Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Assay
Type

 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
57383409 109935 None 0 Human Functional pAC50 = 7.0 7.0 - 1
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 109935 None 0 Human Functional pAC50 = 7.0 7.0 - 1
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 109961 None 0 Human Functional pAC50 = 7.0 7.0 - 1
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 109961 None 0 Human Functional pAC50 = 7.0 7.0 - 1
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 109974 None 0 Human Functional pAC50 = 7.0 7.0 - 1
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 109974 None 0 Human Functional pAC50 = 7.0 7.0 - 1
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 109982 None 0 Human Functional pAC50 = 7.0 7.0 9 2
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 109982 None 0 Human Functional pAC50 = 7.0 7.0 9 2
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 109970 None 0 Human Functional pAC50 = 5.0 5.0 - 1
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 109970 None 0 Human Functional pAC50 = 5.0 5.0 - 1
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 109952 None 0 Human Functional pAC50 = 6.9 6.9 - 1
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 109952 None 0 Human Functional pAC50 = 6.9 6.9 - 1
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 109953 None 0 Human Functional pAC50 = 6.9 6.9 - 1
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 109953 None 0 Human Functional pAC50 = 6.9 6.9 - 1
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 109958 None 0 Human Functional pAC50 = 6.9 6.9 - 1
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 109958 None 0 Human Functional pAC50 = 6.9 6.9 - 1
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 109967 None 0 Human Functional pAC50 = 6.9 6.9 - 1
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 109967 None 0 Human Functional pAC50 = 6.9 6.9 - 1
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 109977 None 0 Human Functional pAC50 = 6.9 6.9 7 2
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 109977 None 0 Human Functional pAC50 = 6.9 6.9 7 2
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 109963 None 0 Human Functional pAC50 = 5.8 5.8 - 1
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 109963 None 0 Human Functional pAC50 = 5.8 5.8 - 1
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 45659 None 5 Human Functional pAC50 = 6.8 6.8 - 1
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 45659 None 5 Human Functional pAC50 = 6.8 6.8 - 1
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 109955 None 0 Human Functional pAC50 = 5.8 5.8 - 1
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 109955 None 0 Human Functional pAC50 = 5.8 5.8 - 1
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 109950 None 0 Human Functional pAC50 = 6.7 6.7 - 1
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 109950 None 0 Human Functional pAC50 = 6.7 6.7 - 1
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 109965 None 0 Human Functional pAC50 = 6.7 6.7 - 1
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 109965 None 0 Human Functional pAC50 = 6.7 6.7 - 1
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 109980 None 0 Human Functional pAC50 = 6.7 6.7 - 1
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 109980 None 0 Human Functional pAC50 = 6.7 6.7 - 1
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 109983 None 0 Human Functional pAC50 = 6.7 6.7 16 2
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 109983 None 0 Human Functional pAC50 = 6.7 6.7 16 2
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 42914 None 2 Human Functional pAC50 = 6.6 6.6 6 2
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 42914 None 2 Human Functional pAC50 = 6.6 6.6 6 2
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 109986 None 0 Human Functional pAC50 = 6.6 6.6 11 2
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 109986 None 0 Human Functional pAC50 = 6.6 6.6 11 2
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 109968 None 0 Human Functional pAC50 = 6.6 6.6 - 1
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 109968 None 0 Human Functional pAC50 = 6.6 6.6 - 1
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 109971 None 0 Human Functional pAC50 = 6.6 6.6 - 1
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 109971 None 0 Human Functional pAC50 = 6.6 6.6 - 1
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 109951 None 0 Human Functional pAC50 = 6.5 6.5 - 1
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 109951 None 0 Human Functional pAC50 = 6.5 6.5 - 1
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 109954 None 0 Human Functional pAC50 = 6.5 6.5 - 1
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 109954 None 0 Human Functional pAC50 = 6.5 6.5 - 1
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 109956 None 2 Human Functional pAC50 = 6.5 6.5 - 1
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 109956 None 2 Human Functional pAC50 = 6.5 6.5 - 1
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 109959 None 0 Human Functional pAC50 = 6.5 6.5 - 1
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 109959 None 0 Human Functional pAC50 = 6.5 6.5 - 1
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 109964 None 0 Human Functional pAC50 = 6.5 6.5 - 1
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 109964 None 0 Human Functional pAC50 = 6.5 6.5 - 1
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 109966 None 0 Human Functional pAC50 = 6.5 6.5 - 1
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 109966 None 0 Human Functional pAC50 = 6.5 6.5 - 1
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 109984 None 0 Human Functional pAC50 = 6.5 6.5 32 2
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 109984 None 0 Human Functional pAC50 = 6.5 6.5 32 2
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 109936 None 0 Human Functional pAC50 = 6.4 6.4 - 1
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 109936 None 0 Human Functional pAC50 = 6.4 6.4 - 1
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 109988 None 0 Human Functional pAC50 = 6.4 6.4 12 2
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 109988 None 0 Human Functional pAC50 = 6.4 6.4 12 2
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 59813 None 5 Human Functional pAC50 = 5.4 5.4 - 1
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 59813 None 5 Human Functional pAC50 = 5.4 5.4 - 1
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 59504 None 5 Human Functional pAC50 = 6.3 6.3 - 1
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 59504 None 5 Human Functional pAC50 = 6.3 6.3 - 1
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 109981 None 0 Human Functional pAC50 = 7.3 7.3 18 2
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 109981 None 0 Human Functional pAC50 = 7.3 7.3 18 2
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 109949 None 1 Human Functional pAC50 = 6.3 6.3 - 1
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 109949 None 1 Human Functional pAC50 = 6.3 6.3 - 1
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 109975 None 0 Human Functional pAC50 = 6.3 6.3 - 1
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 109975 None 0 Human Functional pAC50 = 6.3 6.3 - 1
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 109978 None 0 Human Functional pAC50 = 4.3 4.3 - 1
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 109978 None 0 Human Functional pAC50 = 4.3 4.3 - 1
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 2572 None 1 Human Functional pAC50 = 7.2 7.2 57 2
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 2572 None 1 Human Functional pAC50 = 7.2 7.2 57 2
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 2572 None 1 Human Functional pAC50 = 7.2 7.2 57 2
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 109989 None 0 Human Functional pAC50 = 7.2 7.2 28 2
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 109989 None 0 Human Functional pAC50 = 7.2 7.2 28 2
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 109962 None 0 Human Functional pAC50 = 6.2 6.2 - 1
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 109962 None 0 Human Functional pAC50 = 6.2 6.2 - 1
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 109976 None 0 Human Functional pAC50 = 6.2 6.2 - 1
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 109976 None 0 Human Functional pAC50 = 6.2 6.2 - 1
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 109979 None 0 Human Functional pAC50 = 6.2 6.2 - 1
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 109979 None 0 Human Functional pAC50 = 6.2 6.2 - 1
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 109969 None 0 Human Functional pAC50 = 7.2 7.2 - 1
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 109969 None 0 Human Functional pAC50 = 7.2 7.2 - 1
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 109957 None 0 Human Functional pAC50 = 6.1 6.1 - 1
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 109957 None 0 Human Functional pAC50 = 6.1 6.1 - 1
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 109960 None 0 Human Functional pAC50 = 6.1 6.1 - 1
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 109960 None 0 Human Functional pAC50 = 6.1 6.1 - 1
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 59280 None 5 Human Functional pAC50 = 5.1 5.1 - 1
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 59280 None 5 Human Functional pAC50 = 5.1 5.1 - 1
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 67517 None 1 Human Functional pAC50 = 7.1 7.1 - 1
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 67517 None 1 Human Functional pAC50 = 7.1 7.1 - 1
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 109972 None 0 Human Functional pAC50 = 7.1 7.1 70 2
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 109972 None 0 Human Functional pAC50 = 7.1 7.1 70 2
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 109973 None 0 Human Functional pAC50 = 7.1 7.1 - 1
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 109973 None 0 Human Functional pAC50 = 7.1 7.1 - 1
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 109987 None 0 Human Functional pAC50 = 7.1 7.1 15 2
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 109987 None 0 Human Functional pAC50 = 7.1 7.1 15 2
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 210628 None 0 Rat Functional pEC50 = 10.9 10.9 - 1
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 210628 None 0 Rat Functional pEC50 = 10.9 10.9 - 1
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 205703 None 0 Human Functional pEC50 = 10.7 10.7 - 1
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 205703 None 0 Human Functional pEC50 = 10.7 10.7 - 1
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 205703 None 0 Human Functional pEC50 = 10.7 10.7 - 1
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 106478 None 0 Human Functional pEC50 = 10.5 10.5 - 1
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 106478 None 0 Human Functional pEC50 = 10.5 10.5 - 1
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 106478 None 0 Human Functional pEC50 = 10.5 10.5 - 1
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 2876 None 8 Human Functional pEC50 = 10.4 10.4 6 4
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 2876 None 8 Human Functional pEC50 = 10.4 10.4 6 4
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 2876 None 8 Human Functional pEC50 = 10.4 10.4 6 4
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 2876 None 8 Human Functional pEC50 = 10.4 10.4 6 4
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 2876 None 8 Human Functional pEC50 = 10.4 10.4 6 4
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 2876 None 8 Human Functional pEC50 = 10.4 10.4 6 4
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 106446 None 0 Human Functional pEC50 = 10.3 10.3 - 1
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 106446 None 0 Human Functional pEC50 = 10.3 10.3 - 1
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 106446 None 0 Human Functional pEC50 = 10.3 10.3 - 1
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 159768 None 0 Human Functional pEC50 = 10.0 10.0 12589 2
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 159768 None 0 Human Functional pEC50 = 10.0 10.0 12589 2
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 159768 None 0 Human Functional pEC50 = 10.0 10.0 12589 2
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 159768 None 0 Human Functional pEC50 = 10.0 10.0 12589 2
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 146516 None 0 Human Functional pEC50 = 10 10.0 - 1
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 146516 None 0 Human Functional pEC50 = 10 10.0 - 1
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
172471847 197200 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 406 10 2 5 4.6 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5441140 197200 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 406 10 2 5 4.6 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
172471847 197200 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 406 10 2 5 4.6 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5441140 197200 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 406 10 2 5 4.6 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
44554472 106339 None 0 Human Functional pEC50 = 9.9 9.9 1071 2
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 106339 None 0 Human Functional pEC50 = 9.9 9.9 1071 2
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 106339 None 0 Human Functional pEC50 = 9.9 9.9 1071 2
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 106428 None 0 Human Functional pEC50 = 9.8 9.8 - 1
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 106428 None 0 Human Functional pEC50 = 9.8 9.8 - 1
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 106428 None 0 Human Functional pEC50 = 9.8 9.8 - 1
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 174609 None 0 Human Functional pEC50 = 9.8 9.8 489 2
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 174609 None 0 Human Functional pEC50 = 9.8 9.8 489 2
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 174609 None 0 Human Functional pEC50 = 9.8 9.8 489 2
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 153422 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 153422 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 139629 None 9 Human Functional pEC50 = 9.7 9.7 -1 3
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 139629 None 9 Human Functional pEC50 = 9.7 9.7 -1 3
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
172471847 197200 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 406 10 2 5 4.6 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5441140 197200 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 406 10 2 5 4.6 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
172471847 197200 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 406 10 2 5 4.6 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5441140 197200 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 406 10 2 5 4.6 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
137460109 191492 None 0 Human Functional pEC50 = 9.6 9.6 3 2
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 191492 None 0 Human Functional pEC50 = 9.6 9.6 3 2
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
171492446 196607 None 0 Human Functional pEC50 = 9.6 9.6 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
CHEMBL5427695 196607 None 0 Human Functional pEC50 = 9.6 9.6 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
132578416 173910 None 0 Human Functional pEC50 = 9.6 9.6 1 2
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 173910 None 0 Human Functional pEC50 = 9.6 9.6 1 2
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
171492446 196607 None 0 Human Functional pEC50 = 9.6 9.6 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
CHEMBL5427695 196607 None 0 Human Functional pEC50 = 9.6 9.6 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
17449900 139629 None 9 Human Functional pEC50 = 9.6 9.6 -1 3
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 139629 None 9 Human Functional pEC50 = 9.6 9.6 -1 3
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 139799 None 0 Human Functional pEC50 = 9.5 9.5 5 2
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 139799 None 0 Human Functional pEC50 = 9.5 9.5 5 2
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 112569 None 11 Human Functional pEC50 = 9.5 9.5 - 1
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 112569 None 11 Human Functional pEC50 = 9.5 9.5 - 1
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 54075 None 2 Human Functional pEC50 = 9.5 9.5 - 1
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 54075 None 2 Human Functional pEC50 = 9.5 9.5 - 1
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 139799 None 0 Human Functional pEC50 = 9.5 9.5 5 2
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 139799 None 0 Human Functional pEC50 = 9.5 9.5 5 2
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
172468042 196585 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 404 6 1 5 4.1 COc1cccc2c3c(oc12)CN(CCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5427288 196585 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 404 6 1 5 4.1 COc1cccc2c3c(oc12)CN(CCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
172468042 196585 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 404 6 1 5 4.1 COc1cccc2c3c(oc12)CN(CCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5427288 196585 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 404 6 1 5 4.1 COc1cccc2c3c(oc12)CN(CCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
219050 3373 None 19 Human Functional pEC50 = 9.4 9.4 2 5
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 3373 None 19 Human Functional pEC50 = 9.4 9.4 2 5
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 3373 None 19 Human Functional pEC50 = 9.4 9.4 2 5
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 174631 None 2 Human Functional pEC50 = 9.4 9.4 616 2
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 174631 None 2 Human Functional pEC50 = 9.4 9.4 616 2
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 174631 None 2 Human Functional pEC50 = 9.4 9.4 616 2
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 174631 None 2 Human Functional pEC50 = 9.4 9.4 616 2
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 106427 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 106427 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 106427 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 53739 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 53739 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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
228 445 None 20 Rat Functional pEC50 = 9.4 9.4 -4 20
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
33 445 None 20 Rat Functional pEC50 = 9.4 9.4 -4 20
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 445 None 20 Rat Functional pEC50 = 9.4 9.4 -4 20
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
6005.0 445 None 20 Rat Functional pEC50 = 9.4 9.4 -4 20
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 445 None 20 Rat Functional pEC50 = 9.4 9.4 -4 20
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 445 None 20 Rat Functional pEC50 = 9.4 9.4 -4 20
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 154040 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 154040 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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
11154555.0 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 145285 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 145285 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 156716 None 0 Human Functional pEC50 = 9.4 9.4 -12 2
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 156716 None 0 Human Functional pEC50 = 9.4 9.4 -12 2
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 156716 None 0 Human Functional pEC50 = 9.4 9.4 -12 2
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 156716 None 0 Human Functional pEC50 = 9.4 9.4 -12 2
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 83870 None 0 Human Functional pEC50 = 9.4 9.4 2 2
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 83870 None 0 Human Functional pEC50 = 9.4 9.4 2 2
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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
11154555.0 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 800 None 50 Human Functional pEC50 = 9.4 9.4 1 10
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 104322 None 0 Human Functional pEC50 = 9.3 9.3 457 2
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 104322 None 0 Human Functional pEC50 = 9.3 9.3 457 2
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 53670 None 3 Human Functional pEC50 = 9.3 9.3 - 1
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 53670 None 3 Human Functional pEC50 = 9.3 9.3 - 1
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 53670 None 3 Human Functional pEC50 = 9.3 9.3 - 1
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 61194 None 0 Human Functional pEC50 = 9.3 9.3 -489 2
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 61194 None 0 Human Functional pEC50 = 9.3 9.3 -489 2
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 106342 None 0 Human Functional pEC50 = 9.2 9.2 31 2
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 106342 None 0 Human Functional pEC50 = 9.2 9.2 31 2
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 106342 None 0 Human Functional pEC50 = 9.2 9.2 31 2
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 145285 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 145285 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 53670 None 3 Human Functional pEC50 = 9.2 9.2 - 1
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 53670 None 3 Human Functional pEC50 = 9.2 9.2 - 1
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 53670 None 3 Human Functional pEC50 = 9.2 9.2 - 1
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 1465 None 47 Human Functional pEC50 = 9.2 9.2 -19 15
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
681.0 1465 None 47 Human Functional pEC50 = 9.2 9.2 -19 15
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 1465 None 47 Human Functional pEC50 = 9.2 9.2 -19 15
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 1465 None 47 Human Functional pEC50 = 9.2 9.2 -19 15
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 1465 None 47 Human Functional pEC50 = 9.2 9.2 -19 15
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 1465 None 47 Human Functional pEC50 = 9.2 9.2 -19 15
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 106459 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 106459 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 106459 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 6241 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 6241 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 7220 None 0 Human Functional pEC50 = 9.2 9.2 794 3
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 7220 None 0 Human Functional pEC50 = 9.2 9.2 794 3
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 173423 None 19 Human Functional pEC50 = 9.2 9.2 - 1
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 173423 None 19 Human Functional pEC50 = 9.2 9.2 - 1
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 155822 None 0 Human Functional pEC50 = 9.2 9.2 38 2
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 155822 None 0 Human Functional pEC50 = 9.2 9.2 38 2
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 3372 None 50 Human Functional pEC50 = 9.2 9.2 -1 17
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 3372 None 50 Human Functional pEC50 = 9.2 9.2 -1 17
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
59227.0 3372 None 50 Human Functional pEC50 = 9.2 9.2 -1 17
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 3372 None 50 Human Functional pEC50 = 9.2 9.2 -1 17
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 3372 None 50 Human Functional pEC50 = 9.2 9.2 -1 17
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 3372 None 50 Human Functional pEC50 = 9.2 9.2 -1 17
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 173423 None 19 Human Functional pEC50 = 9.2 9.2 - 1
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 173423 None 19 Human Functional pEC50 = 9.2 9.2 - 1
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 155970 None 0 Human Functional pEC50 = 9.1 9.1 2 2
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 155970 None 0 Human Functional pEC50 = 9.1 9.1 2 2
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 155970 None 0 Human Functional pEC50 = 9.1 9.1 2 2
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 155970 None 0 Human Functional pEC50 = 9.1 9.1 2 2
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
172444647 195417 None 0 Human Functional pEC50 = 9.1 9.1 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5403268 195417 None 0 Human Functional pEC50 = 9.1 9.1 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
172444647 195417 None 0 Human Functional pEC50 = 9.1 9.1 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5403268 195417 None 0 Human Functional pEC50 = 9.1 9.1 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
46882053 6242 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 6242 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 54075 None 2 Human Functional pEC50 = 9.1 9.1 - 1
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 54075 None 2 Human Functional pEC50 = 9.1 9.1 - 1
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 54441 None 2 Human Functional pEC50 = 9.1 9.1 - 1
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 54441 None 2 Human Functional pEC50 = 9.1 9.1 - 1
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 169585 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 169585 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 1465 None 47 Human Functional pEC50 = 9.1 9.1 -19 15
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
681.0 1465 None 47 Human Functional pEC50 = 9.1 9.1 -19 15
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 1465 None 47 Human Functional pEC50 = 9.1 9.1 -19 15
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 1465 None 47 Human Functional pEC50 = 9.1 9.1 -19 15
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 1465 None 47 Human Functional pEC50 = 9.1 9.1 -19 15
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 1465 None 47 Human Functional pEC50 = 9.1 9.1 -19 15
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 53739 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 53739 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 106324 None 0 Human Functional pEC50 = 9.1 9.1 151 2
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 106324 None 0 Human Functional pEC50 = 9.1 9.1 151 2
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 106324 None 0 Human Functional pEC50 = 9.1 9.1 151 2
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
172460748 196159 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 392 9 2 5 4.2 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5417857 196159 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 392 9 2 5 4.2 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
172460748 196159 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 392 9 2 5 4.2 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5417857 196159 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 392 9 2 5 4.2 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
66633662 152105 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 152105 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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
2 3261 None 19 Human Functional pEC50 = 9.0 9.0 -10 7
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
54562 3261 None 19 Human Functional pEC50 = 9.0 9.0 -10 7
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
CHEMBL240773 3261 None 19 Human Functional pEC50 = 9.0 9.0 -10 7
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
2 3261 None 19 Human Functional pEC50 = 9.0 9.0 -10 7
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
54562 3261 None 19 Human Functional pEC50 = 9.0 9.0 -10 7
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
CHEMBL240773 3261 None 19 Human Functional pEC50 = 9.0 9.0 -10 7
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
131801153 170096 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 170096 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 1465 None 47 Human Functional pEC50 = 9 9.0 -19 15
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
681.0 1465 None 47 Human Functional pEC50 = 9 9.0 -19 15
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 1465 None 47 Human Functional pEC50 = 9 9.0 -19 15
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 1465 None 47 Human Functional pEC50 = 9 9.0 -19 15
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 1465 None 47 Human Functional pEC50 = 9 9.0 -19 15
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 1465 None 47 Human Functional pEC50 = 9 9.0 -19 15
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
242 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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
34 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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
60795.0 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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 104318 None 0 Human Functional pEC50 = 9 9.0 208 2
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 104318 None 0 Human Functional pEC50 = 9 9.0 208 2
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 139652 None 0 Human Functional pEC50 = 9 9.0 -1 2
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 139652 None 0 Human Functional pEC50 = 9 9.0 -1 2
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
242 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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
34 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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
60795.0 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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 470 None 70 Human Functional pEC50 = 9 9.0 -5 33
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 5606 None 0 Human Functional pEC50 = 9 9.0 - 1
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 5606 None 0 Human Functional pEC50 = 9 9.0 - 1
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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
11154555.0 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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
11154555.0 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 800 None 50 Human Functional pEC50 = 9.0 9.0 1 10
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 106341 None 0 Human Functional pEC50 = 9.0 9.0 301 2
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 106341 None 0 Human Functional pEC50 = 9.0 9.0 301 2
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 106341 None 0 Human Functional pEC50 = 9.0 9.0 301 2
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 1465 None 47 Rat Functional pEC50 = 9.0 9.0 -288 15
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
681.0 1465 None 47 Rat Functional pEC50 = 9.0 9.0 -288 15
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 1465 None 47 Rat Functional pEC50 = 9.0 9.0 -288 15
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 1465 None 47 Rat Functional pEC50 = 9.0 9.0 -288 15
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 1465 None 47 Rat Functional pEC50 = 9.0 9.0 -288 15
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 1465 None 47 Rat Functional pEC50 = 9.0 9.0 -288 15
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
172450959 195711 None 0 Human Functional pEC50 = 8.9 8.9 22 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 195711 None 0 Human Functional pEC50 = 8.9 8.9 22 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
2 3261 None 19 Human Functional pEC50 = 8.9 8.9 -10 7
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 3261 None 19 Human Functional pEC50 = 8.9 8.9 -10 7
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 3261 None 19 Human Functional pEC50 = 8.9 8.9 -10 7
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
172450959 195711 None 0 Human Functional pEC50 = 8.9 8.9 22 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 195711 None 0 Human Functional pEC50 = 8.9 8.9 22 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
2 3261 None 19 Human Functional pEC50 = 8.9 8.9 -10 7
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 3261 None 19 Human Functional pEC50 = 8.9 8.9 -10 7
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 3261 None 19 Human Functional pEC50 = 8.9 8.9 -10 7
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 3261 None 19 Human Functional pEC50 = 8.9 8.9 -10 7
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 3261 None 19 Human Functional pEC50 = 8.9 8.9 -10 7
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 3261 None 19 Human Functional pEC50 = 8.9 8.9 -10 7
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
11154555 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
11154555.0 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
5037 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
7671 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
CHEMBL2028019 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
CHEMBL3085826 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
DB06016 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
11154555 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
11154555.0 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
5037 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
7671 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
CHEMBL2028019 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
CHEMBL3085826 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
DB06016 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
11154555 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
11154555.0 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
5037 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
7671 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
