17 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
947 1432 65 None -17 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
CHEMBL59 1432 65 None -17 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
DB00988 1432 65 None -17 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
12899503 53426 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 379 7 1 4 3.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm300603y
CHEMBL160357 53426 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 379 7 1 4 3.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm300603y
44554468 105774 0 None 151 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099225 105774 0 None 151 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139011 105774 0 None 151 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
66633662 151472 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 435 7 1 6 3.3 O=c1ccc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)cc2[nH]1 nan
CHEMBL3966956 151472 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 435 7 1 6 3.3 O=c1ccc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)cc2[nH]1 nan
131801153 169415 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 1 hr by FLIPR assayAgonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 1 hr by FLIPR assay
ChEMBL 418 7 2 4 4.0 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5[nH]ccc45)CC3)cc2N1 10.1021/acs.jmedchem.8b00435
CHEMBL4442260 169415 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 1 hr by FLIPR assayAgonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 1 hr by FLIPR assay
ChEMBL 418 7 2 4 4.0 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5[nH]ccc45)CC3)cc2N1 10.1021/acs.jmedchem.8b00435
681 1432 65 None -17 12 Human 9.0 pEC50 = 9 Functional
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2019.04.014
940 1432 65 None -17 12 Human 9.0 pEC50 = 9 Functional
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2019.04.014
947 1432 65 None -17 12 Human 9.0 pEC50 = 9 Functional
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2019.04.014
CHEMBL59 1432 65 None -17 12 Human 9.0 pEC50 = 9 Functional
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2019.04.014
DB00988 1432 65 None -17 12 Human 9.0 pEC50 = 9 Functional
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2019.04.014
242 467 117 None -6 12 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
34 467 117 None -6 12 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
60795 467 117 None -6 12 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
CHEMBL1112 467 117 None -6 12 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
DB01238 467 117 None -6 12 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
44554984 103773 0 None 208 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099231 103773 0 None 208 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
127047229 139022 0 None -1 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 315 7 0 4 3.3 CCCN(CCC)[C@@H]1Cc2cccc3c2n(c(=O)n3CCC)C1 10.1021/acs.jmedchem.6b01875
CHEMBL3797209 139022 0 None -1 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 315 7 0 4 3.3 CCCN(CCC)[C@@H]1Cc2cccc3c2n(c(=O)n3CCC)C1 10.1021/acs.jmedchem.6b01875
242 467 117 None -6 12 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assayInverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.8b00435
34 467 117 None -6 12 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assayInverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.8b00435
60795 467 117 None -6 12 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assayInverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.8b00435
CHEMBL1112 467 117 None -6 12 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assayInverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.8b00435
DB01238 467 117 None -6 12 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assayInverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.8b00435
46882004 5513 0 None - 1 Human 9.0 pEC50 = 9 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 321 4 0 2 3.5 O=C1N(CCN2CCCCCC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1077344 5513 0 None - 1 Human 9.0 pEC50 = 9 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 321 4 0 2 3.5 O=C1N(CCN2CCCCCC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
11154555 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
11154555 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 786 57 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
44554474 105791 0 None 301 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099227 105791 0 None 301 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139043 105791 0 None 301 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
681 1432 65 None -288 12 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
940 1432 65 None -288 12 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
947 1432 65 None -288 12 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
CHEMBL59 1432 65 None -288 12 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
DB00988 1432 65 None -288 12 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
2 3198 19 None -12 7 Human 8.9 pEC50 = 8.9 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3198 19 None -12 7 Human 8.9 pEC50 = 8.9 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3198 19 None -12 7 Human 8.9 pEC50 = 8.9 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
2 3198 19 None -12 7 Human 8.9 pEC50 = 8.9 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3198 19 None -12 7 Human 8.9 pEC50 = 8.9 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3198 19 None -12 7 Human 8.9 pEC50 = 8.9 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
2 3198 19 None -12 7 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
54562 3198 19 None -12 7 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
CHEMBL240773 3198 19 None -12 7 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
2470 3583 46 None -17 11 Human 8.9 pEC50 = 8.9 Functional
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 nan
3300 3583 46 None -17 11 Human 8.9 pEC50 = 8.9 Functional
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 nan
5265 3583 46 None -17 11 Human 8.9 pEC50 = 8.9 Functional
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 nan
99 3583 46 None -17 11 Human 8.9 pEC50 = 8.9 Functional
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 nan
CHEMBL267930 3583 46 None -17 11 Human 8.9 pEC50 = 8.9 Functional
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 nan
44554982 103772 0 None 58 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099230 103772 0 None 58 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
56597227 153261 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 437 7 1 6 3.3 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)cc2N1 nan
CHEMBL3982360 153261 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 437 7 1 6 3.3 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)cc2N1 nan
24754400 154051 0 None -19 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 423 8 1 5 3.8 CCCN(CCN1CCN(c2ccccc2OC)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
CHEMBL399164 154051 0 None -19 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 423 8 1 5 3.8 CCCN(CCN1CCN(c2ccccc2OC)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
228 441 26 None -2 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 441 26 None -2 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 441 26 None -2 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 441 26 None -2 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 441 26 None -2 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
76321556 105883 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 105883 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 105883 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
164619170 185009 0 None 10 3 Human 8.8 pEC50 = 8.8 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185009 0 None 10 3 Human 8.8 pEC50 = 8.8 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
56593482 3866 1 None 602 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
7650 3866 1 None 602 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
CHEMBL2165119 3866 1 None 602 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
2 3198 19 None -12 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
54562 3198 19 None -12 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
CHEMBL240773 3198 19 None -12 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
164619170 185009 0 None 10 3 Human 8.8 pEC50 = 8.8 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185009 0 None 10 3 Human 8.8 pEC50 = 8.8 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
228 441 26 None -2 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 441 26 None -2 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 441 26 None -2 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 441 26 None -2 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 441 26 None -2 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
45140376 198964 0 None -2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm901618d
CHEMBL599635 198964 0 None -2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm901618d
71459659 83407 0 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 534 16 2 4 7.7 CCCN(CCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
CHEMBL2206264 83407 0 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 534 16 2 4 7.7 CCCN(CCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
44554818 103776 0 None 89 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099234 103776 0 None 89 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
11761412 116438 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporationAgonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporation
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
CHEMBL338606 116438 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporationAgonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporation
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
119570 3098 90 None -34 7 Rat 8.8 pEC50 = 8.8 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 3098 90 None -34 7 Rat 8.8 pEC50 = 8.8 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 3098 90 None -34 7 Rat 8.8 pEC50 = 8.8 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 3098 90 None -34 7 Rat 8.8 pEC50 = 8.8 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 3098 90 None -34 7 Rat 8.8 pEC50 = 8.8 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
11983282 138401 0 None -2 3 Human 8.8 pEC50 = 8.8 Functional
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 138401 0 None -2 3 Human 8.8 pEC50 = 8.8 Functional
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
228 441 26 None -2 8 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 441 26 None -2 8 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 441 26 None -2 8 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 441 26 None -2 8 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 441 26 None -2 8 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
2 3198 19 None -12 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assayAgonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.8b00671
54562 3198 19 None -12 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assayAgonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.8b00671
CHEMBL240773 3198 19 None -12 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assayAgonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.8b00671
2 3198 19 None -12 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
54562 3198 19 None -12 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
CHEMBL240773 3198 19 None -12 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
56597940 153405 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 450 7 2 6 2.9 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCC(=O)N5)CC3)cc2N1 nan
CHEMBL3983588 153405 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 450 7 2 6 2.9 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCC(=O)N5)CC3)cc2N1 nan
2 3198 19 None -12 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
54562 3198 19 None -12 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
CHEMBL240773 3198 19 None -12 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
156785342 184270 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4852524 184270 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