CHEMBL2028019 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
CHEMBL3085826 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
DB06016 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
11154555 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
11154555.0 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
5037 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
7671 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
CHEMBL2028019 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
CHEMBL3085826 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
DB06016 800 None 50 Human Functional pEC50 = 8.9 8.9 1 10
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
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.2c01624
2470 3653 None 40 Human Functional pEC50 = 8.9 8.9 -14 23
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 3653 None 40 Human Functional pEC50 = 8.9 8.9 -14 23
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 3653 None 40 Human Functional pEC50 = 8.9 8.9 -14 23
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 3653 None 40 Human Functional pEC50 = 8.9 8.9 -14 23
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 3653 None 40 Human Functional pEC50 = 8.9 8.9 -14 23
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 104317 None 0 Human Functional pEC50 = 8.8 8.8 58 2
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 104317 None 0 Human Functional pEC50 = 8.8 8.8 58 2
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 153896 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 153896 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 154690 None 0 Human Functional pEC50 = 8.8 8.8 -19 2
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 154690 None 0 Human Functional pEC50 = 8.8 8.8 -19 2
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
228 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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
33 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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
6005.0 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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 106433 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 106433 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 106433 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 185707 None 0 Human Functional pEC50 = 8.8 8.8 10 3
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 185707 None 0 Human Functional pEC50 = 8.8 8.8 10 3
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 3941 None 6 Human Functional pEC50 = 8.8 8.8 602 2
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 3941 None 6 Human Functional pEC50 = 8.8 8.8 602 2
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 3941 None 6 Human Functional pEC50 = 8.8 8.8 602 2
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
164619170 185707 None 0 Human Functional pEC50 = 8.8 8.8 10 3
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 185707 None 0 Human Functional pEC50 = 8.8 8.8 10 3
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
156785362 184992 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Partial agonist activity at D2R (unknown origin) expressed in HEK293 cellsPartial agonist activity at D2R (unknown origin) expressed in HEK293 cells
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1016/j.bmcl.2024.129654
CHEMBL4852835 184992 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Partial agonist activity at D2R (unknown origin) expressed in HEK293 cellsPartial agonist activity at D2R (unknown origin) expressed in HEK293 cells
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1016/j.bmcl.2024.129654
228 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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
33 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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
6005.0 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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 445 None 20 Human Functional pEC50 = 8.8 8.8 -3 20
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 203114 None 0 Human Functional pEC50 = 8.8 8.8 -2 2
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 203114 None 0 Human Functional pEC50 = 8.8 8.8 -2 2
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
169410194 196730 None 6 Human Functional pEC50 = 8.8 8.8 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5431103 196730 None 6 Human Functional pEC50 = 8.8 8.8 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
71459659 83869 None 0 Human Functional pEC50 = 8.8 8.8 -3 2
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 83869 None 0 Human Functional pEC50 = 8.8 8.8 -3 2
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 104321 None 0 Human Functional pEC50 = 8.8 8.8 89 2
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 104321 None 0 Human Functional pEC50 = 8.8 8.8 89 2
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 117015 None 0 Human Functional pEC50 = 8.8 8.8 2 2
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 117015 None 0 Human Functional pEC50 = 8.8 8.8 2 2
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 3159 None 58 Rat Functional pEC50 = 8.8 8.8 -34 11
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
119570.0 3159 None 58 Rat Functional pEC50 = 8.8 8.8 -34 11
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 3159 None 58 Rat Functional pEC50 = 8.8 8.8 -34 11
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 3159 None 58 Rat Functional pEC50 = 8.8 8.8 -34 11
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 3159 None 58 Rat Functional pEC50 = 8.8 8.8 -34 11
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 3159 None 58 Rat Functional pEC50 = 8.8 8.8 -34 11
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 139030 None 0 Human Functional pEC50 = 8.8 8.8 -2 3
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 139030 None 0 Human Functional pEC50 = 8.8 8.8 -2 3
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
169410194 196730 None 6 Human Functional pEC50 = 8.8 8.8 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5431103 196730 None 6 Human Functional pEC50 = 8.8 8.8 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
228 445 None 20 Human Functional pEC50 = 8.7 8.7 -3 20
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
33 445 None 20 Human Functional pEC50 = 8.7 8.7 -3 20
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 445 None 20 Human Functional pEC50 = 8.7 8.7 -3 20
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
6005.0 445 None 20 Human Functional pEC50 = 8.7 8.7 -3 20
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 445 None 20 Human Functional pEC50 = 8.7 8.7 -3 20
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 445 None 20 Human Functional pEC50 = 8.7 8.7 -3 20
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 3261 None 19 Human Functional pEC50 = 8.7 8.7 -10 7
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 3261 None 19 Human Functional pEC50 = 8.7 8.7 -10 7
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 3261 None 19 Human Functional pEC50 = 8.7 8.7 -10 7
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 3261 None 19 Human Functional pEC50 = 8.7 8.7 -10 7
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 3261 None 19 Human Functional pEC50 = 8.7 8.7 -10 7
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 3261 None 19 Human Functional pEC50 = 8.7 8.7 -10 7
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 154040 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 154040 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 3261 None 19 Human Functional pEC50 = 8.7 8.7 -10 7
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 3261 None 19 Human Functional pEC50 = 8.7 8.7 -10 7
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 3261 None 19 Human Functional pEC50 = 8.7 8.7 -10 7
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 184969 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 184969 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 184 None 17 Rat Functional pEC50 = 8.7 8.7 -52 4
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 184 None 17 Rat Functional pEC50 = 8.7 8.7 -52 4
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 184 None 17 Rat Functional pEC50 = 8.7 8.7 -52 4
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
950 184 None 17 Rat Functional pEC50 = 8.7 8.7 -52 4
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 184 None 17 Rat Functional pEC50 = 8.7 8.7 -52 4
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 184969 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 184969 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 208197 None 20 Human Functional pEC50 = 8.7 8.7 -15 2
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 208197 None 20 Human Functional pEC50 = 8.7 8.7 -15 2
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
172460539 196501 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 9 2 5 4.3 COc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5425434 196501 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 9 2 5 4.3 COc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
66559778 82001 None 0 Human Functional pEC50 = 8 8.0 - 1
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 82001 None 0 Human Functional pEC50 = 8 8.0 - 1
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 171695 None 0 Human Functional pEC50 = 8 8.0 - 1
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 171695 None 0 Human Functional pEC50 = 8 8.0 - 1
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 11505 None 0 Human Functional pEC50 = 8 8.0 - 1
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 11505 None 0 Human Functional pEC50 = 8 8.0 - 1
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 11505 None 0 Human Functional pEC50 = 8 8.0 - 1
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 3261 None 19 Human Functional pEC50 = 8 8.0 -10 7
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 3261 None 19 Human Functional pEC50 = 8 8.0 -10 7
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 3261 None 19 Human Functional pEC50 = 8 8.0 -10 7
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 185718 None 0 Human Functional pEC50 = 8 8.0 - 1
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 185718 None 0 Human Functional pEC50 = 8 8.0 - 1
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 721 None 58 Human Functional pEC50 = 8 8.0 363 2
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
11978813.0 721 None 58 Human Functional pEC50 = 8 8.0 363 2
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 721 None 58 Human Functional pEC50 = 8 8.0 363 2
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 721 None 58 Human Functional pEC50 = 8 8.0 363 2
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 721 None 58 Human Functional pEC50 = 8 8.0 363 2
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 721 None 58 Human Functional pEC50 = 8 8.0 363 2
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
171492372 197072 None 0 Human Functional pEC50 = 8 8.0 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5438081 197072 None 0 Human Functional pEC50 = 8 8.0 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
146025775 170056 None 0 Human Functional pEC50 = 8 8.0 - 1
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 170056 None 0 Human Functional pEC50 = 8 8.0 - 1
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 6216 None 0 Human Functional pEC50 = 8 8.0 - 1
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 6216 None 0 Human Functional pEC50 = 8 8.0 - 1
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 6243 None 0 Human Functional pEC50 = 8 8.0 - 1
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 6243 None 0 Human Functional pEC50 = 8 8.0 - 1
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 6760 None 0 Human Functional pEC50 = 8 8.0 - 1
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 6760 None 0 Human Functional pEC50 = 8 8.0 - 1
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 721 None 58 Human Functional pEC50 = 8.0 8.0 363 2
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
11978813.0 721 None 58 Human Functional pEC50 = 8.0 8.0 363 2
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 721 None 58 Human Functional pEC50 = 8.0 8.0 363 2
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 721 None 58 Human Functional pEC50 = 8.0 8.0 363 2
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 721 None 58 Human Functional pEC50 = 8.0 8.0 363 2
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 721 None 58 Human Functional pEC50 = 8.0 8.0 363 2
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 None 8 Human Functional pEC50 = 8.0 8.0 -50 3
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 None 8 Human Functional pEC50 = 8.0 8.0 -50 3
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 None 8 Human Functional pEC50 = 8.0 8.0 -50 3
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 159652 None 0 Human Functional pEC50 = 8.0 8.0 1 2
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 159652 None 0 Human Functional pEC50 = 8.0 8.0 1 2
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 115835 None 0 Human Functional pEC50 = 8.0 8.0 6 2
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 115835 None 0 Human Functional pEC50 = 8.0 8.0 6 2
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 185418 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 185418 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 170793 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 170793 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 3706 None 25 Rat Functional pEC50 = 8.0 8.0 4 3
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 3706 None 25 Rat Functional pEC50 = 8.0 8.0 4 3
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 3706 None 25 Rat Functional pEC50 = 8.0 8.0 4 3
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 3706 None 25 Rat Functional pEC50 = 8.0 8.0 4 3
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
171492372 197072 None 0 Human Functional pEC50 = 8.0 8.0 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5438081 197072 None 0 Human Functional pEC50 = 8.0 8.0 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
2 3261 None 19 Human Functional pEC50 = 8.0 8.0 -10 7
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 3261 None 19 Human Functional pEC50 = 8.0 8.0 -10 7
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 3261 None 19 Human Functional pEC50 = 8.0 8.0 -10 7
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 186270 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 186270 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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
172469879 197088 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 413 8 2 4 4.7 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N4CCCC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5438433 197088 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 413 8 2 4 4.7 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N4CCCC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
163728602 186270 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 186270 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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
171492372 197072 None 0 Human Functional pEC50 = 8.0 8.0 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5438081 197072 None 0 Human Functional pEC50 = 8.0 8.0 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 0 4 4.2 COCCC(=O)N1CCC(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
172444647 195417 None 0 Human Functional pEC50 = 8.0 8.0 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5403268 195417 None 0 Human Functional pEC50 = 8.0 8.0 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
172469879 197088 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 413 8 2 4 4.7 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N4CCCC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5438433 197088 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 413 8 2 4 4.7 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N4CCCC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
119570 3159 None 58 Human Functional pEC50 = 7 7.0 -28 11
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
119570.0 3159 None 58 Human Functional pEC50 = 7 7.0 -28 11
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 3159 None 58 Human Functional pEC50 = 7 7.0 -28 11
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 3159 None 58 Human Functional pEC50 = 7 7.0 -28 11
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 3159 None 58 Human Functional pEC50 = 7 7.0 -28 11
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 3159 None 58 Human Functional pEC50 = 7 7.0 -28 11
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 3942 None 7 Human Functional pEC50 = 7 7.0 - 1
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 3942 None 7 Human Functional pEC50 = 7 7.0 - 1
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 3942 None 7 Human Functional pEC50 = 7 7.0 - 1
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 82011 None 0 Human Functional pEC50 = 7 7.0 - 1
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 82011 None 0 Human Functional pEC50 = 7 7.0 - 1
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
172461590 196841 None 0 Human Functional pEC50 = 7 7.0 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 406 6 1 5 4.2 COc1cccc2c3c(oc12)CN(CCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5433201 196841 None 0 Human Functional pEC50 = 7 7.0 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 406 6 1 5 4.2 COc1cccc2c3c(oc12)CN(CCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
137651073 157560 None 0 Human Functional pEC50 = 6 6.0 -36 2
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 157560 None 0 Human Functional pEC50 = 6 6.0 -36 2
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 82006 None 0 Human Functional pEC50 = 6 6.0 - 1
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 82006 None 0 Human Functional pEC50 = 6 6.0 - 1
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 159000 None 0 Human Functional pEC50 = 6 6.0 - 1
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 159000 None 0 Human Functional pEC50 = 6 6.0 - 1
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 205 None 17 Rat Functional pEC50 = 5.0 5.0 -3235 4
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 205 None 17 Rat Functional pEC50 = 5.0 5.0 -3235 4
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 205 None 17 Rat Functional pEC50 = 5.0 5.0 -3235 4
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 205 None 17 Rat Functional pEC50 = 5.0 5.0 -3235 4
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 205 None 17 Rat Functional pEC50 = 5.0 5.0 -3235 4
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 205 None 17 Rat Functional pEC50 = 5.0 5.0 -3235 4
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 92012 None 2 Human Functional pEC50 = 5.0 5.0 - 1
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 92012 None 2 Human Functional pEC50 = 5.0 5.0 - 1
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 92012 None 2 Human Functional pEC50 = 5.0 5.0 - 1
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 92012 None 2 Human Functional pEC50 = 5.0 5.0 - 1
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 185483 None 0 Human Functional pEC50 = 6.0 6.0 -66 11
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 185483 None 0 Human Functional pEC50 = 6.0 6.0 -66 11
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
56852956 112106 None 1 Human Functional pEC50 = 6.0 6.0 -154 3
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL3289656 112106 None 1 Human Functional pEC50 = 6.0 6.0 -154 3
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
56599143 82015 None 10 Human Functional pEC50 = 7.0 7.0 - 1
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 82015 None 10 Human Functional pEC50 = 7.0 7.0 - 1
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 159849 None 0 Human Functional pEC50 = 6.0 6.0 -11 2
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 159849 None 0 Human Functional pEC50 = 6.0 6.0 -11 2
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 184542 None 0 Human Functional pEC50 = 6.0 6.0 -10 3
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 184542 None 0 Human Functional pEC50 = 6.0 6.0 -10 3
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 16976 None 0 Human Functional pEC50 = 7.0 7.0 -104 2
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 16976 None 0 Human Functional pEC50 = 7.0 7.0 -104 2
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 79697 None 0 Rat Functional pEC50 = 5.0 5.0 -75 2
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 79697 None 0 Rat Functional pEC50 = 5.0 5.0 -75 2
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 111852 None 0 Human Functional pEC50 = 7.0 7.0 -9 2
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 111852 None 0 Human Functional pEC50 = 7.0 7.0 -9 2
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 123314 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 123314 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 185009 None 0 Human Functional pEC50 = 6.0 6.0 -12 3
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 185009 None 0 Human Functional pEC50 = 6.0 6.0 -12 3
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 185418 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 185418 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 170793 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 170793 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 148498 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 148498 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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
172444647 195417 None 0 Human Functional pEC50 = 8.0 8.0 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5403268 195417 None 0 Human Functional pEC50 = 8.0 8.0 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 9 1 5 3.1 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(OC)c3F)CC2)CC1 10.1021/acs.jmedchem.2c01624
164617831 184836 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 184836 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 184836 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 184836 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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
172465074 196712 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 432 8 1 5 4.9 CCOc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5430494 196712 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 432 8 1 5 4.9 CCOc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
172465074 196712 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 432 8 1 5 4.9 CCOc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5430494 196712 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 432 8 1 5 4.9 CCOc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
172439032 195309 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5400528 195309 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
172439032 195309 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5400528 195309 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
127046952 140188 None 0 Human Functional pEC50 = 7.0 7.0 87 2
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 140188 None 0 Human Functional pEC50 = 7.0 7.0 87 2
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 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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
11154555.0 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 111852 None 0 Human Functional pEC50 = 7.0 7.0 -9 2
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 111852 None 0 Human Functional pEC50 = 7.0 7.0 -9 2
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 61194 None 0 Human Functional pEC50 = 7.0 7.0 -489 2
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 61194 None 0 Human Functional pEC50 = 7.0 7.0 -489 2
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 121273 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 121273 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 159849 None 0 Human Functional pEC50 = 6.0 6.0 -11 2
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 159849 None 0 Human Functional pEC50 = 6.0 6.0 -11 2
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
164937988 195320 None 4 Human Functional pEC50 = 6.0 6.0 -154 5
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL5400876 195320 None 4 Human Functional pEC50 = 6.0 6.0 -154 5
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
11154555 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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
11154555.0 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 800 None 50 Human Functional pEC50 = 7.0 7.0 1 10
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 117266 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 117266 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 123315 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 123315 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 192914 None 0 Human Functional pEC50 = 6.0 6.0 -16 3
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 192914 None 0 Human Functional pEC50 = 6.0 6.0 -16 3
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 192914 None 0 Human Functional pEC50 = 6.0 6.0 -16 3
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 184696 None 0 Human Functional pEC50 = 6.0 6.0 -27 3
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 184696 None 0 Human Functional pEC50 = 6.0 6.0 -27 3
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 80891 None 0 Human Functional pEC50 = 6.9 6.9 -446 2
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 80891 None 0 Human Functional pEC50 = 6.9 6.9 -446 2
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 92157 None 0 Human Functional pEC50 = 6.9 6.9 -38 2
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 92157 None 0 Human Functional pEC50 = 6.9 6.9 -38 2
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 117266 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 117266 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 80890 None 0 Human Functional pEC50 = 6.9 6.9 -446 2
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 80890 None 0 Human Functional pEC50 = 6.9 6.9 -446 2
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 79669 None 1 Rat Functional pEC50 = 6.9 6.9 - 1
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 79669 None 1 Rat Functional pEC50 = 6.9 6.9 - 1
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 200248 None 0 Human Functional pEC50 = 6.9 6.9 -173 2
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 200248 None 0 Human Functional pEC50 = 6.9 6.9 -173 2
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 200248 None 0 Human Functional pEC50 = 6.9 6.9 -173 2
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 200248 None 0 Human Functional pEC50 = 6.9 6.9 -173 2
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 200248 None 0 Human Functional pEC50 = 6.9 6.9 -173 2
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 200248 None 0 Human Functional pEC50 = 6.9 6.9 -173 2
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 155970 None 0 Human Functional pEC50 = 6.9 6.9 2 2
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 155970 None 0 Human Functional pEC50 = 6.9 6.9 2 2
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
172439985 195264 None 0 Human Functional pEC50 = 5.9 5.9 -14 3
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 367 6 0 5 4.5 COc1ccc2nc(CCCN3CCC(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
CHEMBL5399720 195264 None 0 Human Functional pEC50 = 5.9 5.9 -14 3
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 367 6 0 5 4.5 COc1ccc2nc(CCCN3CCC(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
44241577 14019 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
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 14019 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
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 14019 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
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 3159 None 58 Rat Functional pEC50 = 7.9 7.9 -34 11
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
119570.0 3159 None 58 Rat Functional pEC50 = 7.9 7.9 -34 11
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 3159 None 58 Rat Functional pEC50 = 7.9 7.9 -34 11
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 3159 None 58 Rat Functional pEC50 = 7.9 7.9 -34 11
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 3159 None 58 Rat Functional pEC50 = 7.9 7.9 -34 11
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 3159 None 58 Rat Functional pEC50 = 7.9 7.9 -34 11
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 103612 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 103612 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 9502 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 9502 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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
CHEMBL129483 9502 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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
72736203 103612 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 103612 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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
10178704 49673 None 0 Human Functional pEC50 = 7.9 7.9 -17 2
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 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm070860r
CHEMBL156639 49673 None 0 Human Functional pEC50 = 7.9 7.9 -17 2
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 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm070860r
172440653 195350 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 9 2 5 4.3 CCOc1cccc2cc(CNCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5401818 195350 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 9 2 5 4.3 CCOc1cccc2cc(CNCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
242 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795.0 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
172440653 195350 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 9 2 5 4.3 CCOc1cccc2cc(CNCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5401818 195350 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 9 2 5 4.3 CCOc1cccc2cc(CNCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
242 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795.0 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
242 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
34 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
60795 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
60795.0 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
DB01238 470 None 70 Human Functional pEC50 = 7.9 7.9 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
201536 111531 None 2 Human Functional pEC50 = 7.9 7.9 -1 2
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 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL3276140 111531 None 2 Human Functional pEC50 = 7.9 7.9 -1 2
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 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
228 445 None 20 Human Functional pEC50 = 7.9 7.9 -3 20
Agonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2018.04.059
33 445 None 20 Human Functional pEC50 = 7.9 7.9 -3 20
Agonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2018.04.059
6005 445 None 20 Human Functional pEC50 = 7.9 7.9 -3 20
Agonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2018.04.059
6005.0 445 None 20 Human Functional pEC50 = 7.9 7.9 -3 20
Agonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2018.04.059
CHEMBL53 445 None 20 Human Functional pEC50 = 7.9 7.9 -3 20
Agonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2018.04.059
DB00714 445 None 20 Human Functional pEC50 = 7.9 7.9 -3 20
Agonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2018.04.059
201536 111531 None 2 Human Functional pEC50 = 7.9 7.9 -1 2
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 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL3276140 111531 None 2 Human Functional pEC50 = 7.9 7.9 -1 2
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 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
25072002 156205 None 0 Human Functional pEC50 = 7.9 7.9 -3 2
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 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 156205 None 0 Human Functional pEC50 = 7.9 7.9 -3 2
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 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
156785342 184969 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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)cc1[C@@H]1C[C@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4852524 184969 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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)cc1[C@@H]1C[C@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
156785342 184969 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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)cc1[C@@H]1C[C@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4852524 184969 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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)cc1[C@@H]1C[C@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
121418441 174436 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 331 6 0 3 4.3 CC1(Oc2ccc(Cl)cc2)CCN(CCOc2ccccc2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL4550815 174436 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 331 6 0 3 4.3 CC1(Oc2ccc(Cl)cc2)CCN(CCOc2ccccc2)C1 10.1021/acs.jmedchem.8b00435
25093832 155970 None 0 Human Functional pEC50 = 6.9 6.9 2 2
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 155970 None 0 Human Functional pEC50 = 6.9 6.9 2 2
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
164616642 184672 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 412 9 2 3 5.2 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2[nH]1 10.1021/acs.jmedchem.1c01327
CHEMBL4848451 184672 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 412 9 2 3 5.2 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2[nH]1 10.1021/acs.jmedchem.1c01327
164616642 184672 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 412 9 2 3 5.2 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2[nH]1 10.1021/acs.jmedchem.1c01327