11957566 183 20 None -52 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1007/s00044-004-0006-x
1219 183 20 None -52 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1007/s00044-004-0006-x
3296 183 20 None -52 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1007/s00044-004-0006-x
950 183 20 None -52 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1007/s00044-004-0006-x
CHEMBL285755 183 20 None -52 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1007/s00044-004-0006-x
156785342 184270 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4852524 184270 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
183812 204015 21 None -15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assayAgonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assay
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1021/ml4005232
CHEMBL82663 204015 21 None -15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assayAgonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assay
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1021/ml4005232
66559778 81544 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 423 9 1 5 4.0 CCOc1cccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c1 10.1021/jm300603y
CHEMBL2165123 81544 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 423 9 1 5 4.0 CCOc1cccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c1 10.1021/jm300603y
121418538 171016 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at dopamine D2long receptor (unknown origin) assessed as increased in cAMP accumulationAgonist activity at dopamine D2long receptor (unknown origin) assessed as increased in cAMP accumulation
ChEMBL 345 6 0 3 4.7 CC1(Oc2ccc(Cl)cc2)CCN(CCOc2ccccc2)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL4465147 171016 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at dopamine D2long receptor (unknown origin) assessed as increased in cAMP accumulationAgonist activity at dopamine D2long receptor (unknown origin) assessed as increased in cAMP accumulation
ChEMBL 345 6 0 3 4.7 CC1(Oc2ccc(Cl)cc2)CCN(CCOc2ccccc2)CC1 10.1021/acs.jmedchem.8b00435
11102013 11381 0 None - 1 Human 8.0 pEC50 = 8 Functional
Effective concentration for Dopamine receptor D3 was determinedEffective concentration for Dopamine receptor D3 was determined
ChEMBL 427 9 1 4 4.1 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(Cl)cc2)CC1 10.1021/jm030836n
CHEMBL1180455 11381 0 None - 1 Human 8.0 pEC50 = 8 Functional
Effective concentration for Dopamine receptor D3 was determinedEffective concentration for Dopamine receptor D3 was determined
ChEMBL 427 9 1 4 4.1 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(Cl)cc2)CC1 10.1021/jm030836n
CHEMBL126725 11381 0 None - 1 Human 8.0 pEC50 = 8 Functional
Effective concentration for Dopamine receptor D3 was determinedEffective concentration for Dopamine receptor D3 was determined
ChEMBL 427 9 1 4 4.1 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(Cl)cc2)CC1 10.1021/jm030836n
2 3198 19 None -12 7 Human 8.0 pEC50 = 8 Functional
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
54562 3198 19 None -12 7 Human 8.0 pEC50 = 8 Functional
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
CHEMBL240773 3198 19 None -12 7 Human 8.0 pEC50 = 8 Functional
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
164619589 185020 0 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 380 9 2 4 3.7 COc1ccccc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4863992 185020 0 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 380 9 2 4 3.7 COc1ccccc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
11978813 712 72 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
5014 712 72 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
7672 712 72 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
CHEMBL2105760 712 72 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
DB09128 712 72 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
146025775 169375 0 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 373 4 1 4 3.0 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cc4c(cc3C2)OCO4)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4441636 169375 0 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 373 4 1 4 3.0 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cc4c(cc3C2)OCO4)CC1 10.1021/acs.jmedchem.9b00508
46882009 6122 0 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 301 4 0 2 3.1 Cc1cccc(N2CCN(CCN3CCCCCC3)C2=O)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1081311 6122 0 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 301 4 0 2 3.1 Cc1cccc(N2CCN(CCN3CCCCCC3)C2=O)c1 10.1016/j.bmcl.2010.01.090
46882054 6149 0 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 305 4 0 2 2.9 O=C1N(CCN2CCCCCC2)CCN1c1ccc(F)cc1 10.1016/j.bmcl.2010.01.090
CHEMBL1081491 6149 0 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 305 4 0 2 2.9 O=C1N(CCN2CCCCCC2)CCN1c1ccc(F)cc1 10.1016/j.bmcl.2010.01.090
46881408 6665 0 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 339 4 0 2 3.6 O=C1N(CCN2CCCCCC2)CCN1c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1083813 6665 0 None - 1 Human 8.0 pEC50 = 8 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 339 4 0 2 3.6 O=C1N(CCN2CCCCCC2)CCN1c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2010.01.090
11978813 712 72 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
5014 712 72 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
7672 712 72 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
CHEMBL2105760 712 72 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
DB09128 712 72 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
128 149 9 None -50 3 Human 8.0 pEC50 = 8.0 Functional
Activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1016/j.bmc.2009.04.031
172267 149 9 None -50 3 Human 8.0 pEC50 = 8.0 Functional
Activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1016/j.bmc.2009.04.031
CHEMBL273273 149 9 None -50 3 Human 8.0 pEC50 = 8.0 Functional
Activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1016/j.bmc.2009.04.031
90467323 158999 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D2 receptor-short expressed in CHO-K1 cells assessed as reduction in adenylyl cyclase activator NKH 477 induced cAMP accumulation preincubated for 10 mins followed by NKH 477 addition by HTRF assayAgonist activity at human dopamine D2 receptor-short expressed in CHO-K1 cells assessed as reduction in adenylyl cyclase activator NKH 477 induced cAMP accumulation preincubated for 10 mins followed by NKH 477 addition by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4102620 158999 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D2 receptor-short expressed in CHO-K1 cells assessed as reduction in adenylyl cyclase activator NKH 477 induced cAMP accumulation preincubated for 10 mins followed by NKH 477 addition by HTRF assayAgonist activity at human dopamine D2 receptor-short expressed in CHO-K1 cells assessed as reduction in adenylyl cyclase activator NKH 477 induced cAMP accumulation preincubated for 10 mins followed by NKH 477 addition by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
10047648 115258 0 None 6 2 Human 8.0 pEC50 = 8.0 Functional
In vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptorIn vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptor
ChEMBL 418 4 1 4 4.0 O=C(N[C@@H]1CC[C@H]2C[C@@H](N3CCN(c4ccccn4)CC3)CC[C@@H]2C1)c1ccccc1 10.1021/jm00050a022
CHEMBL335403 115258 0 None 6 2 Human 8.0 pEC50 = 8.0 Functional
In vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptorIn vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptor
ChEMBL 418 4 1 4 4.0 O=C(N[C@@H]1CC[C@H]2C[C@@H](N3CCN(c4ccccn4)CC3)CC[C@@H]2C1)c1ccccc1 10.1021/jm00050a022
164616008 184720 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4859410 184720 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
146025779 170113 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 363 4 1 2 3.9 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(Cl)c3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4451797 170113 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 363 4 1 2 3.9 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(Cl)c3C2)CC1 10.1021/acs.jmedchem.9b00508
3949 3637 31 None 4 3 Rat 8.0 pEC50 = 8.0 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
ChEMBL 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/jm030505a
9818479 3637 31 None 4 3 Rat 8.0 pEC50 = 8.0 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
ChEMBL 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/jm030505a
CHEMBL419792 3637 31 None 4 3 Rat 8.0 pEC50 = 8.0 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
ChEMBL 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/jm030505a
DB06477 3637 31 None 4 3 Rat 8.0 pEC50 = 8.0 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
ChEMBL 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/jm030505a
2 3198 19 None -12 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.6b01875
54562 3198 19 None -12 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.6b01875
CHEMBL240773 3198 19 None -12 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.6b01875
163728602 185572 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4872467 185572 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
163728602 185572 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4872467 185572 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
119570 3098 90 None -9 7 Human 7.0 pEC50 = 7 Functional
Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.7b00363
2233 3098 90 None -9 7 Human 7.0 pEC50 = 7 Functional
Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.7b00363
953 3098 90 None -9 7 Human 7.0 pEC50 = 7 Functional
Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.7b00363
CHEMBL301265 3098 90 None -9 7 Human 7.0 pEC50 = 7 Functional
Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.7b00363
DB00413 3098 90 None -9 7 Human 7.0 pEC50 = 7 Functional
Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.7b00363
56599142 3867 3 None - 1 Human 7.0 pEC50 = 7 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 420 6 0 4 6.3 Clc1cccc(c1Cl)C1CCN(CC1)CCCOc1ccc2c(c1)ncs2 nan
7652 3867 3 None - 1 Human 7.0 pEC50 = 7 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 420 6 0 4 6.3 Clc1cccc(c1Cl)C1CCN(CC1)CCCOc1ccc2c(c1)ncs2 nan
CHEMBL2165138 3867 3 None - 1 Human 7.0 pEC50 = 7 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 420 6 0 4 6.3 Clc1cccc(c1Cl)C1CCN(CC1)CCCOc1ccc2c(c1)ncs2 nan
56597091 81554 0 None - 1 Human 7.0 pEC50 = 7 Functional
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 418 7 1 4 4.9 Clc1cccc(N2CCN(CCCCOc3ccc4cn[nH]c4c3)CC2)c1Cl 10.1021/jm300603y
CHEMBL2165134 81554 0 None - 1 Human 7.0 pEC50 = 7 Functional
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 418 7 1 4 4.9 Clc1cccc(N2CCN(CCCCOc3ccc4cn[nH]c4c3)CC2)c1Cl 10.1021/jm300603y
137651073 156914 0 None -36 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4079301 156914 0 None -36 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
56599147 81549 0 None - 1 Human 6.0 pEC50 = 6 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 443 4 1 4 4.1 O=C1CCc2ccc(OCC#CCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 nan
CHEMBL2165129 81549 0 None - 1 Human 6.0 pEC50 = 6 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 443 4 1 4 4.1 O=C1CCc2ccc(OCC#CCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 nan
137653359 158350 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 524 14 2 9 2.0 CN[C@@H]1Cc2cccc3c2n(c(=O)n3CCOCCOCCOCCOc2ccc3c(c2)NC(=O)CC3)C1 10.1021/acs.jmedchem.6b01875
CHEMBL4095452 158350 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 524 14 2 9 2.0 CN[C@@H]1Cc2cccc3c2n(c(=O)n3CCOCCOCCOCCOc2ccc3c(c2)NC(=O)CC3)C1 10.1021/acs.jmedchem.6b01875
122324 203 17 None -3235 4 Rat 5.0 pEC50 = 5.0 Functional
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
6077 203 17 None -3235 4 Rat 5.0 pEC50 = 5.0 Functional
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
CHEMBL86931 203 17 None -3235 4 Rat 5.0 pEC50 = 5.0 Functional
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
122324 203 17 None -3235 4 Rat 5.0 pEC50 = 5.0 Functional
Formation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobeFormation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobe
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
6077 203 17 None -3235 4 Rat 5.0 pEC50 = 5.0 Functional