CHEMBL4848451 184672 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 412 9 2 3 5.2 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2[nH]1 10.1021/acs.jmedchem.1c01327
10515841 210724 None 0 Rat Functional pEC50 = 6.9 6.9 -3 2
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
CHEMBL98836 210724 None 0 Rat Functional pEC50 = 6.9 6.9 -3 2
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
132435 130777 None 2 Human Functional pEC50 = 6.9 6.9 -8 2
Dopamine receptor D2 agonist activity was determined for inhibition of release of NE in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of release of NE in an isolated perfused rabbit ear artery preparation
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL130795 130777 None 2 Human Functional pEC50 = 6.9 6.9 -8 2
Dopamine receptor D2 agonist activity was determined for inhibition of release of NE in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of release of NE in an isolated perfused rabbit ear artery preparation
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL368456 130777 None 2 Human Functional pEC50 = 6.9 6.9 -8 2
Dopamine receptor D2 agonist activity was determined for inhibition of release of NE in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of release of NE in an isolated perfused rabbit ear artery preparation
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
137662136 159450 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 423 12 1 6 3.0 CN[C@@H]1Cc2cccc3c2n(c(=O)n3CCOCCOCCCCc2ccccc2)C1 10.1021/acs.jmedchem.6b01875
CHEMBL4100322 159450 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 423 12 1 6 3.0 CN[C@@H]1Cc2cccc3c2n(c(=O)n3CCOCCOCCCCc2ccccc2)C1 10.1021/acs.jmedchem.6b01875
172449047 195971 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4oc(C)nc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5414422 195971 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4oc(C)nc4c3)oc12 10.1021/acs.jmedchem.3c00098
46881411 6763 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 319 4 0 4 3.2 O=c1n(CCN2CCCCCC2)ccn1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1083816 6763 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 319 4 0 4 3.2 O=c1n(CCN2CCCCCC2)ccn1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
46881412 6859 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 357 4 0 3 2.6 O=S1(=O)N(CCN2CCCCCC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1084121 6859 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 357 4 0 3 2.6 O=S1(=O)N(CCN2CCCCCC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
56599143 82015 None 10 Human Functional pEC50 = 6.9 6.9 - 1
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 421 6 0 5 5.2 Clc1cccc(N2CCN(CCCOc3ccc4scnc4c3)CC2)c1Cl 10.1021/jm300603y
CHEMBL2165139 82015 None 10 Human Functional pEC50 = 6.9 6.9 - 1
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 421 6 0 5 5.2 Clc1cccc(N2CCN(CCCOc3ccc4scnc4c3)CC2)c1Cl 10.1021/jm300603y
56597938 3940 None 4 Human Functional pEC50 = 6.9 6.9 204 2
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 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7651 3940 None 4 Human Functional pEC50 = 6.9 6.9 204 2
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 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165126 3940 None 4 Human Functional pEC50 = 6.9 6.9 204 2
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 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
71456928 82007 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 459 6 1 4 4.6 O=C1CCc2ccc(CO[C@@H]3C[C@H]3CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 10.1021/jm300603y
CHEMBL2165130 82007 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 459 6 1 4 4.6 O=C1CCc2ccc(CO[C@@H]3C[C@H]3CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 10.1021/jm300603y
164624917 185712 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 393 7 2 2 4.8 CN(C)C(=O)N[C@H]1CC[C@H](CCNCC2CC2c2cccc3ccccc23)CC1 10.1021/acs.jmedchem.1c01327
CHEMBL4863920 185712 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 393 7 2 2 4.8 CN(C)C(=O)N[C@H]1CC[C@H](CCNCC2CC2c2cccc3ccccc23)CC1 10.1021/acs.jmedchem.1c01327
146025781 172251 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 407 4 1 2 4.0 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(Br)c3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4473178 172251 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 407 4 1 2 4.0 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(Br)c3C2)CC1 10.1021/acs.jmedchem.9b00508
25072632 111839 None 0 Human Functional pEC50 = 5.9 5.9 -30 2
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 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287392 111839 None 0 Human Functional pEC50 = 5.9 5.9 -30 2
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 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
146025781 172251 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 407 4 1 2 4.0 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(Br)c3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4473178 172251 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 407 4 1 2 4.0 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(Br)c3C2)CC1 10.1021/acs.jmedchem.9b00508
46917563 68357 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayAgonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1916551 68357 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayAgonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
137636351 155963 None 0 Human Functional pEC50 = 7.9 7.9 2 2
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 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4060403 155963 None 0 Human Functional pEC50 = 7.9 7.9 2 2
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 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
25072002 156205 None 0 Human Functional pEC50 = 7.9 7.9 -3 2
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 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 156205 None 0 Human Functional pEC50 = 7.9 7.9 -3 2
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 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
44555137 104319 None 0 Human Functional pEC50 = 7.9 7.9 28 2
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 403 5 1 5 3.9 CCCN1C[C@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099232 104319 None 0 Human Functional pEC50 = 7.9 7.9 28 2
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 403 5 1 5 3.9 CCCN1C[C@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
85469680 156807 None 0 Human Functional pEC50 = 7.9 7.9 -5 2
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 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4070196 156807 None 0 Human Functional pEC50 = 7.9 7.9 -5 2
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 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
90466574 158686 None 0 Human Functional pEC50 = 7.9 7.9 -3 2
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 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4092052 158686 None 0 Human Functional pEC50 = 7.9 7.9 -3 2
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 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
56593482 3941 None 6 Human Functional pEC50 = 7.9 7.9 602 2
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 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7650 3941 None 6 Human Functional pEC50 = 7.9 7.9 602 2
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 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165119 3941 None 6 Human Functional pEC50 = 7.9 7.9 602 2
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 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
56598074 145764 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 445 6 1 4 4.8 O=c1ccc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
CHEMBL3916047 145764 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 445 6 1 4 4.8 O=c1ccc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
164610211 185173 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 442 10 1 4 5.1 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4855583 185173 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 442 10 1 4 5.1 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
172450959 195711 None 0 Human Functional pEC50 = 7.9 7.9 22 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 195711 None 0 Human Functional pEC50 = 7.9 7.9 22 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
164610211 185173 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 442 10 1 4 5.1 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4855583 185173 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 442 10 1 4 5.1 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
172450959 195711 None 0 Human Functional pEC50 = 7.9 7.9 22 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 195711 None 0 Human Functional pEC50 = 7.9 7.9 22 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
24866114 178793 None 0 Human Functional pEC50 = 7.9 7.9 -223 2
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 7 1 6 4.4 CCCN(CCN1CCN(c2cccc(Cl)c2Cl)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
CHEMBL468017 178793 None 0 Human Functional pEC50 = 7.9 7.9 -223 2
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 7 1 6 4.4 CCCN(CCN1CCN(c2cccc(Cl)c2Cl)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
45486328 199818 None 0 Human Functional pEC50 = 7.9 7.9 -25 2
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(c2cccc3ncccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
CHEMBL569107 199818 None 0 Human Functional pEC50 = 7.9 7.9 -25 2
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(c2cccc3ncccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
90467021 156762 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4069565 156762 None 0 Human Functional pEC50 = 7.9 7.9 1 2
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 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
11316847 70371 None 0 Human Functional pEC50 = 7.9 7.9 -6 2
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cells
ChEMBL 448 7 1 5 4.0 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc([N+](=O)[O-])cc1 10.1021/jm049465g
CHEMBL194493 70371 None 0 Human Functional pEC50 = 7.9 7.9 -6 2
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cells
ChEMBL 448 7 1 5 4.0 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc([N+](=O)[O-])cc1 10.1021/jm049465g
242 470 None 70 Human Functional pEC50 = 6.9 6.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
34 470 None 70 Human Functional pEC50 = 6.9 6.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
60795 470 None 70 Human Functional pEC50 = 6.9 6.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
60795.0 470 None 70 Human Functional pEC50 = 6.9 6.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL1112 470 None 70 Human Functional pEC50 = 6.9 6.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
DB01238 470 None 70 Human Functional pEC50 = 6.9 6.9 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
71733935 91017 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2396663 91017 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL5078893 217080 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human D2 receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation by measuring dopamine EC50 at 0.01 nM pretreated for 10 mins followed by forskolin stimulation for 5 mins and measured after 1 hr by HTRF assayPositive allosteric modulation of human D2 receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation by measuring dopamine EC50 at 0.01 nM pretreated for 10 mins followed by forskolin stimulation for 5 mins and measured after 1 hr by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)c1ccoc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c00252
25072632 111839 None 0 Human Functional pEC50 = 5.9 5.9 -30 2
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 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287392 111839 None 0 Human Functional pEC50 = 5.9 5.9 -30 2
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 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
71733935 91017 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2396663 91017 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
146025770 171419 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 314 5 1 2 3.5 CCC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4461089 171419 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 314 5 1 2 3.5 CCC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
146025770 171419 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 314 5 1 2 3.5 CCC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4461089 171419 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 314 5 1 2 3.5 CCC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
172449047 195971 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4oc(C)nc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5414422 195971 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4oc(C)nc4c3)oc12 10.1021/acs.jmedchem.3c00098
172454723 196020 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 406 7 1 5 4.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)C2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5415178 196020 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 406 7 1 5 4.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)C2)CC3 10.1021/acs.jmedchem.3c00098
90467171 161242 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4079093 161242 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4117318 161242 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
13720688 11558 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Dopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparation
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1180542 11558 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Dopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparation
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL129634 11558 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Dopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparation
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
164624917 185712 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 393 7 2 2 4.8 CN(C)C(=O)N[C@H]1CC[C@H](CCNCC2CC2c2cccc3ccccc23)CC1 10.1021/acs.jmedchem.1c01327
CHEMBL4863920 185712 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 393 7 2 2 4.8 CN(C)C(=O)N[C@H]1CC[C@H](CCNCC2CC2c2cccc3ccccc23)CC1 10.1021/acs.jmedchem.1c01327
118726003 120948 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
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 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394259 120948 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
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 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3559207 120948 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
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 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
118726003 120948 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
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 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394259 120948 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
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 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3559207 120948 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
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 878 31 5 13 7.1 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
101885476 121603 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 857 37 4 6 9.9 CCCN(CCCNC(=O)CCCCCCCCCCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585372 121603 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 857 37 4 6 9.9 CCCN(CCCNC(=O)CCCCCCCCCCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
46929184 103622 None 22 Human Functional pEC50 = 7.9 7.9 - 1
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 455 5 1 4 5.6 CC(C)(C)OC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL3085821 103622 None 22 Human Functional pEC50 = 7.9 7.9 - 1
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 455 5 1 4 5.6 CC(C)(C)OC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.9b00508
146025768 170433 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 2 3.8 O=C(N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1)N1CCCC1 10.1021/acs.jmedchem.9b00508
CHEMBL4447058 170433 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 2 3.8 O=C(N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1)N1CCCC1 10.1021/acs.jmedchem.9b00508
164621372 185800 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 440 11 1 4 5.0 CCN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4865389 185800 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 440 11 1 4 5.0 CCN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
101885476 121603 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 857 37 4 6 9.9 CCCN(CCCNC(=O)CCCCCCCCCCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585372 121603 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 857 37 4 6 9.9 CCCN(CCCNC(=O)CCCCCCCCCCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
164621372 185800 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 440 11 1 4 5.0 CCN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4865389 185800 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 440 11 1 4 5.0 CCN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
46929184 103622 None 22 Human Functional pEC50 = 7.8 7.8 - 1
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 455 5 1 4 5.6 CC(C)(C)OC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL3085821 103622 None 22 Human Functional pEC50 = 7.8 7.8 - 1
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 455 5 1 4 5.6 CC(C)(C)OC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.9b00508
146025768 170433 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 2 3.8 O=C(N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1)N1CCCC1 10.1021/acs.jmedchem.9b00508
CHEMBL4447058 170433 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 2 3.8 O=C(N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1)N1CCCC1 10.1021/acs.jmedchem.9b00508
137658100 159710 None 0 Human Functional pEC50 = 7.8 7.8 2 2
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 483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4103339 159710 None 0 Human Functional pEC50 = 7.8 7.8 2 2
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 483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
156785362 184992 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4852835 184992 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
172465305 196931 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 387 8 2 4 4.1 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5435054 196931 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 387 8 2 4 4.1 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)oc12 10.1021/acs.jmedchem.3c00098
164615405 185392 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 430 9 2 3 5.4 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2[nH]1 10.1021/acs.jmedchem.1c01327
CHEMBL4859080 185392 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 430 9 2 3 5.4 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2[nH]1 10.1021/acs.jmedchem.1c01327
156785362 184992 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4852835 184992 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164620035 185746 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 398 9 2 4 3.9 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4864436 185746 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 398 9 2 4 3.9 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
164615405 185392 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 430 9 2 3 5.4 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2[nH]1 10.1021/acs.jmedchem.1c01327
CHEMBL4859080 185392 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 430 9 2 3 5.4 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2[nH]1 10.1021/acs.jmedchem.1c01327
172465305 196931 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 387 8 2 4 4.1 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5435054 196931 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 387 8 2 4 4.1 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)oc12 10.1021/acs.jmedchem.3c00098
164620035 185746 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 398 9 2 4 3.9 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4864436 185746 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 398 9 2 4 3.9 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
2 3261 None 19 Human Functional pEC50 = 6.9 6.9 -10 7
Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayAgonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm2009919
54562 3261 None 19 Human Functional pEC50 = 6.9 6.9 -10 7
Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayAgonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm2009919
CHEMBL240773 3261 None 19 Human Functional pEC50 = 6.9 6.9 -10 7
Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayAgonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm2009919
137651073 157560 None 0 Human Functional pEC50 = 5.9 5.9 -36 2
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 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4079301 157560 None 0 Human Functional pEC50 = 5.9 5.9 -36 2
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 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
44554644 106338 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 259 2 1 3 2.0 Oc1cccc2c1C[C@@H]1OCCN(CC3CC3)[C@H]1C2 10.1016/j.bmc.2013.11.012
CHEMBL3099229 106338 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 259 2 1 3 2.0 Oc1cccc2c1C[C@@H]1OCCN(CC3CC3)[C@H]1C2 10.1016/j.bmc.2013.11.012
CHEMBL3139036 106338 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 259 2 1 3 2.0 Oc1cccc2c1C[C@@H]1OCCN(CC3CC3)[C@H]1C2 10.1016/j.bmc.2013.11.012
57335757 71572 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Antagonist activity at dopamine D2 receptorAntagonist activity at dopamine D2 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@H]1C2 10.1016/j.bmcl.2012.01.005
CHEMBL1950492 71572 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Antagonist activity at dopamine D2 receptorAntagonist activity at dopamine D2 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@H]1C2 10.1016/j.bmcl.2012.01.005
CHEMBL1963011 71572 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Antagonist activity at dopamine D2 receptorAntagonist activity at dopamine D2 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@H]1C2 10.1016/j.bmcl.2012.01.005
168278471 192957 None 0 Human Functional pEC50 = 5.9 5.9 -77 3
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 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5183205 192957 None 0 Human Functional pEC50 = 5.9 5.9 -77 3
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 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221757 192957 None 0 Human Functional pEC50 = 5.9 5.9 -77 3
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 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
137651073 157560 None 0 Human Functional pEC50 = 5.9 5.9 -36 2
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 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4079301 157560 None 0 Human Functional pEC50 = 5.9 5.9 -36 2
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 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
172454723 196020 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 406 7 1 5 4.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)C2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5415178 196020 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 406 7 1 5 4.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)C2)CC3 10.1021/acs.jmedchem.3c00098
122179562 121597 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 532 13 2 6 4.7 CCCN(CCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2CCCNC(=O)OC(C)(C)C 10.1039/C4MD00066H
CHEMBL3585366 121597 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 532 13 2 6 4.7 CCCN(CCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2CCCNC(=O)OC(C)(C)C 10.1039/C4MD00066H
681 1465 None 47 Rat Functional pEC50 = 5.9 5.9 -288 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
681.0 1465 None 47 Rat Functional pEC50 = 5.9 5.9 -288 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
940 1465 None 47 Rat Functional pEC50 = 5.9 5.9 -288 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
947 1465 None 47 Rat Functional pEC50 = 5.9 5.9 -288 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
CHEMBL59 1465 None 47 Rat Functional pEC50 = 5.9 5.9 -288 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
DB00988 1465 None 47 Rat Functional pEC50 = 5.9 5.9 -288 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
72736199 103805 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 330 5 1 3 3.7 CCOC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL3088211 103805 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 330 5 1 3 3.7 CCOC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
72736199 103805 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 330 5 1 3 3.7 CCOC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL3088211 103805 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 330 5 1 3 3.7 CCOC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
122179562 121597 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 532 13 2 6 4.7 CCCN(CCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2CCCNC(=O)OC(C)(C)C 10.1039/C4MD00066H
CHEMBL3585366 121597 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 532 13 2 6 4.7 CCCN(CCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2CCCNC(=O)OC(C)(C)C 10.1039/C4MD00066H
137660751 159490 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 532 15 2 6 5.8 CN[C@@H]1Cc2cccc3c2n(c(=O)n3CCCCCCCCCCCCOc2ccc3c(c2)NC(=O)CC3)C1 10.1021/acs.jmedchem.6b01875
CHEMBL4100734 159490 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 532 15 2 6 5.8 CN[C@@H]1Cc2cccc3c2n(c(=O)n3CCCCCCCCCCCCOc2ccc3c(c2)NC(=O)CC3)C1 10.1021/acs.jmedchem.6b01875
90466867 156402 None 0 Human Functional pEC50 = 6.8 6.8 -5 2
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 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4065510 156402 None 0 Human Functional pEC50 = 6.8 6.8 -5 2
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 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
118725997 117267 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 652 17 4 12 3.4 CCCN(CCCNC(=O)COc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394255 117267 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 652 17 4 12 3.4 CCCN(CCCNC(=O)COc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
118725997 117267 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 652 17 4 12 3.4 CCCN(CCCNC(=O)COc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394255 117267 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 652 17 4 12 3.4 CCCN(CCCNC(=O)COc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
53328901 66502 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 371 4 3 5 3.4 CN1CCc2cc(SCCC(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1802236 66502 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 371 4 3 5 3.4 CN1CCc2cc(SCCC(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1852245 66502 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 371 4 3 5 3.4 CN1CCc2cc(SCCC(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
10780928 10437 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
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 305 5 1 5 3.3 CCCN(CCC)C1COc2ccc3nc(N)sc3c2C1 10.1021/jm000087z
CHEMBL116372 10437 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
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 305 5 1 5 3.3 CCCN(CCC)C1COc2ccc3nc(N)sc3c2C1 10.1021/jm000087z
29945476 174402 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 0 3 3.5 COc1ccc2c(c1OC)-c1cccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4550010 174402 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 0 3 3.5 COc1ccc2c(c1OC)-c1cccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
164609095 184548 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 412 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4846472 184548 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 412 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164609095 184548 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 412 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4846472 184548 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 412 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
44438201 93660 None 1 Human Functional pEC50 = 7.8 7.8 2 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 374 3 2 2 5.0 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246637 93660 None 1 Human Functional pEC50 = 7.8 7.8 2 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 374 3 2 2 5.0 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
2 3261 None 19 Human Functional pEC50 = 7.8 7.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3261 None 19 Human Functional pEC50 = 7.8 7.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3261 None 19 Human Functional pEC50 = 7.8 7.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
44427827 93328 None 0 Human Functional pEC50 = 7.8 7.8 -15 2
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 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL244990 93328 None 0 Human Functional pEC50 = 7.8 7.8 -15 2
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 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
25071385 159250 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098236 159250 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
2 3261 None 19 Human Functional pEC50 = 7.8 7.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3261 None 19 Human Functional pEC50 = 7.8 7.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3261 None 19 Human Functional pEC50 = 7.8 7.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
56941366 105755 None 0 Human Functional pEC50 = 7.8 7.8 -158 2
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 491 8 2 7 4.5 CCCN(CCN1CCN(c2ccc(-c3cccc(O)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm401883v
CHEMBL3125990 105755 None 0 Human Functional pEC50 = 7.8 7.8 -158 2
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 491 8 2 7 4.5 CCCN(CCN1CCN(c2ccc(-c3cccc(O)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm401883v
2 3261 None 19 Human Functional pEC50 = 6.8 6.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jnatprod.9b00921
54562 3261 None 19 Human Functional pEC50 = 6.8 6.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jnatprod.9b00921
CHEMBL240773 3261 None 19 Human Functional pEC50 = 6.8 6.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jnatprod.9b00921
25072941 156565 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 156565 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
137643951 158351 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4088639 158351 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
44427841 86173 None 0 Human Functional pEC50 = 6.8 6.8 -21 2
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 494 7 1 4 5.2 O=C(NC[C@H]1C[C@@H]1CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL231156 86173 None 0 Human Functional pEC50 = 6.8 6.8 -21 2
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 494 7 1 4 5.2 O=C(NC[C@H]1C[C@@H]1CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
71733935 91017 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2396663 91017 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
2 3261 None 19 Human Functional pEC50 = 6.8 6.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jnatprod.9b00921
54562 3261 None 19 Human Functional pEC50 = 6.8 6.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jnatprod.9b00921
CHEMBL240773 3261 None 19 Human Functional pEC50 = 6.8 6.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jnatprod.9b00921
164616851 185056 None 0 Human Functional pEC50 = 5.8 5.8 -9 3
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 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4853772 185056 None 0 Human Functional pEC50 = 5.8 5.8 -9 3
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 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
25072941 156565 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 156565 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
70684207 76097 None 0 Human Functional pEC50 = 4.8 4.8 -5 2
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 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057452 76097 None 0 Human Functional pEC50 = 4.8 4.8 -5 2
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 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 nan
10114519 55258 None 46 Human Functional pEC50 = 6.8 6.8 - 1
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 445 7 1 5 5.2 Oc1ccc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2n1 10.1021/jm300603y
CHEMBL161792 55258 None 46 Human Functional pEC50 = 6.8 6.8 - 1
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 445 7 1 5 5.2 Oc1ccc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2n1 10.1021/jm300603y
66559778 82001 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 423 9 1 5 4.0 CCOc1cccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c1 10.1021/jm300603y
CHEMBL2165123 82001 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 423 9 1 5 4.0 CCOc1cccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c1 10.1021/jm300603y
242 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
34 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
60795 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
60795.0 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
CHEMBL1112 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
DB01238 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
242 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795.0 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
242 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
34 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795.0 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL1112 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB01238 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
56599146 82005 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 501 6 1 4 5.9 O=C1CCc2ccc(OC[C@H]3CC[C@H](CN4CCN(c5cccc(Cl)c5Cl)CC4)CC3)cc2N1 10.1021/jm300603y
CHEMBL2165128 82005 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 501 6 1 4 5.9 O=C1CCc2ccc(OC[C@H]3CC[C@H](CN4CCN(c5cccc(Cl)c5Cl)CC4)CC3)cc2N1 10.1021/jm300603y
29945476 174402 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 0 3 3.5 COc1ccc2c(c1OC)-c1cccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4550010 174402 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 0 3 3.5 COc1ccc2c(c1OC)-c1cccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
11794899 119635 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 393 7 1 4 3.9 Cc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL346129 119635 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 393 7 1 4 3.9 Cc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
25071385 159250 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098236 159250 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
53327663 66500 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 342 3 3 5 2.9 CN1CCc2cc(SCCN)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1852239 66500 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 342 3 3 5 2.9 CN1CCc2cc(SCCN)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL3215641 66500 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 342 3 3 5 2.9 CN1CCc2cc(SCCN)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
10084583 104834 None 3 Rat Functional pEC50 = 7.8 7.8 -9 3
Effective concentration required for agonistic activity against rat Dopamine receptor D2LEffective concentration required for agonistic activity against rat Dopamine receptor D2L
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 104834 None 3 Rat Functional pEC50 = 7.8 7.8 -9 3
Effective concentration required for agonistic activity against rat Dopamine receptor D2LEffective concentration required for agonistic activity against rat Dopamine receptor D2L
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
56597095 82012 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 434 7 2 4 4.1 O=c1[nH]c2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 10.1021/jm300603y
CHEMBL2165135 82012 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 434 7 2 4 4.1 O=c1[nH]c2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 10.1021/jm300603y
11978813 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
11978813.0 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
5014 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
7672 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
CHEMBL2105760 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
DB09128 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
11978813 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
11978813.0 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
5014 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
7672 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
CHEMBL2105760 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
DB09128 721 None 58 Human Functional pEC50 = 7.8 7.8 363 2
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 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1021/acs.jmedchem.1c01327
164621351 185786 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 10 1 4 4.6 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4865118 185786 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 10 1 4 4.6 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
172445349 195094 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 9 2 5 4.7 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
CHEMBL5396612 195094 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 9 2 5 4.7 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
164621351 185786 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 10 1 4 4.6 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4865118 185786 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 10 1 4 4.6 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
172445349 195094 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 9 2 5 4.7 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
CHEMBL5396612 195094 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 9 2 5 4.7 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
242 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795.0 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
242 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
34 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795.0 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL1112 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB01238 470 None 70 Human Functional pEC50 = 6.8 6.8 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
44417647 82192 None 0 Rat Functional pEC50 = 5.8 5.8 -75 3
Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL1203924 82192 None 0 Rat Functional pEC50 = 5.8 5.8 -75 3
Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL216945 82192 None 0 Rat Functional pEC50 = 5.8 5.8 -75 3
Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
2 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
54562 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
CHEMBL240773 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
2 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
54562 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
CHEMBL240773 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
172447622 195955 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 11 2 5 5.0 CCOc1cccc2cc(CNCCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5414152 195955 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 11 2 5 5.0 CCOc1cccc2cc(CNCCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
70682090 76096 None 0 Human Functional pEC50 = 4.8 4.8 -6 2
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 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057451 76096 None 0 Human Functional pEC50 = 4.8 4.8 -6 2
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 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
11307083 63576 None 0 Human Functional pEC50 = 6.8 6.8 -6 2
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cells
ChEMBL 529 6 1 3 4.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1021/jm049465g
CHEMBL180060 63576 None 0 Human Functional pEC50 = 6.8 6.8 -6 2
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cells
ChEMBL 529 6 1 3 4.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1021/jm049465g
2 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2015.07.050
54562 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2015.07.050
CHEMBL240773 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2015.07.050
2 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
54562 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
CHEMBL240773 3261 None 19 Human Functional pEC50 = 5.8 5.8 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
172447622 195955 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 11 2 5 5.0 CCOc1cccc2cc(CNCCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5414152 195955 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 11 2 5 5.0 CCOc1cccc2cc(CNCCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
5311189 207299 None 9 Human Functional pEC50 = 6.8 6.8 -16 4
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1021/acs.jmedchem.5b01031
CHEMBL7549 207299 None 9 Human Functional pEC50 = 6.8 6.8 -16 4
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1021/acs.jmedchem.5b01031
56598072 152844 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 423 8 1 5 4.0 COc1ccccc1N1CCCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
CHEMBL3973357 152844 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 423 8 1 5 4.0 COc1ccccc1N1CCCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
3949 3706 None 25 Human Functional pEC50 = 6.8 6.8 -4 3
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human 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 3706 None 25 Human Functional pEC50 = 6.8 6.8 -4 3
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human 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 3706 None 25 Human Functional pEC50 = 6.8 6.8 -4 3
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human 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 3706 None 25 Human Functional pEC50 = 6.8 6.8 -4 3
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human 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
164611342 185194 None 0 Human Functional pEC50 = 5.8 5.8 -48 3
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 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856005 185194 None 0 Human Functional pEC50 = 5.8 5.8 -48 3
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 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
44438237 93712 None 1 Human Functional pEC50 = 6.8 6.8 3 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 424 8 1 3 6.4 CCCCCCn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
CHEMBL246855 93712 None 1 Human Functional pEC50 = 6.8 6.8 3 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 424 8 1 3 6.4 CCCCCCn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
164616642 184672 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 412 9 2 3 5.2 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2[nH]1 10.1021/acs.jmedchem.1c01327
CHEMBL4848451 184672 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 412 9 2 3 5.2 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2[nH]1 10.1021/acs.jmedchem.1c01327
164616642 184672 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 412 9 2 3 5.2 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2[nH]1 10.1021/acs.jmedchem.1c01327
CHEMBL4848451 184672 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 412 9 2 3 5.2 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2[nH]1 10.1021/acs.jmedchem.1c01327
164610892 185304 None 0 Human Functional pEC50 = 5.8 5.8 -23 3
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 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4857560 185304 None 0 Human Functional pEC50 = 5.8 5.8 -23 3
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 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
127046949 139996 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799455 139996 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
25071385 159250 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098236 159250 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
56597226 148498 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 410 8 1 6 3.0 COc1ccccc1N1CCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
CHEMBL3937643 148498 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 410 8 1 6 3.0 COc1ccccc1N1CCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
25071385 159250 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098236 159250 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
164622475 186217 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 390 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4871762 186217 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 390 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164622475 186217 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 390 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4871762 186217 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 390 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
169450493 196205 None 2 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)
ChEMBL 518 8 3 5 3.1 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)OC(C)(C)C)C(=O)NCC(=O)NC12CC3CC(CC(C3)C1)C2 10.1021/acsmedchemlett.3c00264
CHEMBL5418802 196205 None 2 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)
ChEMBL 518 8 3 5 3.1 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)OC(C)(C)C)C(=O)NCC(=O)NC12CC3CC(CC(C3)C1)C2 10.1021/acsmedchemlett.3c00264
127045855 139751 None 0 Human Functional pEC50 = 6.8 6.8 -3 3
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 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797876 139751 None 0 Human Functional pEC50 = 6.8 6.8 -3 3
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 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL317488 213663 None 37 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human D2 receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation by measuring dopamine EC50 at 0.01 nM pretreated for 10 mins followed by forskolin stimulation for 5 mins and measured after 1 hr by HTRF assayPositive allosteric modulation of human D2 receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation by measuring dopamine EC50 at 0.01 nM pretreated for 10 mins followed by forskolin stimulation for 5 mins and measured after 1 hr by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c00252
122177643 121275 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577344 121275 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
164614549 185049 None 0 Human Functional pEC50 = 5.8 5.8 -74 3
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 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4853668 185049 None 0 Human Functional pEC50 = 5.8 5.8 -74 3
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 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
71722301 102528 None 0 Human Functional pEC50 = 6.8 6.8 4 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
CHEMBL3040157 102528 None 0 Human Functional pEC50 = 6.8 6.8 4 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
CHEMBL3216146 102528 None 0 Human Functional pEC50 = 6.8 6.8 4 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
13720686 11564 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
Dopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparation
ChEMBL 389 3 3 4 3.7 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1180562 11564 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
Dopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparation
ChEMBL 389 3 3 4 3.7 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL131313 11564 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
Dopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparation
ChEMBL 389 3 3 4 3.7 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
25071066 111837 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287390 111837 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
71660285 90650 None 0 Human Functional pEC50 = 6.8 6.8 -5 2
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 392 7 1 4 3.7 CCCN(CCN1CCN(c2ccccc2)CC1)[C@@H]1CCc2ccc(N)cc2C1 10.1016/j.bmc.2013.03.059
CHEMBL2387709 90650 None 0 Human Functional pEC50 = 6.8 6.8 -5 2
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 392 7 1 4 3.7 CCCN(CCN1CCN(c2ccccc2)CC1)[C@@H]1CCc2ccc(N)cc2C1 10.1016/j.bmc.2013.03.059
681 1465 None 47 Human Functional pEC50 = 7.8 7.8 -19 15
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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
681.0 1465 None 47 Human Functional pEC50 = 7.8 7.8 -19 15
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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 1465 None 47 Human Functional pEC50 = 7.8 7.8 -19 15
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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 1465 None 47 Human Functional pEC50 = 7.8 7.8 -19 15
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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 1465 None 47 Human Functional pEC50 = 7.8 7.8 -19 15
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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 1465 None 47 Human Functional pEC50 = 7.8 7.8 -19 15
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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
44554643 106326 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 259 2 1 3 2.0 Oc1cccc2c1C[C@H]1OCCN(CC3CC3)[C@@H]1C2 10.1016/j.bmc.2013.11.012
CHEMBL3099228 106326 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 259 2 1 3 2.0 Oc1cccc2c1C[C@H]1OCCN(CC3CC3)[C@@H]1C2 10.1016/j.bmc.2013.11.012
CHEMBL3139013 106326 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 259 2 1 3 2.0 Oc1cccc2c1C[C@H]1OCCN(CC3CC3)[C@@H]1C2 10.1016/j.bmc.2013.11.012
56599145 82010 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 447 7 1 4 4.3 O=C1NCCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc21 nan
CHEMBL2165133 82010 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 447 7 1 4 4.3 O=C1NCCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc21 nan
681 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2020.112709
681.0 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2020.112709
940 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2020.112709
947 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2020.112709
CHEMBL59 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2020.112709
DB00988 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2020.112709
161553599 184990 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 414 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4852808 184990 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 414 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
10637198 12484 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2ccc3nc(N)sc3c2C1 10.1021/jm000087z
CHEMBL118636 12484 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2ccc3nc(N)sc3c2C1 10.1021/jm000087z
161553599 184990 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 414 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4852808 184990 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 414 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
172463952 196538 None 0 Human Functional pEC50 = 7.7 7.7 4 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 196538 None 0 Human Functional pEC50 = 7.7 7.7 4 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
242 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795.0 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
164615867 185548 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4861553 185548 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
242 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
34 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
60795 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
60795.0 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
DB01238 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.3c00098
25071066 111837 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287390 111837 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
71452040 1091 None 1 Human Functional pEC50 = 6.7 6.7 -5 3
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 295 8 1 2 3.9 Oc1cccc(c1)CCN(CC1CC1)CCc1ccccc1 10.1021/jm301258w
9190 1091 None 1 Human Functional pEC50 = 6.7 6.7 -5 3
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 295 8 1 2 3.9 Oc1cccc(c1)CCN(CC1CC1)CCc1ccccc1 10.1021/jm301258w
CHEMBL2180638 1091 None 1 Human Functional pEC50 = 6.7 6.7 -5 3
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 295 8 1 2 3.9 Oc1cccc(c1)CCN(CC1CC1)CCc1ccccc1 10.1021/jm301258w
681 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
681.0 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
940 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
947 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
DB00988 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01031
24936042 157681 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4080762 157681 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
122189389 123311 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613875 123311 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
164938010 195433 None 0 Human Functional pEC50 = 4.7 4.7 -85 3
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 5 0 5 3.8 Cc1ccc2nc(CCCN3CCN(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
CHEMBL5403610 195433 None 0 Human Functional pEC50 = 4.7 4.7 -85 3
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 5 0 5 3.8 Cc1ccc2nc(CCCN3CCN(c4ccccn4)CC3)sc2c1 10.1021/acs.jmedchem.3c00734
681 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assayAgonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
681.0 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assayAgonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
940 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assayAgonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
947 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assayAgonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
CHEMBL59 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assayAgonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
DB00988 1465 None 47 Human Functional pEC50 = 7.7 7.7 -19 15
Agonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assayAgonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
2 3261 None 19 Human Functional pEC50 = 7.7 7.7 -10 7
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm301258w
54562 3261 None 19 Human Functional pEC50 = 7.7 7.7 -10 7
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm301258w
CHEMBL240773 3261 None 19 Human Functional pEC50 = 7.7 7.7 -10 7
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm301258w
5311189 207299 None 9 Rat Functional pEC50 = 7.7 7.7 -11 4
Effective concentration required for agonistic activity against rat D2 long receptorEffective concentration required for agonistic activity against rat D2 long receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
CHEMBL7549 207299 None 9 Rat Functional pEC50 = 7.7 7.7 -11 4
Effective concentration required for agonistic activity against rat D2 long receptorEffective concentration required for agonistic activity against rat D2 long receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
5311189 207299 None 9 Rat Functional pEC50 = 7.7 7.7 -11 4
Effective concentration required for agonistic activity against rat D2 short receptorEffective concentration required for agonistic activity against rat D2 short receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
CHEMBL7549 207299 None 9 Rat Functional pEC50 = 7.7 7.7 -11 4
Effective concentration required for agonistic activity against rat D2 short receptorEffective concentration required for agonistic activity against rat D2 short receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
146025784 171349 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 359 5 1 3 3.3 COc1cccc2c1CN(CC[C@H]1CC[C@H](NC(=O)N(C)C)CC1)CC2 10.1021/acs.jmedchem.9b00508
CHEMBL4460025 171349 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 359 5 1 3 3.3 COc1cccc2c1CN(CC[C@H]1CC[C@H](NC(=O)N(C)C)CC1)CC2 10.1021/acs.jmedchem.9b00508
242 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795.0 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 470 None 70 Human Functional pEC50 = 7.7 7.7 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
164615867 185548 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4861553 185548 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
172463952 196538 None 0 Human Functional pEC50 = 7.7 7.7 4 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 196538 None 0 Human Functional pEC50 = 7.7 7.7 4 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
146025784 171349 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 359 5 1 3 3.3 COc1cccc2c1CN(CC[C@H]1CC[C@H](NC(=O)N(C)C)CC1)CC2 10.1021/acs.jmedchem.9b00508
CHEMBL4460025 171349 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 359 5 1 3 3.3 COc1cccc2c1CN(CC[C@H]1CC[C@H](NC(=O)N(C)C)CC1)CC2 10.1021/acs.jmedchem.9b00508
24866612 189730 None 0 Human Functional pEC50 = 7.7 7.7 -72 2
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 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
CHEMBL514885 189730 None 0 Human Functional pEC50 = 7.7 7.7 -72 2
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 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
24936081 178742 None 0 Human Functional pEC50 = 7.7 7.7 -234 2
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
CHEMBL467540 178742 None 0 Human Functional pEC50 = 7.7 7.7 -234 2
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
24936042 157681 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4080762 157681 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
137640203 157054 None 0 Human Functional pEC50 = 6.7 6.7 -7 2
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 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
CHEMBL4072821 157054 None 0 Human Functional pEC50 = 6.7 6.7 -7 2
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 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
122189388 123310 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613874 123310 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
137640203 157054 None 0 Human Functional pEC50 = 6.7 6.7 -7 2
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 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
CHEMBL4072821 157054 None 0 Human Functional pEC50 = 6.7 6.7 -7 2
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 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
164622481 186219 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 406 11 2 4 4.5 COc1ccccc1C1CC1CNCCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4871774 186219 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 406 11 2 4 4.5 COc1ccccc1C1CC1CNCCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164622481 186219 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 406 11 2 4 4.5 COc1ccccc1C1CC1CNCCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4871774 186219 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 406 11 2 4 4.5 COc1ccccc1C1CC1CNCCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
122177642 121274 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 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
CHEMBL3577343 121274 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 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
21852778 175182 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 0 3 3.5 COc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4568388 175182 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 0 3 3.5 COc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
44320357 208857 None 0 Rat Functional pEC50 = 6.7 6.7 -54 2
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 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87734 208857 None 0 Rat Functional pEC50 = 6.7 6.7 -54 2
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 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
156785369 185962 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4867794 185962 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
156785369 185962 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4867794 185962 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
53328721 66456 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1851968 66456 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL3216523 66456 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
56599147 82006 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 443 4 1 4 4.1 O=C1CCc2ccc(OCC#CCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 10.1021/jm300603y
CHEMBL2165129 82006 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 443 4 1 4 4.1 O=C1CCc2ccc(OCC#CCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 10.1021/jm300603y
122189390 123312 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613876 123312 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
21852778 175182 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 0 3 3.5 COc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4568388 175182 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 0 3 3.5 COc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
10549689 51121 None 21 Human Functional pEC50 = 8.7 8.7 - 1
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 413 7 1 4 4.2 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4Cl)CC3)cc2N1 10.1021/jm300603y
CHEMBL157923 51121 None 21 Human Functional pEC50 = 8.7 8.7 - 1
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 413 7 1 4 4.2 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4Cl)CC3)cc2N1 10.1021/jm300603y
15124098 81999 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 437 9 1 5 4.3 CC(C)Oc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL2165121 81999 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 437 9 1 5 4.3 CC(C)Oc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
66559782 82003 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 446 7 1 3 5.9 O=C1CCc2ccc(OCCCCN3CCC(c4cccc(Cl)c4Cl)CC3)cc2N1 10.1021/jm300603y
CHEMBL2165125 82003 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 446 7 1 3 5.9 O=C1CCc2ccc(OCCCCN3CCC(c4cccc(Cl)c4Cl)CC3)cc2N1 10.1021/jm300603y
137660837 159173 None 0 Human Functional pEC50 = 8.7 8.7 -4 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 159173 None 0 Human Functional pEC50 = 8.7 8.7 -4 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
57242 3259 None 18 Human Functional pEC50 = 8.7 8.7 -9 4
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1016/j.bmcl.2007.10.059
954 3259 None 18 Human Functional pEC50 = 8.7 8.7 -9 4
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1016/j.bmcl.2007.10.059
CHEMBL155731 3259 None 18 Human Functional pEC50 = 8.7 8.7 -9 4
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1016/j.bmcl.2007.10.059
56597938 3940 None 4 Human Functional pEC50 = 8.7 8.7 204 2
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 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
7651 3940 None 4 Human Functional pEC50 = 8.7 8.7 204 2
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 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
CHEMBL2165126 3940 None 4 Human Functional pEC50 = 8.7 8.7 204 2
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 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
172460539 196501 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 9 2 5 4.3 COc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5425434 196501 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 9 2 5 4.3 COc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
163728602 186270 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4872467 186270 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164628178 186453 None 0 Human Functional pEC50 = 8.7 8.7 10 3
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186453 None 0 Human Functional pEC50 = 8.7 8.7 10 3
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
156785369 185962 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Partial agonist activity at D2R (unknown origin) expressed in HEK293 cellsPartial agonist activity at D2R (unknown origin) expressed in HEK293 cells
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1016/j.bmcl.2024.129654
CHEMBL4867794 185962 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Partial agonist activity at D2R (unknown origin) expressed in HEK293 cellsPartial agonist activity at D2R (unknown origin) expressed in HEK293 cells
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@@H]1C[C@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1016/j.bmcl.2024.129654
137660837 159173 None 0 Human Functional pEC50 = 8.7 8.7 -4 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 159173 None 0 Human Functional pEC50 = 8.7 8.7 -4 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
164628178 186453 None 0 Human Functional pEC50 = 8.7 8.7 10 3
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186453 None 0 Human Functional pEC50 = 8.7 8.7 10 3
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
155522454 170818 None 0 Human Functional pEC50 = 8.7 8.7 -2 2
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 403 10 2 6 4.4 CCCN(CCCCCc1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4452046 170818 None 0 Human Functional pEC50 = 8.7 8.7 -2 2
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 403 10 2 6 4.4 CCCN(CCCCCc1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
44554986 106340 None 0 Human Functional pEC50 = 8.7 8.7 35 2
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 361 4 1 5 2.9 CCCN1C[C@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099236 106340 None 0 Human Functional pEC50 = 8.7 8.7 35 2
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 361 4 1 5 2.9 CCCN1C[C@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139041 106340 None 0 Human Functional pEC50 = 8.7 8.7 35 2
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 361 4 1 5 2.9 CCCN1C[C@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
122177645 121277 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577346 121277 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
44438230 93610 None 2 Human Functional pEC50 = 8.7 8.7 9 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246439 93610 None 2 Human Functional pEC50 = 8.7 8.7 9 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
2 3261 None 19 Rat Functional pEC50 = 8.7 8.7 -21 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0000113
54562 3261 None 19 Rat Functional pEC50 = 8.7 8.7 -21 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0000113
CHEMBL240773 3261 None 19 Rat Functional pEC50 = 8.7 8.7 -21 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0000113
56598074 145764 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 445 6 1 4 4.8 O=c1ccc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
CHEMBL3916047 145764 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 445 6 1 4 4.8 O=c1ccc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
24742011 94367 None 0 Human Functional pEC50 = 8.7 8.7 -18 2
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 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
CHEMBL250552 94367 None 0 Human Functional pEC50 = 8.7 8.7 -18 2
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 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
169410194 196730 None 6 Human Functional pEC50 = 8.7 8.7 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5431103 196730 None 6 Human Functional pEC50 = 8.7 8.7 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
169410194 196730 None 6 Human Functional pEC50 = 8.7 8.7 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5431103 196730 None 6 Human Functional pEC50 = 8.7 8.7 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 441 8 1 4 4.2 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
172460748 196159 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 392 9 2 5 4.2 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5417857 196159 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 392 9 2 5 4.2 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