Formation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobeFormation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobe
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
CHEMBL86931 203 17 None -3235 4 Rat 5.0 pEC50 = 5.0 Functional
Formation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobeFormation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobe
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
151086 91532 4 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to controlAgonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to control
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1021/acs.jnatprod.9b00921
CHEMBL2414991 91532 4 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to controlAgonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to control
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1021/acs.jnatprod.9b00921
151086 91532 4 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to controlAgonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to control
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1021/acs.jnatprod.9b00921
CHEMBL2414991 91532 4 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to controlAgonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to control
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1021/acs.jnatprod.9b00921
164612037 184785 0 None -181 12 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4860528 184785 0 None -181 12 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
56599143 81558 3 None - 1 Human 7.0 pEC50 = 7.0 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 421 6 0 5 5.2 Clc1cccc(N2CCN(CCCOc3ccc4scnc4c3)CC2)c1Cl nan
CHEMBL2165139 81558 3 None - 1 Human 7.0 pEC50 = 7.0 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 421 6 0 5 5.2 Clc1cccc(N2CCN(CCCOc3ccc4scnc4c3)CC2)c1Cl nan
137657115 159196 0 None -11 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4105030 159196 0 None -11 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
164609493 183844 0 None -109 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4846380 183844 0 None -109 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
16038360 16773 0 None -104 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2ccc(O)cc2C1 10.1016/j.bmc.2010.06.025
CHEMBL1253770 16773 0 None -104 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2ccc(O)cc2C1 10.1016/j.bmc.2010.06.025
15696481 79241 0 None -75 2 Rat 5.0 pEC50 = 5.0 Functional
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL2115213 79241 0 None -75 2 Rat 5.0 pEC50 = 5.0 Functional
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
25071692 111284 0 None -9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287405 111284 0 None -9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
122189392 122718 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613878 122718 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
164611757 184310 0 None -12 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4853107 184310 0 None -12 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
164616008 184720 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4859410 184720 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
146025779 170113 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 363 4 1 2 3.9 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(Cl)c3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4451797 170113 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 363 4 1 2 3.9 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(Cl)c3C2)CC1 10.1021/acs.jmedchem.9b00508
56597226 147866 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 410 8 1 6 3.0 COc1ccccc1N1CCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
CHEMBL3937643 147866 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 410 8 1 6 3.0 COc1ccccc1N1CCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
164617831 184137 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 378 9 2 4 3.7 COc1ccccc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4850635 184137 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 378 9 2 4 3.7 COc1ccccc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164617831 184137 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 378 9 2 4 3.7 COc1ccccc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4850635 184137 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 378 9 2 4 3.7 COc1ccccc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
127046952 139558 0 None 87 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800636 139558 0 None 87 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
11154555 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
5037 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
7671 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL2028019 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL3085826 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB06016 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
25071692 111284 0 None -9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287405 111284 0 None -9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
52937876 60831 0 None -489 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP accumulation by bioluminescence assayAgonist activity at human dopamine D2long receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP accumulation by bioluminescence assay
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765633 60831 0 None -489 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP accumulation by bioluminescence assayAgonist activity at human dopamine D2long receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP accumulation by bioluminescence assay
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
122177641 120683 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577342 120683 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
137657115 159196 0 None -11 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4105030 159196 0 None -11 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
11154555 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
5037 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