172460748 196159 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 392 9 2 5 4.2 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5417857 196159 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 392 9 2 5 4.2 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
11154555 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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
11154555.0 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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
11154555.0 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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 800 None 50 Human Functional pEC50 = 8.6 8.6 1 10
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 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
66559588 81998 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 459 7 1 4 5.2 O=c1ccc2ccc(OCCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 10.1021/jm300603y
CHEMBL2165120 81998 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 459 7 1 4 5.2 O=c1ccc2ccc(OCCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 10.1021/jm300603y
66559777 82000 None 1 Human Functional pEC50 = 8.6 8.6 - 1
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 447 7 1 4 4.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4C(F)(F)F)CC3)cc2N1 10.1021/jm300603y
CHEMBL2165122 82000 None 1 Human Functional pEC50 = 8.6 8.6 - 1
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 447 7 1 4 4.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4C(F)(F)F)CC3)cc2N1 10.1021/jm300603y
66633791 150955 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 8 1 5 3.9 COc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
CHEMBL3957278 150955 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 8 1 5 3.9 COc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
10895039 18527 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Effective concentration for Dopamine receptor D3 was determinedEffective concentration for Dopamine receptor D3 was determined
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm030836n
CHEMBL127400 18527 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Effective concentration for Dopamine receptor D3 was determinedEffective concentration for Dopamine receptor D3 was determined
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm030836n
CHEMBL129022 18527 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Effective concentration for Dopamine receptor D3 was determinedEffective concentration for Dopamine receptor D3 was determined
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm030836n
164619127 185631 None 0 Human Functional pEC50 = 8.6 8.6 8 3
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)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185631 None 0 Human Functional pEC50 = 8.6 8.6 8 3
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)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
10692886 53670 None 3 Human Functional pEC50 = 8.6 8.6 - 1
Partial agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayPartial agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL160296 53670 None 3 Human Functional pEC50 = 8.6 8.6 - 1
Partial agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayPartial agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL1813590 53670 None 3 Human Functional pEC50 = 8.6 8.6 - 1
Partial agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayPartial agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
172469898 197091 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 362 8 2 4 4.2 O=c1ccc2ccc(OCCCCNCc3cc4ccccc4o3)cc2[nH]1 10.1021/acs.jmedchem.3c00098
CHEMBL5438499 197091 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 362 8 2 4 4.2 O=c1ccc2ccc(OCCCCNCc3cc4ccccc4o3)cc2[nH]1 10.1021/acs.jmedchem.3c00098
164619127 185631 None 0 Human Functional pEC50 = 8.6 8.6 8 3
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)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185631 None 0 Human Functional pEC50 = 8.6 8.6 8 3
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)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
163728602 186270 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4872467 186270 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
172469898 197091 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 362 8 2 4 4.2 O=c1ccc2ccc(OCCCCNCc3cc4ccccc4o3)cc2[nH]1 10.1021/acs.jmedchem.3c00098
CHEMBL5438499 197091 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 362 8 2 4 4.2 O=c1ccc2ccc(OCCCCNCc3cc4ccccc4o3)cc2[nH]1 10.1021/acs.jmedchem.3c00098
46882005 5848 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 307 3 0 2 3.1 CN1CCCCC1CN1CCN(c2cccc(Cl)c2)C1=O 10.1016/j.bmcl.2010.01.090
CHEMBL1079190 5848 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 307 3 0 2 3.1 CN1CCCCC1CN1CCN(c2cccc(Cl)c2)C1=O 10.1016/j.bmcl.2010.01.090
127047859 140138 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800341 140138 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
164609095 184548 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 412 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4846472 184548 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 412 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
146025774 171837 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 397 4 1 2 4.6 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3c(ccc(Cl)c3Cl)C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4467173 171837 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 397 4 1 2 4.6 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3c(ccc(Cl)c3Cl)C2)CC1 10.1021/acs.jmedchem.9b00508
71722299 102535 None 0 Human Functional pEC50 = 8.6 8.6 3 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397383 102535 None 0 Human Functional pEC50 = 8.6 8.6 3 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040217 102535 None 0 Human Functional pEC50 = 8.6 8.6 3 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
66559588 81998 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 459 7 1 4 5.2 O=c1ccc2ccc(OCCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
CHEMBL2165120 81998 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 459 7 1 4 5.2 O=c1ccc2ccc(OCCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
9886609 165424 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Inhibition of [3H]thymidine uptake by Dopamine receptor D2Inhibition of [3H]thymidine uptake by Dopamine receptor D2
ChEMBL 388 5 1 3 5.0 c1ccc(N2CCN(CC[C@H]3CC[C@H](c4c[nH]c5ccccc54)CC3)CC2)nc1 10.1021/jm960597m
CHEMBL423499 165424 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Inhibition of [3H]thymidine uptake by Dopamine receptor D2Inhibition of [3H]thymidine uptake by Dopamine receptor D2
ChEMBL 388 5 1 3 5.0 c1ccc(N2CCN(CC[C@H]3CC[C@H](c4c[nH]c5ccccc54)CC3)CC2)nc1 10.1021/jm960597m
146025776 171191 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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](CCN2CCc3c(Cl)cccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4457507 171191 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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](CCN2CCc3c(Cl)cccc3C2)CC1 10.1021/acs.jmedchem.9b00508
164626610 186645 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 408 10 2 4 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4877827 186645 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 408 10 2 4 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
137633863 156716 None 0 Human Functional pEC50 = 8.5 8.5 -12 2
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(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 156716 None 0 Human Functional pEC50 = 8.5 8.5 -12 2
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(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
164626610 186645 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 408 10 2 4 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4877827 186645 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 408 10 2 4 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
137633863 156716 None 0 Human Functional pEC50 = 8.5 8.5 -12 2
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(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 156716 None 0 Human Functional pEC50 = 8.5 8.5 -12 2
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(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
122177645 121277 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577346 121277 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
172467076 196942 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 446 8 1 5 5.3 CC(C)Oc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5435325 196942 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 446 8 1 5 5.3 CC(C)Oc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
172467076 196942 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 446 8 1 5 5.3 CC(C)Oc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5435325 196942 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 446 8 1 5 5.3 CC(C)Oc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
60148497 80883 None 0 Human Functional pEC50 = 8.5 8.5 -2 2
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 438 7 2 6 3.6 CCCN(CCN1CCN(c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL2152633 80883 None 0 Human Functional pEC50 = 8.5 8.5 -2 2
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 438 7 2 6 3.6 CCCN(CCN1CCN(c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
2 3261 None 19 Human Functional pEC50 = 8.5 8.5 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3261 None 19 Human Functional pEC50 = 8.5 8.5 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.5 8.5 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
56599144 81994 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 433 7 2 3 5.2 O=c1[nH]c2ccc(OCCCCN3CCC(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 10.1021/jm300603y
CHEMBL2165115 81994 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 433 7 2 3 5.2 O=c1[nH]c2ccc(OCCCCN3CCC(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 10.1021/jm300603y
56597092 81996 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 433 6 1 4 3.9 O=C1NCCc2ccc(OCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc21 10.1021/jm300603y
CHEMBL2165117 81996 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 433 6 1 4 3.9 O=C1NCCc2ccc(OCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc21 10.1021/jm300603y
228 445 None 20 Human Functional pEC50 = 7.7 7.7 -3 20
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
33 445 None 20 Human Functional pEC50 = 7.7 7.7 -3 20
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
6005 445 None 20 Human Functional pEC50 = 7.7 7.7 -3 20
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
6005.0 445 None 20 Human Functional pEC50 = 7.7 7.7 -3 20
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
CHEMBL53 445 None 20 Human Functional pEC50 = 7.7 7.7 -3 20
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
DB00714 445 None 20 Human Functional pEC50 = 7.7 7.7 -3 20
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2007.10.059
44438236 154990 None 1 Human Functional pEC50 = 7.7 7.7 4 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 1 3 4.3 Cn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
CHEMBL400827 154990 None 1 Human Functional pEC50 = 7.7 7.7 4 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 1 3 4.3 Cn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
172444560 195514 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 8 2 5 4.3 COc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
CHEMBL5405133 195514 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 8 2 5 4.3 COc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
172444560 195514 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 8 2 5 4.3 COc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
CHEMBL5405133 195514 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 8 2 5 4.3 COc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
56597939 81995 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 6 1 4 4.5 Clc1cccc(N2CCN(CCCOc3ccc4cn[nH]c4c3)CC2)c1Cl 10.1021/jm300603y
CHEMBL2165116 81995 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 6 1 4 4.5 Clc1cccc(N2CCN(CCCOc3ccc4cn[nH]c4c3)CC2)c1Cl 10.1021/jm300603y
10811378 54231 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 407 7 1 4 4.2 Cc1cccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c1C 10.1021/jm300603y
CHEMBL160744 54231 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 407 7 1 4 4.2 Cc1cccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c1C 10.1021/jm300603y
127046950 140132 None 0 Human Functional pEC50 = 6.7 6.7 2 3
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 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800303 140132 None 0 Human Functional pEC50 = 6.7 6.7 2 3
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 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
681 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.7b00363
681.0 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.7b00363
940 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.7b00363
947 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.7b00363
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.7b00363
DB00988 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.7b00363
118725999 120952 None 0 Human Functional pEC50 = 6.7 6.7 -11 2
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 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394256 120952 None 0 Human Functional pEC50 = 6.7 6.7 -11 2
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 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3559222 120952 None 0 Human Functional pEC50 = 6.7 6.7 -11 2
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 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
44320257 208633 None 0 Rat Functional pEC50 = 6.7 6.7 -2 2
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 315 5 3 5 2.3 NC[C@@H]1OC(COCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86325 208633 None 0 Rat Functional pEC50 = 6.7 6.7 -2 2
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 315 5 3 5 2.3 NC[C@@H]1OC(COCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
118725999 120952 None 0 Human Functional pEC50 = 6.7 6.7 -11 2
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 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394256 120952 None 0 Human Functional pEC50 = 6.7 6.7 -11 2
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 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3559222 120952 None 0 Human Functional pEC50 = 6.7 6.7 -11 2
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 680 19 4 12 4.1 CCCN(CCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
681 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
681.0 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
940 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
947 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
DB00988 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.031
681 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
681.0 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
940 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
947 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
DB00988 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm070860r
681 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
681.0 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
940 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
947 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
DB00988 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.06.025
681 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
681.0 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
940 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
947 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
DB00988 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901618d
681 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
681.0 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
940 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
947 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
DB00988 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm901184n
681 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
681.0 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
940 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
947 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
DB00988 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm701524h
56597090 82014 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 434 7 0 4 6.6 Clc1cccc(C2CCN(CCCCOc3ccc4scnc4c3)CC2)c1Cl nan
CHEMBL2165137 82014 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 434 7 0 4 6.6 Clc1cccc(C2CCN(CCCCOc3ccc4scnc4c3)CC2)c1Cl nan
119570 3159 None 58 Rat Functional pEC50 = 7.7 7.7 -34 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1007/s00044-004-0006-x
119570.0 3159 None 58 Rat Functional pEC50 = 7.7 7.7 -34 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1007/s00044-004-0006-x
2233 3159 None 58 Rat Functional pEC50 = 7.7 7.7 -34 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1007/s00044-004-0006-x
953 3159 None 58 Rat Functional pEC50 = 7.7 7.7 -34 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1007/s00044-004-0006-x
CHEMBL301265 3159 None 58 Rat Functional pEC50 = 7.7 7.7 -34 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1007/s00044-004-0006-x
DB00413 3159 None 58 Rat Functional pEC50 = 7.7 7.7 -34 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1007/s00044-004-0006-x
90466717 157002 None 0 Human Functional pEC50 = 7.7 7.7 -5 2
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 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4072282 157002 None 0 Human Functional pEC50 = 7.7 7.7 -5 2
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 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
127037828 137009 None 0 Human Functional pEC50 = 7.7 7.7 -30 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3740778 137009 None 0 Human Functional pEC50 = 7.7 7.7 -30 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742429 137009 None 0 Human Functional pEC50 = 7.7 7.7 -30 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
164616128 184772 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 456 11 1 4 5.5 CCN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4849780 184772 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 456 11 1 4 5.5 CCN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
172464337 196969 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5435745 196969 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
164616128 184772 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 456 11 1 4 5.5 CCN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4849780 184772 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 456 11 1 4 5.5 CCN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
172464337 196969 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5435745 196969 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
56599146 144187 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 501 6 1 4 5.9 O=C1CCc2ccc(OCC3CCC(CN4CCN(c5cccc(Cl)c5Cl)CC4)CC3)cc2N1 nan
CHEMBL3903542 144187 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 501 6 1 4 5.9 O=C1CCc2ccc(OCC3CCC(CN4CCN(c5cccc(Cl)c5Cl)CC4)CC3)cc2N1 nan
53328719 66493 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1852163 66493 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL3216980 66493 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
44438209 154051 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 406 9 2 3 5.6 CCCCCCOc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL398368 154051 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 406 9 2 3 5.6 CCCCCCOc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
681 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
681.0 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
940 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
947 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
DB00988 1465 None 47 Human Functional pEC50 = 6.7 6.7 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
122179561 121596 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 375 9 2 4 3.4 CCCN(CCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585365 121596 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 375 9 2 4 3.4 CCCN(CCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
122179561 121596 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 375 9 2 4 3.4 CCCN(CCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585365 121596 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 375 9 2 4 3.4 CCCN(CCCNC(=O)OC(C)(C)C)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
101885473 121600 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 688 25 4 6 5.2 CCCN(CCCNC(=O)CCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585369 121600 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 688 25 4 6 5.2 CCCN(CCCNC(=O)CCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
101885473 121600 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 688 25 4 6 5.2 CCCN(CCCNC(=O)CCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585369 121600 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 688 25 4 6 5.2 CCCN(CCCNC(=O)CCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
155525527 171171 None 0 Human Functional pEC50 = 7.6 7.6 -8 2
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 389 9 3 6 4.1 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4457171 171171 None 0 Human Functional pEC50 = 7.6 7.6 -8 2
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 389 9 3 6 4.1 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
164617999 185182 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 392 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4855775 185182 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 392 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
25072633 159314 None 0 Human Functional pEC50 = 7.6 7.6 7 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 159314 None 0 Human Functional pEC50 = 7.6 7.6 7 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
164617999 185182 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 392 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4855775 185182 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 392 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
169753704 195382 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 402 7 0 5 5.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2cccnc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5402456 195382 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 402 7 0 5 5.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2cccnc2c1)CC3 10.1021/acs.jmedchem.3c00098
56598877 147483 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 424 8 1 6 3.3 COc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
CHEMBL3929710 147483 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 424 8 1 6 3.3 COc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
169753704 195382 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 402 7 0 5 5.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2cccnc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5402456 195382 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 402 7 0 5 5.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2cccnc2c1)CC3 10.1021/acs.jmedchem.3c00098
44438222 93544 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 349 3 1 2 4.9 N#CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246230 93544 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 349 3 1 2 4.9 N#CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
681 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
681.0 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
940 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
947 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
DB00988 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm300268s
681 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
681.0 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
940 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
947 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
DB00988 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.03.059
131801150 171859 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293T cells co-expressing luciferase based cAMP biosensor assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by microbeta luminescence counting assayAgonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293T cells co-expressing luciferase based cAMP biosensor assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by microbeta luminescence counting assay
ChEMBL 446 7 1 5 4.4 Cc1cc2c(N3CCN(CCCCOc4ccc5c(c4)NC(=O)CC5)CC3)cccc2n1C 10.1021/acs.jmedchem.8b00435
CHEMBL4467404 171859 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293T cells co-expressing luciferase based cAMP biosensor assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by microbeta luminescence counting assayAgonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293T cells co-expressing luciferase based cAMP biosensor assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by microbeta luminescence counting assay
ChEMBL 446 7 1 5 4.4 Cc1cc2c(N3CCN(CCCCOc4ccc5c(c4)NC(=O)CC5)CC3)cccc2n1C 10.1021/acs.jmedchem.8b00435
25072633 159314 None 0 Human Functional pEC50 = 7.6 7.6 7 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 159314 None 0 Human Functional pEC50 = 7.6 7.6 7 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
11515697 178337 None 0 Rat Functional pEC50 = 7.6 7.6 -1 2
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 343 1 2 3 4.5 CN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL458397 178337 None 0 Rat Functional pEC50 = 7.6 7.6 -1 2
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 343 1 2 3 4.5 CN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL465054 178337 None 0 Rat Functional pEC50 = 7.6 7.6 -1 2
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 343 1 2 3 4.5 CN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
56598070 81993 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 449 7 0 5 6.0 Clc1cccc(N2CCCN(CCCCOc3ccc4scnc4c3)CC2)c1Cl nan
CHEMBL2165114 81993 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 449 7 0 5 6.0 Clc1cccc(N2CCCN(CCCCOc3ccc4scnc4c3)CC2)c1Cl nan
172449834 195954 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 416 6 1 5 4.3 COc1cccc2c3c(oc12)CN(C/C=C/COc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5414097 195954 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 416 6 1 5 4.3 COc1cccc2c3c(oc12)CN(C/C=C/COc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
164613755 185428 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 420 9 2 5 3.9 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4c3OCCO4)cc2[nH]1 10.1021/acs.jmedchem.1c01327
CHEMBL4859567 185428 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 420 9 2 5 3.9 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4c3OCCO4)cc2[nH]1 10.1021/acs.jmedchem.1c01327
164613755 185428 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 420 9 2 5 3.9 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4c3OCCO4)cc2[nH]1 10.1021/acs.jmedchem.1c01327
CHEMBL4859567 185428 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 420 9 2 5 3.9 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4c3OCCO4)cc2[nH]1 10.1021/acs.jmedchem.1c01327
172449834 195954 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 416 6 1 5 4.3 COc1cccc2c3c(oc12)CN(C/C=C/COc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5414097 195954 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 416 6 1 5 4.3 COc1cccc2c3c(oc12)CN(C/C=C/COc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL317488 213663 None 37 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1)C(=O)NCC(N)=O 10.1021/acsmedchemlett.3c00264
172463952 196538 None 0 Human Functional pEC50 = 7.6 7.6 4 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 196538 None 0 Human Functional pEC50 = 7.6 7.6 4 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
2 3261 None 19 Human Functional pEC50 = 6.6 6.6 -10 7
Intrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS 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 3261 None 19 Human Functional pEC50 = 6.6 6.6 -10 7
Intrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS 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 3261 None 19 Human Functional pEC50 = 6.6 6.6 -10 7
Intrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
2 3261 None 19 Human Functional pEC50 = 5.6 5.6 -10 7
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
54562 3261 None 19 Human Functional pEC50 = 5.6 5.6 -10 7
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
CHEMBL240773 3261 None 19 Human Functional pEC50 = 5.6 5.6 -10 7
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
44427823 93276 None 0 Human Functional pEC50 = 6.6 6.6 -60 2
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 496 7 1 4 4.4 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccc[n+]2[O-])cc1 10.1021/jm0704200
CHEMBL244774 93276 None 0 Human Functional pEC50 = 6.6 6.6 -60 2
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 496 7 1 4 4.4 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccc[n+]2[O-])cc1 10.1021/jm0704200
25071691 111850 None 0 Human Functional pEC50 = 6.6 6.6 -2 2
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 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111850 None 0 Human Functional pEC50 = 6.6 6.6 -2 2
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 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
172447344 195758 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 7 0 6 5.3 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2scnc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5410217 195758 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 7 0 6 5.3 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2scnc2c1)CC3 10.1021/acs.jmedchem.3c00098
172447344 195758 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 7 0 6 5.3 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2scnc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5410217 195758 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 7 0 6 5.3 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2scnc2c1)CC3 10.1021/acs.jmedchem.3c00098
53327665 66501 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 400 4 3 7 2.4 COC(=O)[C@@H](N)CSc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.ejmech.2011.04.028
CHEMBL1852240 66501 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 400 4 3 7 2.4 COC(=O)[C@@H](N)CSc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.ejmech.2011.04.028
CHEMBL3216759 66501 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 400 4 3 7 2.4 COC(=O)[C@@H](N)CSc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.ejmech.2011.04.028
172463952 196538 None 0 Human Functional pEC50 = 7.6 7.6 4 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 196538 None 0 Human Functional pEC50 = 7.6 7.6 4 4
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
172461590 196841 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 406 6 1 5 4.2 COc1cccc2c3c(oc12)CN(CCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5433201 196841 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 406 6 1 5 4.2 COc1cccc2c3c(oc12)CN(CCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
172461590 196841 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 406 6 1 5 4.2 COc1cccc2c3c(oc12)CN(CCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5433201 196841 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 406 6 1 5 4.2 COc1cccc2c3c(oc12)CN(CCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
44438220 93503 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 381 4 2 2 4.4 CC(=O)NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246021 93503 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 381 4 2 2 4.4 CC(=O)NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
2 3261 None 19 Human Functional pEC50 = 6.6 6.6 -10 7
Agonist activity at dopamine D2 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assayAgonist activity at dopamine D2 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2009.06.019
54562 3261 None 19 Human Functional pEC50 = 6.6 6.6 -10 7
Agonist activity at dopamine D2 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assayAgonist activity at dopamine D2 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2009.06.019
CHEMBL240773 3261 None 19 Human Functional pEC50 = 6.6 6.6 -10 7
Agonist activity at dopamine D2 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assayAgonist activity at dopamine D2 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2009.06.019
137642380 158599 None 0 Human Functional pEC50 = 6.6 6.6 -5 2
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 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4091155 158599 None 0 Human Functional pEC50 = 6.6 6.6 -5 2
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 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
681 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
681.0 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
940 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
947 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
DB00988 1465 None 47 Human Functional pEC50 = 6.6 6.6 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/ml3002117
25071691 111850 None 0 Human Functional pEC50 = 6.6 6.6 -2 2
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 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111850 None 0 Human Functional pEC50 = 6.6 6.6 -2 2
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 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
10025039 78841 None 0 Human Functional pEC50 = 6.6 6.6 4 2
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
CHEMBL2112745 78841 None 0 Human Functional pEC50 = 6.6 6.6 4 2
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
71733932 91086 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2397389 91086 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
56598070 81993 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 449 7 0 5 6.0 Clc1cccc(N2CCCN(CCCCOc3ccc4scnc4c3)CC2)c1Cl 10.1021/jm300603y
CHEMBL2165114 81993 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 449 7 0 5 6.0 Clc1cccc(N2CCCN(CCCCOc3ccc4scnc4c3)CC2)c1Cl 10.1021/jm300603y
15124098 81999 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 437 9 1 5 4.3 CC(C)Oc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL2165121 81999 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 437 9 1 5 4.3 CC(C)Oc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
66559777 82000 None 1 Human Functional pEC50 = 7.6 7.6 - 1
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 4.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4C(F)(F)F)CC3)cc2N1 10.1021/jm300603y
CHEMBL2165122 82000 None 1 Human Functional pEC50 = 7.6 7.6 - 1
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 4.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4C(F)(F)F)CC3)cc2N1 10.1021/jm300603y
127047996 139733 None 0 Human Functional pEC50 = 7.6 7.6 28 2
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 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797758 139733 None 0 Human Functional pEC50 = 7.6 7.6 28 2
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 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
13851600 130701 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 217 0 1 2 2.2 CN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099223 130701 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 217 0 1 2 2.2 CN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL368188 130701 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 217 0 1 2 2.2 CN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
56599144 81994 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 433 7 2 3 5.2 O=c1[nH]c2ccc(OCCCCN3CCC(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
CHEMBL2165115 81994 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 433 7 2 3 5.2 O=c1[nH]c2ccc(OCCCCN3CCC(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
56597094 148145 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 2 4 3.8 O=c1[nH]c2ccc(OCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
CHEMBL3934712 148145 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 2 4 3.8 O=c1[nH]c2ccc(OCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
11983282 139030 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
Intrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 139030 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
Intrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
167715 2876 None 8 Human Functional pEC50 = 7.6 7.6 6 4
Activity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayActivity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm049484q
969 2876 None 8 Human Functional pEC50 = 7.6 7.6 6 4
Activity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayActivity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm049484q
CHEMBL225230 2876 None 8 Human Functional pEC50 = 7.6 7.6 6 4
Activity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayActivity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm049484q
137635157 155882 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 435 13 1 5 4.5 CCCN[C@@H]1Cc2cccc3c2n(c(=O)n3CCCCOCCCCc2ccccc2)C1 10.1021/acs.jmedchem.6b01875
CHEMBL4059581 155882 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 435 13 1 5 4.5 CCCN[C@@H]1Cc2cccc3c2n(c(=O)n3CCCCOCCCCc2ccccc2)C1 10.1021/acs.jmedchem.6b01875
137660837 159173 None 0 Human Functional pEC50 = 7.6 7.6 -4 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 159173 None 0 Human Functional pEC50 = 7.6 7.6 -4 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
172469898 197091 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 362 8 2 4 4.2 O=c1ccc2ccc(OCCCCNCc3cc4ccccc4o3)cc2[nH]1 10.1021/acs.jmedchem.3c00098
CHEMBL5438499 197091 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 362 8 2 4 4.2 O=c1ccc2ccc(OCCCCNCc3cc4ccccc4o3)cc2[nH]1 10.1021/acs.jmedchem.3c00098
172469898 197091 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 362 8 2 4 4.2 O=c1ccc2ccc(OCCCCNCc3cc4ccccc4o3)cc2[nH]1 10.1021/acs.jmedchem.3c00098
CHEMBL5438499 197091 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 362 8 2 4 4.2 O=c1ccc2ccc(OCCCCNCc3cc4ccccc4o3)cc2[nH]1 10.1021/acs.jmedchem.3c00098
25072002 156205 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
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(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 156205 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
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(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
71460601 82002 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 423 9 1 5 4.0 CCOc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1021/jm300603y
CHEMBL2165124 82002 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 423 9 1 5 4.0 CCOc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1021/jm300603y
14289494 82004 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 433 6 1 4 4.5 O=C1CCc2ccc(OCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 10.1021/jm300603y
CHEMBL2165127 82004 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 433 6 1 4 4.5 O=C1CCc2ccc(OCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 10.1021/jm300603y
25072002 156205 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
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(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 156205 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
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(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
13720690 13095 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Dopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparation
ChEMBL 311 3 3 4 3.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1190300 13095 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Dopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparation
ChEMBL 311 3 3 4 3.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL540575 13095 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Dopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparationDopamine receptor D2 agonist activity was determined for inhibition of the constrictor response to electrical stimulation in an isolated perfused rabbit ear artery preparation
ChEMBL 311 3 3 4 3.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccc(O)cc2)C1 10.1021/jm00384a006
137649770 157418 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 420 7 2 6 2.7 CN[C@@H]1Cc2cccc3c2n(c(=O)n3CCCCOc2ccc3c(c2)NC(=O)CC3)C1 10.1021/acs.jmedchem.6b01875
CHEMBL4077430 157418 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 420 7 2 6 2.7 CN[C@@H]1Cc2cccc3c2n(c(=O)n3CCCCOc2ccc3c(c2)NC(=O)CC3)C1 10.1021/acs.jmedchem.6b01875
72736203 103617 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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
CHEMBL3085816 103617 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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
72736203 103617 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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
CHEMBL3085816 103617 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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
137660837 159173 None 0 Human Functional pEC50 = 7.6 7.6 -4 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 159173 None 0 Human Functional pEC50 = 7.6 7.6 -4 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
52937876 61194 None 0 Human Functional pEC50 = 7.6 7.6 -489 2
Agonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation countingAgonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation counting
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765633 61194 None 0 Human Functional pEC50 = 7.6 7.6 -489 2
Agonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation countingAgonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation counting
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
66633745 143354 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 445 6 1 4 4.6 O=C1CCc2ccc(OC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 nan
CHEMBL3896746 143354 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 445 6 1 4 4.6 O=C1CCc2ccc(OC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1 nan
172459790 196485 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5424897 196485 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
164613755 185428 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 420 9 2 5 3.9 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4c3OCCO4)cc2[nH]1 10.1021/acs.jmedchem.1c01327
CHEMBL4859567 185428 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 420 9 2 5 3.9 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc4c3OCCO4)cc2[nH]1 10.1021/acs.jmedchem.1c01327
164623044 186274 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 392 10 2 4 4.1 COc1ccccc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4872548 186274 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 392 10 2 4 4.1 COc1ccccc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
172459790 196485 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5424897 196485 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
172450793 197429 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)
ChEMBL 418 8 4 4 1.5 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1)C(=O)NCC(=O)NC12CC3CC(CC(C3)C1)C2 10.1021/acsmedchemlett.3c00264
CHEMBL5406031 197429 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)
ChEMBL 418 8 4 4 1.5 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1)C(=O)NCC(=O)NC12CC3CC(CC(C3)C1)C2 10.1021/acsmedchemlett.3c00264
CHEMBL5499160 197429 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)Positive allosteric modulator activity at human dopamine D2 receptor expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP level preincubated for 10 mins followed by forskolin addition measured after 5 mins in presence of dopamine by HTRF assay (Rvb = 87.08 +/- 24.87 nM)
ChEMBL 418 8 4 4 1.5 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1)C(=O)NCC(=O)NC12CC3CC(CC(C3)C1)C2 10.1021/acsmedchemlett.3c00264
172468042 196585 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 404 6 1 5 4.1 COc1cccc2c3c(oc12)CN(CCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5427288 196585 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 404 6 1 5 4.1 COc1cccc2c3c(oc12)CN(CCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
172467420 196886 None 0 Human Functional pEC50 = 7.6 7.6 -8 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 442 8 1 5 3.3 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5434229 196886 None 0 Human Functional pEC50 = 7.6 7.6 -8 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 442 8 1 5 3.3 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1 10.1021/acs.jmedchem.2c01624
172468042 196585 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 404 6 1 5 4.1 COc1cccc2c3c(oc12)CN(CCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5427288 196585 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 404 6 1 5 4.1 COc1cccc2c3c(oc12)CN(CCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
146025782 173677 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 347 4 1 2 3.4 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(F)c3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4532767 173677 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 347 4 1 2 3.4 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(F)c3C2)CC1 10.1021/acs.jmedchem.9b00508
44438211 147550 None 1 Human Functional pEC50 = 6.6 6.6 - 1
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 2 2 4.7 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL393027 147550 None 1 Human Functional pEC50 = 6.6 6.6 - 1
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 2 2 4.7 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
172449681 195826 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 450 12 1 5 5.8 CCCN(CCCCOc1ccc2c(c1)NC(=O)CC2)Cc1cc2cccc(OCC)c2o1 10.1021/acs.jmedchem.3c00098
CHEMBL5411545 195826 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 450 12 1 5 5.8 CCCN(CCCCOc1ccc2c(c1)NC(=O)CC2)Cc1cc2cccc(OCC)c2o1 10.1021/acs.jmedchem.3c00098
172449047 195971 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4oc(C)nc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5414422 195971 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4oc(C)nc4c3)oc12 10.1021/acs.jmedchem.3c00098
24759792 184514 None 0 Human Functional pEC50 = 6.6 6.6 -190 2
Activation of human dopamine D2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 286 2 1 3 2.0 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)CNC4=O 10.1016/j.bmcl.2009.03.015
CHEMBL484598 184514 None 0 Human Functional pEC50 = 6.6 6.6 -190 2
Activation of human dopamine D2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 286 2 1 3 2.0 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)CNC4=O 10.1016/j.bmcl.2009.03.015
172444560 195514 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 8 2 5 4.3 COc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
CHEMBL5405133 195514 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 8 2 5 4.3 COc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
172449681 195826 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 450 12 1 5 5.8 CCCN(CCCCOc1ccc2c(c1)NC(=O)CC2)Cc1cc2cccc(OCC)c2o1 10.1021/acs.jmedchem.3c00098
CHEMBL5411545 195826 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 450 12 1 5 5.8 CCCN(CCCCOc1ccc2c(c1)NC(=O)CC2)Cc1cc2cccc(OCC)c2o1 10.1021/acs.jmedchem.3c00098
164622330 185968 None 0 Human Functional pEC50 = 5.6 5.6 -11 2
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 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4867962 185968 None 0 Human Functional pEC50 = 5.6 5.6 -11 2
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 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
172449047 195971 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4oc(C)nc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5414422 195971 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4oc(C)nc4c3)oc12 10.1021/acs.jmedchem.3c00098
119570 3159 None 58 Human Functional pEC50 = 7.6 7.6 -28 11
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
119570.0 3159 None 58 Human Functional pEC50 = 7.6 7.6 -28 11
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
2233 3159 None 58 Human Functional pEC50 = 7.6 7.6 -28 11
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
953 3159 None 58 Human Functional pEC50 = 7.6 7.6 -28 11
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
CHEMBL301265 3159 None 58 Human Functional pEC50 = 7.6 7.6 -28 11
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
DB00413 3159 None 58 Human Functional pEC50 = 7.6 7.6 -28 11
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
146025782 173677 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 347 4 1 2 3.4 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(F)c3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4532767 173677 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 347 4 1 2 3.4 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3cccc(F)c3C2)CC1 10.1021/acs.jmedchem.9b00508
66633584 149296 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 435 9 1 5 4.3 CCOc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
CHEMBL3944009 149296 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 435 9 1 5 4.3 CCOc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
172467420 196886 None 0 Human Functional pEC50 = 7.6 7.6 -8 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 442 8 1 5 3.3 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5434229 196886 None 0 Human Functional pEC50 = 7.6 7.6 -8 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 442 8 1 5 3.3 COCCC(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(C(F)(F)F)n3)CC2)CC1 10.1021/acs.jmedchem.2c01624
164615405 185392 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 430 9 2 3 5.4 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2[nH]1 10.1021/acs.jmedchem.1c01327
CHEMBL4859080 185392 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 430 9 2 3 5.4 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2[nH]1 10.1021/acs.jmedchem.1c01327
164615405 185392 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 430 9 2 3 5.4 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2[nH]1 10.1021/acs.jmedchem.1c01327
CHEMBL4859080 185392 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 430 9 2 3 5.4 O=c1ccc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2[nH]1 10.1021/acs.jmedchem.1c01327
2 3261 None 19 Human Functional pEC50 = 6.6 6.6 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.7b00363
54562 3261 None 19 Human Functional pEC50 = 6.6 6.6 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.7b00363
CHEMBL240773 3261 None 19 Human Functional pEC50 = 6.6 6.6 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.7b00363
25093832 155970 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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 155970 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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
25071691 111850 None 0 Human Functional pEC50 = 6.6 6.6 -2 2
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 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111850 None 0 Human Functional pEC50 = 6.6 6.6 -2 2
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 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
172444560 195514 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 8 2 5 4.3 COc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
CHEMBL5405133 195514 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 8 2 5 4.3 COc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
2 3261 None 19 Human Functional pEC50 = 5.6 5.6 -10 7
Intrinsic activity at human dopamine D2L 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 D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
54562 3261 None 19 Human Functional pEC50 = 5.6 5.6 -10 7
Intrinsic activity at human dopamine D2L 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 D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
CHEMBL240773 3261 None 19 Human Functional pEC50 = 5.6 5.6 -10 7
Intrinsic activity at human dopamine D2L 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 D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
25093832 155970 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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 155970 None 0 Human Functional pEC50 = 6.6 6.6 2 2
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
25071691 111850 None 0 Human Functional pEC50 = 6.6 6.6 -2 2
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 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111850 None 0 Human Functional pEC50 = 6.6 6.6 -2 2
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 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
137647058 158087 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 467 15 1 7 3.0 CN[C@@H]1Cc2cccc3c2n(c(=O)n3CCOCCOCCOCCCCc2ccccc2)C1 10.1021/acs.jmedchem.6b01875
CHEMBL4085282 158087 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 467 15 1 7 3.0 CN[C@@H]1Cc2cccc3c2n(c(=O)n3CCOCCOCCOCCCCc2ccccc2)C1 10.1021/acs.jmedchem.6b01875
101885474 121599 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 632 21 4 6 3.7 CCCN(CCCNC(=O)CCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585368 121599 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 632 21 4 6 3.7 CCCN(CCCNC(=O)CCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
122177641 121273 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 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 121273 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 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
2 3261 None 19 Human Functional pEC50 = 7.6 7.6 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00692
54562 3261 None 19 Human Functional pEC50 = 7.6 7.6 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00692
CHEMBL240773 3261 None 19 Human Functional pEC50 = 7.6 7.6 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00692
101885474 121599 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 632 21 4 6 3.7 CCCN(CCCNC(=O)CCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585368 121599 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 632 21 4 6 3.7 CCCN(CCCNC(=O)CCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
2 3261 None 19 Human Functional pEC50 = 7.6 7.6 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2021.113190
54562 3261 None 19 Human Functional pEC50 = 7.6 7.6 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2021.113190
CHEMBL240773 3261 None 19 Human Functional pEC50 = 7.6 7.6 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2021.113190
CHEMBL5078216 217032 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human D2 receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation by measuring dopamine EC50 at 0.01 nM pretreated for 10 mins followed by forskolin stimulation for 5 mins and measured after 1 hr by HTRF assayPositive allosteric modulation of human D2 receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation by measuring dopamine EC50 at 0.01 nM pretreated for 10 mins followed by forskolin stimulation for 5 mins and measured after 1 hr by HTRF assay
ChEMBL None None None COC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)c1ccoc1 10.1021/acs.jmedchem.1c00252
2 3261 None 19 Human Functional pEC50 = 5.6 5.6 -10 7
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
54562 3261 None 19 Human Functional pEC50 = 5.6 5.6 -10 7
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
CHEMBL240773 3261 None 19 Human Functional pEC50 = 5.6 5.6 -10 7
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
14809026 208245 None 1 Rat Functional pEC50 = 5.5 5.5 2 2
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](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL83080 208245 None 1 Rat Functional pEC50 = 5.5 5.5 2 2
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](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
13864380 208890 None 1 Rat Functional pEC50 = 5.5 5.5 -5 2
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 195 1 3 4 0.7 NC[C@@H]1OCCc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87958 208890 None 1 Rat Functional pEC50 = 5.5 5.5 -5 2
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 195 1 3 4 0.7 NC[C@@H]1OCCc2c1ccc(O)c2O 10.1021/jm00112a034
13864381 210803 None 1 Rat Functional pEC50 = 5.5 5.5 -5 3
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 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL542683 210803 None 1 Rat Functional pEC50 = 5.5 5.5 -5 3
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 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL99361 210803 None 1 Rat Functional pEC50 = 5.5 5.5 -5 3
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 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
44320123 107139 None 0 Rat Functional pEC50 = 6.5 6.5 -4 2
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 233 2 3 4 1.1 C#CCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL315849 107139 None 0 Rat Functional pEC50 = 6.5 6.5 -4 2
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 233 2 3 4 1.1 C#CCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
164622475 186217 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 390 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4871762 186217 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 390 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164937999 197010 None 0 Human Functional pEC50 = 7.5 7.5 -8 3
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 6 0 5 3.8 c1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL5436702 197010 None 0 Human Functional pEC50 = 7.5 7.5 -8 3
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 352 6 0 5 3.8 c1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
137644833 158231 None 0 Human Functional pEC50 = 5.5 5.5 -95 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4087187 158231 None 0 Human Functional pEC50 = 5.5 5.5 -95 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
122177642 121274 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 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
CHEMBL3577343 121274 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 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
162650164 180198 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 1205 38 2 15 10.9 CCCN(CCCCNC(=O)c1ccc(-c2ccc(OCc3cn(CCOCCOCCOCCn4cc(COc5ccc(-c6ccc(C(=O)NCCCCN(CCC)C7Cc8ccccc8C7)cc6)cc5)nn4)nn3)cc2)cc1)C1Cc2ccccc2C1 10.1016/j.ejmech.2020.113151
CHEMBL4748201 180198 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 1205 38 2 15 10.9 CCCN(CCCCNC(=O)c1ccc(-c2ccc(OCc3cn(CCOCCOCCOCCn4cc(COc5ccc(-c6ccc(C(=O)NCCCCN(CCC)C7Cc8ccccc8C7)cc6)cc5)nn4)nn3)cc2)cc1)C1Cc2ccccc2C1 10.1016/j.ejmech.2020.113151
172459921 196115 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 396 10 1 6 5.4 CCOc1cccc2cc(CNCCCCOc3ccc4scnc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5417227 196115 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 396 10 1 6 5.4 CCOc1cccc2cc(CNCCCCOc3ccc4scnc4c3)oc12 10.1021/acs.jmedchem.3c00098
172459921 196115 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 396 10 1 6 5.4 CCOc1cccc2cc(CNCCCCOc3ccc4scnc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5417227 196115 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 396 10 1 6 5.4 CCOc1cccc2cc(CNCCCCOc3ccc4scnc4c3)oc12 10.1021/acs.jmedchem.3c00098
155568278 176210 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 347 2 2 3 3.6 CN1CCc2cc(O)c(O)cc2C1Cc1ccccc1Br 10.1021/acs.jnatprod.9b00921
CHEMBL4591554 176210 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 347 2 2 3 3.6 CN1CCc2cc(O)c(O)cc2C1Cc1ccccc1Br 10.1021/acs.jnatprod.9b00921
155568278 176210 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 347 2 2 3 3.6 CN1CCc2cc(O)c(O)cc2C1Cc1ccccc1Br 10.1021/acs.jnatprod.9b00921
CHEMBL4591554 176210 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 347 2 2 3 3.6 CN1CCc2cc(O)c(O)cc2C1Cc1ccccc1Br 10.1021/acs.jnatprod.9b00921
164609017 184531 None 0 Human Functional pEC50 = 5.5 5.5 -7 3
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 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4846201 184531 None 0 Human Functional pEC50 = 5.5 5.5 -7 3
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 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
172456605 196210 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4c(C)noc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5418890 196210 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4c(C)noc4c3)oc12 10.1021/acs.jmedchem.3c00098
145986176 165667 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 404 9 2 3 4.6 C#CCCC(=O)Nc1ccc(CCN(CCC)C2CCc3c(O)cccc3C2)cc1 10.1021/acs.jmedchem.8b00671
CHEMBL4242192 165667 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 404 9 2 3 4.6 C#CCCC(=O)Nc1ccc(CCN(CCC)C2CCc3c(O)cccc3C2)cc1 10.1021/acs.jmedchem.8b00671
11983282 139030 None 0 Human Functional pEC50 = 8.5 8.5 -2 3
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 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 139030 None 0 Human Functional pEC50 = 8.5 8.5 -2 3
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 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
11154555 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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
11154555.0 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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
146025776 171191 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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](CCN2CCc3c(Cl)cccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4457507 171191 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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](CCN2CCc3c(Cl)cccc3C2)CC1 10.1021/acs.jmedchem.9b00508
146025774 171837 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 397 4 1 2 4.6 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3c(ccc(Cl)c3Cl)C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4467173 171837 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 397 4 1 2 4.6 CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCc3c(ccc(Cl)c3Cl)C2)CC1 10.1021/acs.jmedchem.9b00508
2 3261 None 19 Human Functional pEC50 = 8.5 8.5 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3261 None 19 Human Functional pEC50 = 8.5 8.5 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.5 8.5 -10 7
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 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
137655953 159094 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 420 7 2 5 2.9 CN(CCCCOc1ccc2c(c1)NC(=O)CC2)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.6b01875
CHEMBL4096422 159094 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 420 7 2 5 2.9 CN(CCCCOc1ccc2c(c1)NC(=O)CC2)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.6b01875
56597937 146129 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 447 6 1 4 4.9 O=C1CCc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2N1 nan
CHEMBL3918805 146129 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 447 6 1 4 4.9 O=C1CCc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2N1 nan
122177645 121277 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Intrinsic activity at human dopamine D2L 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 D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577346 121277 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Intrinsic activity at human dopamine D2L 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 D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
11213062 61947 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 448 7 1 5 4.3 O=C1CCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nc2N1 10.1021/jm300603y
CHEMBL1774063 61947 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 448 7 1 5 4.3 O=C1CCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nc2N1 10.1021/jm300603y
11794899 119635 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 393 7 1 4 3.9 Cc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL346129 119635 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 393 7 1 4 3.9 Cc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
162654269 180782 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 843 34 0 13 6.1 CCCN(CCCCc1cn(CCOCCOCCOCCOCCOCCn2cc(CCCCN(CCC)C3Cc4ccccc4C3)nn2)nn1)C1Cc2ccccc2C1 10.1016/j.ejmech.2020.113151
CHEMBL4755336 180782 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 843 34 0 13 6.1 CCCN(CCCCc1cn(CCOCCOCCOCCOCCOCCn2cc(CCCCN(CCC)C3Cc4ccccc4C3)nn2)nn1)C1Cc2ccccc2C1 10.1016/j.ejmech.2020.113151
2407 3372 None 50 Human Functional pEC50 = 8.5 8.5 -1 17
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 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/acs.jmedchem.7b00363
59227 3372 None 50 Human Functional pEC50 = 8.5 8.5 -1 17
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 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/acs.jmedchem.7b00363
59227.0 3372 None 50 Human Functional pEC50 = 8.5 8.5 -1 17
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 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/acs.jmedchem.7b00363
941 3372 None 50 Human Functional pEC50 = 8.5 8.5 -1 17
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 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/acs.jmedchem.7b00363
CHEMBL1303 3372 None 50 Human Functional pEC50 = 8.5 8.5 -1 17
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 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/acs.jmedchem.7b00363
DB05271 3372 None 50 Human Functional pEC50 = 8.5 8.5 -1 17
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 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/acs.jmedchem.7b00363
127037825 137006 None 0 Human Functional pEC50 = 8.5 8.5 -2 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3740041 137006 None 0 Human Functional pEC50 = 8.5 8.5 -2 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742426 137006 None 0 Human Functional pEC50 = 8.5 8.5 -2 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
11154555 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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
11154555.0 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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 800 None 50 Human Functional pEC50 = 8.5 8.5 1 10
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
145984484 165649 None 0 Human Functional pEC50 = 8.5 8.5 51 2
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 930 28 3 12 8.6 CCCN(CCc1ccc(NC(=O)CCc2cn(CCCCCCCCN(C)CCCCCNC(=O)COc3cncc(C#Cc4csc(C)n4)c3)nn2)cc1)C1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.8b00671
CHEMBL4241844 165649 None 0 Human Functional pEC50 = 8.5 8.5 51 2
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 930 28 3 12 8.6 CCCN(CCc1ccc(NC(=O)CCc2cn(CCCCCCCCN(C)CCCCCNC(=O)COc3cncc(C#Cc4csc(C)n4)c3)nn2)cc1)C1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.8b00671
56597938 3940 None 4 Human Functional pEC50 = 8.5 8.5 204 2
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 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7651 3940 None 4 Human Functional pEC50 = 8.5 8.5 204 2
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 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165126 3940 None 4 Human Functional pEC50 = 8.5 8.5 204 2
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 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
56593482 3941 None 6 Human Functional pEC50 = 8.5 8.5 602 2
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 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7650 3941 None 6 Human Functional pEC50 = 8.5 8.5 602 2
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 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165119 3941 None 6 Human Functional pEC50 = 8.5 8.5 602 2
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 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
25093832 155970 None 0 Human Functional pEC50 = 8.5 8.5 2 2
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 155970 None 0 Human Functional pEC50 = 8.5 8.5 2 2
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
164628178 186453 None 0 Human Functional pEC50 = 8.5 8.5 10 3
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186453 None 0 Human Functional pEC50 = 8.5 8.5 10 3
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
162664513 182180 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 255 7 0 1 3.7 C#CCCCCN(CCC)C1Cc2ccccc2C1 10.1016/j.ejmech.2020.113151
CHEMBL4781480 182180 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 255 7 0 1 3.7 C#CCCCCN(CCC)C1Cc2ccccc2C1 10.1016/j.ejmech.2020.113151