7671 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL2028019 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL3085826 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB06016 786 57 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
118725996 116687 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 572 21 3 5 6.4 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394254 116687 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 572 21 3 5 6.4 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
122189393 122719 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613879 122719 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
168273640 192193 0 None -16 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D2 long receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD2longR-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D2 long receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD2longR-ElucC by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176229 192193 0 None -16 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D2 long receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD2longR-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D2 long receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD2longR-ElucC by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 192193 0 None -16 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D2 long receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD2longR-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D2 long receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD2longR-ElucC by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
164617783 183997 0 None -27 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4848815 183997 0 None -27 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
60148494 80433 0 None -446 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL2152747 80433 0 None -446 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
44427818 91677 0 None -38 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 444 9 1 5 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
CHEMBL241973 91677 0 None -38 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 444 9 1 5 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
118725996 116687 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 572 21 3 5 6.4 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394254 116687 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 572 21 3 5 6.4 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
60165801 80432 0 None -446 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)C1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
CHEMBL2152746 80432 0 None -446 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)C1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
14659268 79213 2 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 297 1 2 4 2.9 COc1cc2c3c(c1)-c1c(ccc(O)c1O)CC3N(C)CC2 10.1016/j.bmc.2008.02.038
CHEMBL2115032 79213 2 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 297 1 2 4 2.9 COc1cc2c3c(c1)-c1c(ccc(O)c1O)CC3N(C)CC2 10.1016/j.bmc.2008.02.038
45486330 196105 0 None -173 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL571992 196105 0 None -173 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
45486330 196105 0 None -173 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
CHEMBL571992 196105 0 None -173 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
45486330 196105 0 None -173 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
CHEMBL571992 196105 0 None -173 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
25093832 155327 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155327 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
44241577 13885 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation countingAgonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting
ChEMBL 387 3 3 4 5.0 CCCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1197140 13885 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation countingAgonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting
ChEMBL 387 3 3 4 5.0 CCCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL560721 13885 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation countingAgonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting
ChEMBL 387 3 3 4 5.0 CCCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
119570 3098 90 None -34 7 Rat 7.9 pEC50 = 7.9 Functional
Effective concentration required for agonistic activity against rat D2 short receptorEffective concentration required for agonistic activity against rat D2 short receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2233 3098 90 None -34 7 Rat 7.9 pEC50 = 7.9 Functional
Effective concentration required for agonistic activity against rat D2 short receptorEffective concentration required for agonistic activity against rat D2 short receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
953 3098 90 None -34 7 Rat 7.9 pEC50 = 7.9 Functional
Effective concentration required for agonistic activity against rat D2 short receptorEffective concentration required for agonistic activity against rat D2 short receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
CHEMBL301265 3098 90 None -34 7 Rat 7.9 pEC50 = 7.9 Functional
Effective concentration required for agonistic activity against rat D2 short receptorEffective concentration required for agonistic activity against rat D2 short receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
DB00413 3098 90 None -34 7 Rat 7.9 pEC50 = 7.9 Functional
Effective concentration required for agonistic activity against rat D2 short receptorEffective concentration required for agonistic activity against rat D2 short receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
72736203 103069 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 329 4 1 2 3.3 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL3085802 103069 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 329 4 1 2 3.3 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
10939167 9394 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrsPartial agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrs
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
CHEMBL112065 9394 0 None - 1 Human 7.9