25093832 155970 None 0 Human Functional pEC50 = 8.5 8.5 2 2
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 155970 None 0 Human Functional pEC50 = 8.5 8.5 2 2
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
71722297 102527 None 0 Human Functional pEC50 = 8.5 8.5 34 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397382 102527 None 0 Human Functional pEC50 = 8.5 8.5 34 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040156 102527 None 0 Human Functional pEC50 = 8.5 8.5 34 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
164628178 186453 None 0 Human Functional pEC50 = 8.5 8.5 10 3
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186453 None 0 Human Functional pEC50 = 8.5 8.5 10 3
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 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164620035 185746 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 398 9 2 4 3.9 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4864436 185746 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 398 9 2 4 3.9 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
164620035 185746 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 398 9 2 4 3.9 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4864436 185746 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 398 9 2 4 3.9 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
44554987 104323 None 0 Human Functional pEC50 = 8.5 8.5 114 2
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 361 4 1 5 2.9 CCCN1C[C@@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099239 104323 None 0 Human Functional pEC50 = 8.5 8.5 114 2
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 361 4 1 5 2.9 CCCN1C[C@@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
164623991 185643 None 0 Human Functional pEC50 = 8.4 8.4 2 3
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
CHEMBL4862890 185643 None 0 Human Functional pEC50 = 8.4 8.4 2 3
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
164623991 185643 None 0 Human Functional pEC50 = 8.4 8.4 2 3
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
CHEMBL4862890 185643 None 0 Human Functional pEC50 = 8.4 8.4 2 3
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
172465305 196931 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 387 8 2 4 4.1 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5435054 196931 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 387 8 2 4 4.1 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)oc12 10.1021/acs.jmedchem.3c00098
172465305 196931 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 387 8 2 4 4.1 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5435054 196931 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 387 8 2 4 4.1 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)oc12 10.1021/acs.jmedchem.3c00098
101885475 121601 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 745 29 4 6 6.8 CCCN(CCCNC(=O)CCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585370 121601 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 745 29 4 6 6.8 CCCN(CCCNC(=O)CCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
101885475 121601 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 745 29 4 6 6.8 CCCN(CCCNC(=O)CCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585370 121601 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 745 29 4 6 6.8 CCCN(CCCNC(=O)CCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
172439032 195309 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5400528 195309 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
172439032 195309 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5400528 195309 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 412 4 0 3 3.9 CN(C)C(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
228 445 None 20 Rat Functional pEC50 = 7.5 7.5 -4 20
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
33 445 None 20 Rat Functional pEC50 = 7.5 7.5 -4 20
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
6005 445 None 20 Rat Functional pEC50 = 7.5 7.5 -4 20
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
6005.0 445 None 20 Rat Functional pEC50 = 7.5 7.5 -4 20
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
CHEMBL53 445 None 20 Rat Functional pEC50 = 7.5 7.5 -4 20
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
DB00714 445 None 20 Rat Functional pEC50 = 7.5 7.5 -4 20
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
56597092 81996 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 433 6 1 4 3.9 O=C1NCCc2ccc(OCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc21 nan
CHEMBL2165117 81996 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 433 6 1 4 3.9 O=C1NCCc2ccc(OCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc21 nan
172440653 195350 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 9 2 5 4.3 CCOc1cccc2cc(CNCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5401818 195350 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 9 2 5 4.3 CCOc1cccc2cc(CNCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
172440653 195350 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 9 2 5 4.3 CCOc1cccc2cc(CNCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5401818 195350 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 9 2 5 4.3 CCOc1cccc2cc(CNCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
137644833 158231 None 0 Human Functional pEC50 = 5.5 5.5 -95 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4087187 158231 None 0 Human Functional pEC50 = 5.5 5.5 -95 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
2402 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
5095 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
5095.0 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
7295 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
CHEMBL589 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
DB00268 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
172444683 194946 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 419 7 0 6 4.8 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)oc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5393856 194946 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 419 7 0 6 4.8 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)oc2c1)CC3 10.1021/acs.jmedchem.3c00098
172456605 196210 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4c(C)noc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5418890 196210 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4c(C)noc4c3)oc12 10.1021/acs.jmedchem.3c00098
2402 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
5095 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
5095.0 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
7295 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
CHEMBL589 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
DB00268 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
2402 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
5095 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
5095.0 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
7295 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
CHEMBL589 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
DB00268 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
2402 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
5095 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
5095.0 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
7295 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
CHEMBL589 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
DB00268 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm501254d
2402 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
5095 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
5095.0 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
7295 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
CHEMBL589 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
DB00268 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
172444683 194946 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 419 7 0 6 4.8 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)oc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5393856 194946 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 419 7 0 6 4.8 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)oc2c1)CC3 10.1021/acs.jmedchem.3c00098
66633791 150955 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 421 8 1 5 3.9 COc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
CHEMBL3957278 150955 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 421 8 1 5 3.9 COc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
44567597 169567 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
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 592 5 4 8 5.5 CN1CCc2cc(OCCOc3cc4c5c(c3)-c3c(ccc(O)c3O)C[C@H]5N(C)CC4)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
CHEMBL442926 169567 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
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 592 5 4 8 5.5 CN1CCc2cc(OCCOc3cc4c5c(c3)-c3c(ccc(O)c3O)C[C@H]5N(C)CC4)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
172444683 194946 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 419 7 0 6 4.8 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)oc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5393856 194946 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 419 7 0 6 4.8 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)oc2c1)CC3 10.1021/acs.jmedchem.3c00098
118726007 120747 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394262 120747 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3547017 120747 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
172444683 194946 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 419 7 0 6 4.8 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)oc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5393856 194946 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 419 7 0 6 4.8 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)oc2c1)CC3 10.1021/acs.jmedchem.3c00098
118726007 120747 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394262 120747 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3547017 120747 None 0 Human Functional pEC50 = 6.5 6.5 -2 2
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 774 18 4 17 4.1 CCCN(CCCNc1nc(Oc2ccc(CCNc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc(N2CCOCC2)n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
44438218 93502 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 338 3 1 1 5.4 CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246020 93502 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 338 3 1 1 5.4 CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
44567595 175381 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
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 327 3 3 5 2.2 CN1CCc2cc(OCCO)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
CHEMBL457275 175381 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
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 327 3 3 5 2.2 CN1CCc2cc(OCCO)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
66559506 82008 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 481 5 1 4 6.0 O=C1CCc2ccc(Oc3cccc(CN4CCN(c5cccc(Cl)c5Cl)CC4)c3)cc2N1 10.1021/jm300603y
CHEMBL2165131 82008 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 481 5 1 4 6.0 O=C1CCc2ccc(Oc3cccc(CN4CCN(c5cccc(Cl)c5Cl)CC4)c3)cc2N1 10.1021/jm300603y
11983282 139030 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
Intrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 139030 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
Intrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
3949 3706 None 25 Human Functional pEC50 = 7.5 7.5 -4 3
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 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/acs.jmedchem.6b01875
9818479 3706 None 25 Human Functional pEC50 = 7.5 7.5 -4 3
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 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/acs.jmedchem.6b01875
CHEMBL419792 3706 None 25 Human Functional pEC50 = 7.5 7.5 -4 3
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 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/acs.jmedchem.6b01875
DB06477 3706 None 25 Human Functional pEC50 = 7.5 7.5 -4 3
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 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/acs.jmedchem.6b01875
164623044 186274 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 392 10 2 4 4.1 COc1ccccc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4872548 186274 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 392 10 2 4 4.1 COc1ccccc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164623044 186274 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 392 10 2 4 4.1 COc1ccccc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4872548 186274 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 392 10 2 4 4.1 COc1ccccc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
127037826 137007 None 0 Human Functional pEC50 = 7.5 7.5 -8 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2c(Cl)ccc3[nH]ccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3740286 137007 None 0 Human Functional pEC50 = 7.5 7.5 -8 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2c(Cl)ccc3[nH]ccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742427 137007 None 0 Human Functional pEC50 = 7.5 7.5 -8 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2c(Cl)ccc3[nH]ccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
46176231 63986 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at dopamine D2 receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 30 minsAgonist activity at dopamine D2 receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins
ChEMBL 467 8 0 5 6.8 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)CCCCC2CCSS2)c1-3 10.1021/jm200347t
CHEMBL1806874 63986 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at dopamine D2 receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 30 minsAgonist activity at dopamine D2 receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins
ChEMBL 467 8 0 5 6.8 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)CCCCC2CCSS2)c1-3 10.1021/jm200347t
162673328 183223 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 480 12 1 3 5.8 C#CCOc1ccc(-c2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2)cc1 10.1016/j.ejmech.2020.113151
CHEMBL4794870 183223 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 480 12 1 3 5.8 C#CCOc1ccc(-c2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2)cc1 10.1016/j.ejmech.2020.113151
164608815 184560 None 0 Human Functional pEC50 = 5.5 5.5 -46 3
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 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4846638 184560 None 0 Human Functional pEC50 = 5.5 5.5 -46 3
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 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
44555138 104320 None 0 Human Functional pEC50 = 7.5 7.5 117 2
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 403 5 1 5 3.9 CCCN1C[C@@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099233 104320 None 0 Human Functional pEC50 = 7.5 7.5 117 2
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 403 5 1 5 3.9 CCCN1C[C@@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
72735990 103803 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 358 4 1 3 4.5 CC(C)(C)OC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL3088209 103803 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 358 4 1 3 4.5 CC(C)(C)OC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
24866612 189730 None 0 Human Functional pEC50 = 7.5 7.5 -72 2
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 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL514885 189730 None 0 Human Functional pEC50 = 7.5 7.5 -72 2
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 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
72735990 103803 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 358 4 1 3 4.5 CC(C)(C)OC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL3088209 103803 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 358 4 1 3 4.5 CC(C)(C)OC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
2402 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/acs.jmedchem.7b00363
5095 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/acs.jmedchem.7b00363
5095.0 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/acs.jmedchem.7b00363
7295 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/acs.jmedchem.7b00363
CHEMBL589 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/acs.jmedchem.7b00363
DB00268 3370 None 38 Human Functional pEC50 = 6.5 6.5 -7 17
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 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/acs.jmedchem.7b00363
2 3261 None 19 Human Functional pEC50 = 6.5 6.5 -10 7
Intrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS 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 3261 None 19 Human Functional pEC50 = 6.5 6.5 -10 7
Intrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS 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 3261 None 19 Human Functional pEC50 = 6.5 6.5 -10 7
Intrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
71110290 147248 None 0 Human Functional pEC50 = 5.5 5.5 -8 2
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 355 4 0 5 3.4 COc1cc2c(cc1OC)C1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3927835 147248 None 0 Human Functional pEC50 = 5.5 5.5 -8 2
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 355 4 0 5 3.4 COc1cc2c(cc1OC)C1Cc3c(OC)ccc(OC)c3CN1CC2 nan
137653034 158816 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 487 11 2 5 4.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)[C@@H]1Cc2cccc3c2n(c(=O)n3CCC)C1 10.1021/acs.jmedchem.6b01875
CHEMBL4093477 158816 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 487 11 2 5 4.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)[C@@H]1Cc2cccc3c2n(c(=O)n3CCC)C1 10.1021/acs.jmedchem.6b01875
164618742 185695 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 414 9 2 3 5.3 O=C1CCc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2N1 10.1021/acs.jmedchem.1c01327
CHEMBL4863636 185695 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 414 9 2 3 5.3 O=C1CCc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2N1 10.1021/acs.jmedchem.1c01327
25072635 111846 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
CHEMBL3287399 111846 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
164609729 185204 None 0 Human Functional pEC50 = 6.5 6.5 -21 3
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 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856059 185204 None 0 Human Functional pEC50 = 6.5 6.5 -21 3
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 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
164618742 185695 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 414 9 2 3 5.3 O=C1CCc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2N1 10.1021/acs.jmedchem.1c01327
CHEMBL4863636 185695 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 414 9 2 3 5.3 O=C1CCc2ccc(OCCCCNCC3CC3c3cccc4ccccc34)cc2N1 10.1021/acs.jmedchem.1c01327
168273745 192917 None 0 Human Functional pEC50 = 5.5 5.5 -218 3
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 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5178472 192917 None 0 Human Functional pEC50 = 5.5 5.5 -218 3
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 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221451 192917 None 0 Human Functional pEC50 = 5.5 5.5 -218 3
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 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
44438197 153361 None 1 Human Functional pEC50 = 7.5 7.5 6 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL397770 153361 None 1 Human Functional pEC50 = 7.5 7.5 6 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
164623892 186226 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 432 9 2 3 5.4 O=C1CCc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2N1 10.1021/acs.jmedchem.1c01327
CHEMBL4871833 186226 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 432 9 2 3 5.4 O=C1CCc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2N1 10.1021/acs.jmedchem.1c01327
44438228 93609 None 0 Human Functional pEC50 = 7.5 7.5 7 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246438 93609 None 0 Human Functional pEC50 = 7.5 7.5 7 2
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
164623892 186226 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 432 9 2 3 5.4 O=C1CCc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2N1 10.1021/acs.jmedchem.1c01327
CHEMBL4871833 186226 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 432 9 2 3 5.4 O=C1CCc2ccc(OCCCCNCC3CC3c3cccc(Cl)c3Cl)cc2N1 10.1021/acs.jmedchem.1c01327
25072635 111846 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
CHEMBL3287399 111846 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
681 1465 None 47 Human Functional pEC50 = 5.5 5.5 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assayAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
681.0 1465 None 47 Human Functional pEC50 = 5.5 5.5 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assayAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
940 1465 None 47 Human Functional pEC50 = 5.5 5.5 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assayAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
947 1465 None 47 Human Functional pEC50 = 5.5 5.5 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assayAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
CHEMBL59 1465 None 47 Human Functional pEC50 = 5.5 5.5 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assayAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
DB00988 1465 None 47 Human Functional pEC50 = 5.5 5.5 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assayAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
56598071 82016 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 435 6 0 5 5.6 Clc1cccc(N2CCCN(CCCOc3ccc4scnc4c3)CC2)c1Cl nan
CHEMBL2165140 82016 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 435 6 0 5 5.6 Clc1cccc(N2CCCN(CCCOc3ccc4scnc4c3)CC2)c1Cl nan
3949 3706 None 25 Rat Functional pEC50 = 7.5 7.5 4 3
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret 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 3706 None 25 Rat Functional pEC50 = 7.5 7.5 4 3
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret 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 3706 None 25 Rat Functional pEC50 = 7.5 7.5 4 3
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret 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 3706 None 25 Rat Functional pEC50 = 7.5 7.5 4 3
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret 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
164615867 185548 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4861553 185548 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
164615867 185548 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4861553 185548 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 4.8 CSc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
172456605 196210 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4c(C)noc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5418890 196210 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4c(C)noc4c3)oc12 10.1021/acs.jmedchem.3c00098
172460089 196332 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 383 10 1 6 4.5 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)OCO4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5421574 196332 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 383 10 1 6 4.5 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)OCO4)oc12 10.1021/acs.jmedchem.3c00098
122189390 123312 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613876 123312 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
146025821 169774 None 0 Human Functional pEC50 = 5.5 5.5 -100 2
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 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 169774 None 0 Human Functional pEC50 = 5.5 5.5 -100 2
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 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
172456605 196210 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4c(C)noc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5418890 196210 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 10 1 6 5.2 CCOc1cccc2cc(CNCCCCOc3ccc4c(C)noc4c3)oc12 10.1021/acs.jmedchem.3c00098
172460089 196332 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 383 10 1 6 4.5 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)OCO4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5421574 196332 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 383 10 1 6 4.5 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)OCO4)oc12 10.1021/acs.jmedchem.3c00098
44320092 161981 None 0 Rat Functional pEC50 = 6.5 6.5 -346 2
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 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL415080 161981 None 0 Rat Functional pEC50 = 6.5 6.5 -346 2
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 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
146025821 169774 None 0 Human Functional pEC50 = 5.5 5.5 -100 2
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 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 169774 None 0 Human Functional pEC50 = 5.5 5.5 -100 2
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 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
44320129 167997 None 0 Rat Functional pEC50 = 6.5 6.5 -56 2
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 251 4 3 4 2.2 CCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL431220 167997 None 0 Rat Functional pEC50 = 6.5 6.5 -56 2
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 251 4 3 4 2.2 CCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
681 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
681.0 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
940 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
947 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
CHEMBL59 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
DB00988 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
76329028 105752 None 0 Human Functional pEC50 = 7.4 7.4 -10 2
Partial agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingPartial agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 505 9 1 7 4.8 CCCN(CCN1CCN(c2ccc(-c3cccc(OC)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm401883v
CHEMBL3125987 105752 None 0 Human Functional pEC50 = 7.4 7.4 -10 2
Partial agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingPartial agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 505 9 1 7 4.8 CCCN(CCN1CCN(c2ccc(-c3cccc(OC)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm401883v
66559782 82003 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 446 7 1 3 5.9 O=C1CCc2ccc(OCCCCN3CCC(c4cccc(Cl)c4Cl)CC3)cc2N1 10.1021/jm300603y
CHEMBL2165125 82003 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 446 7 1 3 5.9 O=C1CCc2ccc(OCCCCN3CCC(c4cccc(Cl)c4Cl)CC3)cc2N1 10.1021/jm300603y
11849820 77983 None 0 Human Functional pEC50 = 6.4 6.4 -10 2
Agonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assayAgonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL209645 77983 None 0 Human Functional pEC50 = 6.4 6.4 -10 2
Agonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assayAgonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
118726011 117275 None 0 Human Functional pEC50 = 7.4 7.4 46 2
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 517 14 3 10 3.8 CCCN(CCCCCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394266 117275 None 0 Human Functional pEC50 = 7.4 7.4 46 2
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 517 14 3 10 3.8 CCCN(CCCCCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
155563589 175422 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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 401 9 2 6 4.5 CCCN(CCC/C=C/c1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4573578 175422 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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 401 9 2 6 4.5 CCCN(CCC/C=C/c1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
52937876 61194 None 0 Human Functional pEC50 = 6.4 6.4 -489 2
Agonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphai2 assessed as incorporation of [35S]GTPgammaS into Galphai2 after 30 mins by scintillation countingAgonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphai2 assessed as incorporation of [35S]GTPgammaS into Galphai2 after 30 mins by scintillation counting
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765633 61194 None 0 Human Functional pEC50 = 6.4 6.4 -489 2
Agonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphai2 assessed as incorporation of [35S]GTPgammaS into Galphai2 after 30 mins by scintillation countingAgonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphai2 assessed as incorporation of [35S]GTPgammaS into Galphai2 after 30 mins by scintillation counting
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
56599145 82010 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 447 7 1 4 4.3 O=C1NCCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc21 nan
CHEMBL2165133 82010 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 447 7 1 4 4.3 O=C1NCCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc21 nan
172447344 195758 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 7 0 6 5.3 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2scnc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5410217 195758 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 7 0 6 5.3 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2scnc2c1)CC3 10.1021/acs.jmedchem.3c00098
172447344 195758 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 7 0 6 5.3 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2scnc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5410217 195758 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 7 0 6 5.3 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2scnc2c1)CC3 10.1021/acs.jmedchem.3c00098
681 1465 None 47 Human Functional pEC50 = 6.4 6.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
681.0 1465 None 47 Human Functional pEC50 = 6.4 6.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
940 1465 None 47 Human Functional pEC50 = 6.4 6.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
947 1465 None 47 Human Functional pEC50 = 6.4 6.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.4 6.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
DB00988 1465 None 47 Human Functional pEC50 = 6.4 6.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.08.021
5311189 207299 None 9 Human Functional pEC50 = 6.4 6.4 -16 4
Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 200 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 200 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1021/acs.jmedchem.5b01031
CHEMBL7549 207299 None 9 Human Functional pEC50 = 6.4 6.4 -16 4
Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 200 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 200 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1021/acs.jmedchem.5b01031
172449681 195826 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 450 12 1 5 5.8 CCCN(CCCCOc1ccc2c(c1)NC(=O)CC2)Cc1cc2cccc(OCC)c2o1 10.1021/acs.jmedchem.3c00098
CHEMBL5411545 195826 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 450 12 1 5 5.8 CCCN(CCCCOc1ccc2c(c1)NC(=O)CC2)Cc1cc2cccc(OCC)c2o1 10.1021/acs.jmedchem.3c00098
118726011 117275 None 0 Human Functional pEC50 = 7.4 7.4 46 2
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 517 14 3 10 3.8 CCCN(CCCCCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394266 117275 None 0 Human Functional pEC50 = 7.4 7.4 46 2
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 517 14 3 10 3.8 CCCN(CCCCCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
242 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
34 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
60795 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
60795.0 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
DB01238 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2015.07.050
242 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795.0 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
46917637 68354 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayPartial agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916548 68354 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayPartial agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
172449681 195826 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 450 12 1 5 5.8 CCCN(CCCCOc1ccc2c(c1)NC(=O)CC2)Cc1cc2cccc(OCC)c2o1 10.1021/acs.jmedchem.3c00098
CHEMBL5411545 195826 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 450 12 1 5 5.8 CCCN(CCCCOc1ccc2c(c1)NC(=O)CC2)Cc1cc2cccc(OCC)c2o1 10.1021/acs.jmedchem.3c00098
122177643 121275 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Intrinsic activity at human dopamine D2L 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 D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577344 121275 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Intrinsic activity at human dopamine D2L 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 D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
53328903 66479 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 353 0 2 5 3.5 CN1CCc2c3c(cc4c2[C@H]1Cc1ccc(O)c(O)c1-4)SCCC3=O 10.1016/j.ejmech.2011.04.028
CHEMBL1802237 66479 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 353 0 2 5 3.5 CN1CCc2c3c(cc4c2[C@H]1Cc1ccc(O)c(O)c1-4)SCCC3=O 10.1016/j.ejmech.2011.04.028
CHEMBL1852107 66479 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
ChEMBL 353 0 2 5 3.5 CN1CCc2c3c(cc4c2[C@H]1Cc1ccc(O)c(O)c1-4)SCCC3=O 10.1016/j.ejmech.2011.04.028
172445349 195094 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 9 2 5 4.7 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
CHEMBL5396612 195094 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 9 2 5 4.7 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
118726009 117273 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 447 9 3 10 1.8 CN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394264 117273 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 447 9 3 10 1.8 CN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
118726009 117273 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 447 9 3 10 1.8 CN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394264 117273 None 0 Human Functional pEC50 = 6.4 6.4 2 2
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 447 9 3 10 1.8 CN(CCCNc1nc(N)n2nc(-c3ccco3)nc2n1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
172445349 195094 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 9 2 5 4.7 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
CHEMBL5396612 195094 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 9 2 5 4.7 COc1cccc2cc(CNCCCCOc3ccc4ccc(=O)[nH]c4c3)sc12 10.1021/acs.jmedchem.3c00098
242 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795.0 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 470 None 70 Human Functional pEC50 = 7.4 7.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
114876 12797 None 1 Human Functional pEC50 = 7.4 7.4 -7 6
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm301258w
CHEMBL1188090 12797 None 1 Human Functional pEC50 = 7.4 7.4 -7 6
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm301258w
CHEMBL545783 12797 None 1 Human Functional pEC50 = 7.4 7.4 -7 6
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm301258w
127038171 137010 None 0 Human Functional pEC50 = 7.4 7.4 -46 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742140 137010 None 0 Human Functional pEC50 = 7.4 7.4 -46 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742430 137010 None 0 Human Functional pEC50 = 7.4 7.4 -46 2
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
164622475 186217 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 390 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4871762 186217 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 390 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
2 3261 None 19 Human Functional pEC50 = 7.4 7.4 -10 7
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
54562 3261 None 19 Human Functional pEC50 = 7.4 7.4 -10 7
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
CHEMBL240773 3261 None 19 Human Functional pEC50 = 7.4 7.4 -10 7
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
11957566 184 None 17 Human Functional pEC50 = 7.4 7.4 -56 4
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity 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)cc(cc2)O)CCC 10.1021/jm701524h
1219 184 None 17 Human Functional pEC50 = 7.4 7.4 -56 4
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity 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)cc(cc2)O)CCC 10.1021/jm701524h
3296 184 None 17 Human Functional pEC50 = 7.4 7.4 -56 4
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity 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)cc(cc2)O)CCC 10.1021/jm701524h
950 184 None 17 Human Functional pEC50 = 7.4 7.4 -56 4
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity 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)cc(cc2)O)CCC 10.1021/jm701524h
CHEMBL285755 184 None 17 Human Functional pEC50 = 7.4 7.4 -56 4
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity 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)cc(cc2)O)CCC 10.1021/jm701524h
2 3261 None 19 Human Functional pEC50 = 7.4 7.4 -10 7
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
54562 3261 None 19 Human Functional pEC50 = 7.4 7.4 -10 7
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
CHEMBL240773 3261 None 19 Human Functional pEC50 = 7.4 7.4 -10 7
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.2c01624
90466573 158628 None 0 Human Functional pEC50 = 7.4 7.4 -16 2
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 526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4091498 158628 None 0 Human Functional pEC50 = 7.4 7.4 -16 2
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 526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
14809027 107085 None 0 Rat Functional pEC50 = 5.4 5.4 -1862 3
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]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315468 107085 None 0 Rat Functional pEC50 = 5.4 5.4 -1862 3
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]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
122324 205 None 17 Rat Functional pEC50 = 5.4 5.4 -3235 4
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 205 None 17 Rat Functional pEC50 = 5.4 5.4 -3235 4
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 205 None 17 Rat Functional pEC50 = 5.4 5.4 -3235 4
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
127037828 137009 None 0 Human Functional pEC50 = 5.4 5.4 -30 2
Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 300 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 300 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3740778 137009 None 0 Human Functional pEC50 = 5.4 5.4 -30 2
Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 300 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 300 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742429 137009 None 0 Human Functional pEC50 = 5.4 5.4 -30 2
Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 300 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 300 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
137657115 159849 None 0 Human Functional pEC50 = 6.4 6.4 -11 2
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(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4105030 159849 None 0 Human Functional pEC50 = 6.4 6.4 -11 2
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(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
66559507 82009 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 481 5 1 4 6.0 O=C1CCc2ccc(Oc3ccc(CN4CCN(c5cccc(Cl)c5Cl)CC4)cc3)cc2N1 nan
CHEMBL2165132 82009 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 481 5 1 4 6.0 O=C1CCc2ccc(Oc3ccc(CN4CCN(c5cccc(Cl)c5Cl)CC4)cc3)cc2N1 nan
242 470 None 70 Human Functional pEC50 = 8.4 8.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
34 470 None 70 Human Functional pEC50 = 8.4 8.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
60795 470 None 70 Human Functional pEC50 = 8.4 8.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
60795.0 470 None 70 Human Functional pEC50 = 8.4 8.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
CHEMBL1112 470 None 70 Human Functional pEC50 = 8.4 8.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
DB01238 470 None 70 Human Functional pEC50 = 8.4 8.4 -5 33
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 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
44554470 106325 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 219 0 1 3 1.2 CN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099224 106325 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 219 0 1 3 1.2 CN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139012 106325 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 219 0 1 3 1.2 CN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
228 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
33 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
6005 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
6005.0 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
CHEMBL53 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
DB00714 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
228 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
33 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
6005 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
6005.0 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
CHEMBL53 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
DB00714 445 None 20 Human Functional pEC50 = 8.4 8.4 -3 20
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
56598073 148190 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 9 1 6 3.7 CCOc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
CHEMBL3935170 148190 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 9 1 6 3.7 CCOc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
122177645 121277 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577346 121277 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 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 Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
56599145 82010 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 447 7 1 4 4.3 O=C1NCCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc21 10.1021/jm300603y
CHEMBL2165133 82010 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 447 7 1 4 4.3 O=C1NCCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc21 10.1021/jm300603y
164621351 185786 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 426 10 1 4 4.6 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4865118 185786 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 426 10 1 4 4.6 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
25072633 159314 None 0 Human Functional pEC50 = 8.4 8.4 7 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 159314 None 0 Human Functional pEC50 = 8.4 8.4 7 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
164621351 185786 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 426 10 1 4 4.6 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4865118 185786 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 426 10 1 4 4.6 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.1c01327
164619170 185707 None 0 Human Functional pEC50 = 8.4 8.4 10 3
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185707 None 0 Human Functional pEC50 = 8.4 8.4 10 3
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
171492446 196607 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
CHEMBL5427695 196607 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
172454187 195871 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 384 9 2 4 4.4 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)C4CC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5412359 195871 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 384 9 2 4 4.4 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)C4CC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
172454187 195871 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 384 9 2 4 4.4 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)C4CC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5412359 195871 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 384 9 2 4 4.4 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)C4CC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
25072633 159314 None 0 Human Functional pEC50 = 8.4 8.4 7 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 159314 None 0 Human Functional pEC50 = 8.4 8.4 7 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
171492446 196607 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
CHEMBL5427695 196607 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 406 6 1 4 3.2 COc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)N(C)C)CC3)CC2)c1F 10.1021/acs.jmedchem.2c01624
164619170 185707 None 0 Human Functional pEC50 = 8.4 8.4 10 3
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185707 None 0 Human Functional pEC50 = 8.4 8.4 10 3
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
161553599 184990 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 414 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4852808 184990 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 414 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
161553599 184990 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 414 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4852808 184990 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 414 9 2 4 4.4 COc1ccc(Cl)cc1C1CC1CNCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
164622576 185608 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 412 10 2 4 4.3 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862439 185608 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 412 10 2 4 4.3 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
164628423 186379 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4874021 186379 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
56599011 146516 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 449 9 1 5 4.7 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
CHEMBL3921903 146516 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 449 9 1 5 4.7 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
56598075 150382 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 451 9 1 5 4.7 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
CHEMBL3952761 150382 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 451 9 1 5 4.7 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
164628423 186379 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4874021 186379 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164622576 185608 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 412 10 2 4 4.3 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862439 185608 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 412 10 2 4 4.3 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
172458432 196201 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 407 10 1 6 4.9 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)oc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5418748 196201 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 407 10 1 6 4.9 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)oc4c3)oc12 10.1021/acs.jmedchem.3c00098
172458432 196201 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 407 10 1 6 4.9 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)oc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5418748 196201 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 407 10 1 6 4.9 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)oc4c3)oc12 10.1021/acs.jmedchem.3c00098
56598878 142710 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 9 1 5 4.3 CCOc1ccccc1N1CCCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
CHEMBL3891542 142710 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 9 1 5 4.3 CCOc1ccccc1N1CCCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
133633 2241 None 40 Human Functional pEC50 = 8.4 8.4 20 4
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
177 2241 None 40 Human Functional pEC50 = 8.4 8.4 20 4
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
CHEMBL445102 2241 None 40 Human Functional pEC50 = 8.4 8.4 20 4
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
164158703 185320 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 426 10 2 4 4.7 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4857759 185320 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 426 10 2 4 4.7 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164158703 185320 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 426 10 2 4 4.7 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4857759 185320 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 426 10 2 4 4.7 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
183812 208197 None 20 Human Functional pEC50 = 8.4 8.4 -15 2
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assayAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assay
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2012.07.096
CHEMBL82663 208197 None 20 Human Functional pEC50 = 8.4 8.4 -15 2
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assayAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assay
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2012.07.096
53361666 190730 None 0 Human Functional pEC50 = 8.4 8.4 -2 2
Agonist activity at human D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting methodAgonist activity at human D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting method
ChEMBL 466 7 2 8 3.4 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
CHEMBL5181007 190730 None 0 Human Functional pEC50 = 8.4 8.4 -2 2
Agonist activity at human D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting methodAgonist activity at human D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting method
ChEMBL 466 7 2 8 3.4 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
45140377 203115 None 0 Human Functional pEC50 = 8.4 8.4 -2 2
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)C1CCc2c(O)cccc2C1 10.1021/jm901618d
CHEMBL599636 203115 None 0 Human Functional pEC50 = 8.4 8.4 -2 2
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)C1CCc2c(O)cccc2C1 10.1021/jm901618d
56598072 152844 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 423 8 1 5 4.0 COc1ccccc1N1CCCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
CHEMBL3973357 152844 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 423 8 1 5 4.0 COc1ccccc1N1CCCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
66633659 153422 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 452 9 1 6 4.1 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
CHEMBL3978288 153422 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 452 9 1 6 4.1 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
164619170 185707 None 0 Human Functional pEC50 = 8.3 8.3 10 3
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185707 None 0 Human Functional pEC50 = 8.3 8.3 10 3
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164619170 185707 None 0 Human Functional pEC50 = 8.3 8.3 10 3
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185707 None 0 Human Functional pEC50 = 8.3 8.3 10 3
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 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
66633584 149296 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 9 1 5 4.3 CCOc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
CHEMBL3944009 149296 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 9 1 5 4.3 CCOc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
137651936 157484 None 0 Human Functional pEC50 = 8.3 8.3 -5 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 157484 None 0 Human Functional pEC50 = 8.3 8.3 -5 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137651936 157484 None 0 Human Functional pEC50 = 8.3 8.3 -5 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 157484 None 0 Human Functional pEC50 = 8.3 8.3 -5 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
15045457 25923 None 0 Human Functional pEC50 = 8.3 8.3 91 2
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 392 6 1 4 3.6 O=C(N[C@H]1CC[C@H](CCN2CCN(c3ccccn3)CC2)CC1)c1ccccc1 10.1021/jm00050a022
CHEMBL135387 25923 None 0 Human Functional pEC50 = 8.3 8.3 91 2
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 392 6 1 4 3.6 O=C(N[C@H]1CC[C@H](CCN2CCN(c3ccccn3)CC2)CC1)c1ccccc1 10.1021/jm00050a022
681 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assayAgonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2019.07.050
681.0 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assayAgonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2019.07.050
940 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assayAgonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2019.07.050
947 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assayAgonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2019.07.050
CHEMBL59 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assayAgonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2019.07.050
DB00988 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assayAgonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2019.07.050
45269964 13626 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 309 2 2 3 3.9 CCCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1194295 13626 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 309 2 2 3 3.9 CCCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL550180 13626 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 309 2 2 3 3.9 CCCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
137657115 159849 None 0 Human Functional pEC50 = 6.4 6.4 -11 2
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(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4105030 159849 None 0 Human Functional pEC50 = 6.4 6.4 -11 2
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(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
71733932 91086 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2397389 91086 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
71109989 153864 None 0 Human Functional pEC50 = 5.4 5.4 -26 2
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 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3982119 153864 None 0 Human Functional pEC50 = 5.4 5.4 -26 2
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 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
164624917 185712 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 393 7 2 2 4.8 CN(C)C(=O)N[C@H]1CC[C@H](CCNCC2CC2c2cccc3ccccc23)CC1 10.1021/acs.jmedchem.1c01327
CHEMBL4863920 185712 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 393 7 2 2 4.8 CN(C)C(=O)N[C@H]1CC[C@H](CCNCC2CC2c2cccc3ccccc23)CC1 10.1021/acs.jmedchem.1c01327
164624917 185712 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 393 7 2 2 4.8 CN(C)C(=O)N[C@H]1CC[C@H](CCNCC2CC2c2cccc3ccccc23)CC1 10.1021/acs.jmedchem.1c01327
CHEMBL4863920 185712 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 393 7 2 2 4.8 CN(C)C(=O)N[C@H]1CC[C@H](CCNCC2CC2c2cccc3ccccc23)CC1 10.1021/acs.jmedchem.1c01327
11299620 97337 None 1 Human Functional pEC50 = 7.4 7.4 -64 2
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 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
CHEMBL269004 97337 None 1 Human Functional pEC50 = 7.4 7.4 -64 2
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 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
45273211 198083 None 0 Human Functional pEC50 = 7.4 7.4 -33 2
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 460 7 2 4 3.9 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2009.04.031
CHEMBL556269 198083 None 0 Human Functional pEC50 = 7.4 7.4 -33 2
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 460 7 2 4 3.9 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2009.04.031
128 149 None 8 Human Functional pEC50 = 7.4 7.4 -50 3
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 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1021/jm901184n
172267 149 None 8 Human Functional pEC50 = 7.4 7.4 -50 3
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 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1021/jm901184n
CHEMBL273273 149 None 8 Human Functional pEC50 = 7.4 7.4 -50 3
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 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1021/jm901184n
24936042 157681 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4080762 157681 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
122179563 121598 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 429 17 2 3 5.1 CCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585367 121598 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 429 17 2 3 5.1 CCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
122177642 121274 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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
CHEMBL3577343 121274 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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
164040127 185414 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 408 11 2 4 4.5 COc1ccccc1C1CC1CNCCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4859394 185414 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 408 11 2 4 4.5 COc1ccccc1C1CC1CNCCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
164040127 185414 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 408 11 2 4 4.5 COc1ccccc1C1CC1CNCCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4859394 185414 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 408 11 2 4 4.5 COc1ccccc1C1CC1CNCCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
24936042 157681 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4080762 157681 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
122179563 121598 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 429 17 2 3 5.1 CCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585367 121598 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 429 17 2 3 5.1 CCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
172471633 197192 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 422 10 1 5 5.0 CCOc1cccc2cc(CN(C)CCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5440936 197192 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 422 10 1 5 5.0 CCOc1cccc2cc(CN(C)CCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
171492376 195452 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 504 7 1 4 6.0 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)c4ccnc5ccccc45)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
CHEMBL5404054 195452 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 504 7 1 4 6.0 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)c4ccnc5ccccc45)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
171492376 195452 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 504 7 1 4 6.0 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)c4ccnc5ccccc45)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
CHEMBL5404054 195452 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 504 7 1 4 6.0 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)c4ccnc5ccccc45)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
172471633 197192 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 422 10 1 5 5.0 CCOc1cccc2cc(CN(C)CCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5440936 197192 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 422 10 1 5 5.0 CCOc1cccc2cc(CN(C)CCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
127037828 137009 None 0 Human Functional pEC50 = 6.4 6.4 -30 2
Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 50 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 50 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3740778 137009 None 0 Human Functional pEC50 = 6.4 6.4 -30 2
Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 50 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 50 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742429 137009 None 0 Human Functional pEC50 = 6.4 6.4 -30 2
Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 50 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 50 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
44320378 208521 None 0 Rat Functional pEC50 = 6.4 6.4 -63 2
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 277 3 3 4 2.6 NC[C@@H]1OC(CC2CCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85409 208521 None 0 Rat Functional pEC50 = 6.4 6.4 -63 2
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 277 3 3 4 2.6 NC[C@@H]1OC(CC2CCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
681 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
681.0 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
940 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
947 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
CHEMBL59 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
DB00988 1465 None 47 Human Functional pEC50 = 7.4 7.4 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
44567292 198213 None 0 Rat Functional pEC50 = 7.4 7.4 1 2
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 281 0 2 3 3.2 Cc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2009.04.047
CHEMBL507567 198213 None 0 Rat Functional pEC50 = 7.4 7.4 1 2
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 281 0 2 3 3.2 Cc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2009.04.047
CHEMBL557547 198213 None 0 Rat Functional pEC50 = 7.4 7.4 1 2
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 281 0 2 3 3.2 Cc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2009.04.047
90644226 111842 None 0 Human Functional pEC50 = 6.4 6.4 -7 2
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 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287395 111842 None 0 Human Functional pEC50 = 6.4 6.4 -7 2
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 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
122189391 123313 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613877 123313 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
57242 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1039/C4MD00066H
954 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1039/C4MD00066H
CHEMBL155731 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1039/C4MD00066H
57242 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
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 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1021/jm501254d
954 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
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 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1021/jm501254d
CHEMBL155731 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
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 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1021/jm501254d
172447622 195955 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 11 2 5 5.0 CCOc1cccc2cc(CNCCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5414152 195955 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 11 2 5 5.0 CCOc1cccc2cc(CNCCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
56833378 68355 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayAgonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916549 68355 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayAgonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
90644226 111842 None 0 Human Functional pEC50 = 6.4 6.4 -7 2
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 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287395 111842 None 0 Human Functional pEC50 = 6.4 6.4 -7 2
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 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
168292954 193106 None 0 Human Functional pEC50 = 5.4 5.4 -33 3
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 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5202592 193106 None 0 Human Functional pEC50 = 5.4 5.4 -33 3
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 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 193106 None 0 Human Functional pEC50 = 5.4 5.4 -33 3
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 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
85470564 156915 None 0 Human Functional pEC50 = 7.4 7.4 -37 2
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 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4071240 156915 None 0 Human Functional pEC50 = 7.4 7.4 -37 2
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 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
57242 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1039/C4MD00066H
954 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1039/C4MD00066H
CHEMBL155731 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1039/C4MD00066H
57242 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
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 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1021/jm501254d
954 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
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 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1021/jm501254d
CHEMBL155731 3259 None 18 Human Functional pEC50 = 7.4 7.4 -9 4
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 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1021/jm501254d
172449124 195574 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 422 11 2 5 5.1 CCOc1cccc2cc(CNCCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5406355 195574 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 422 11 2 5 5.1 CCOc1cccc2cc(CNCCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
172449124 195574 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 422 11 2 5 5.1 CCOc1cccc2cc(CNCCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5406355 195574 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 422 11 2 5 5.1 CCOc1cccc2cc(CNCCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
146025766 171701 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 357 6 1 2 4.0 CCN(CC)C(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4465281 171701 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 357 6 1 2 4.0 CCN(CC)C(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
56599146 144187 None 0 Human Functional pEC50 = 4.3 4.3 - 1
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 501 6 1 4 5.9 O=C1CCc2ccc(OCC3CCC(CN4CCN(c5cccc(Cl)c5Cl)CC4)CC3)cc2N1 nan
CHEMBL3903542 144187 None 0 Human Functional pEC50 = 4.3 4.3 - 1
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 501 6 1 4 5.9 O=C1CCc2ccc(OCC3CCC(CN4CCN(c5cccc(Cl)c5Cl)CC4)CC3)cc2N1 nan
681 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
681.0 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
940 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
947 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
DB00988 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
122179564 121604 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 375 12 3 4 1.8 CCCN(CCCNC(=O)CCC(=O)O)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585373 121604 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 375 12 3 4 1.8 CCCN(CCCNC(=O)CCC(=O)O)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
122179564 121604 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 375 12 3 4 1.8 CCCN(CCCNC(=O)CCC(=O)O)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585373 121604 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 375 12 3 4 1.8 CCCN(CCCNC(=O)CCC(=O)O)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
10084583 104834 None 3 Rat Functional pEC50 = 7.3 7.3 -9 3
Effective concentration required for agonistic activity against rat D2 short receptorEffective concentration required for agonistic activity against rat D2 short receptor
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 104834 None 3 Rat Functional pEC50 = 7.3 7.3 -9 3
Effective concentration required for agonistic activity against rat D2 short receptorEffective concentration required for agonistic activity against rat D2 short receptor
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
146025766 171701 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 357 6 1 2 4.0 CCN(CC)C(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4465281 171701 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 357 6 1 2 4.0 CCN(CC)C(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
172458432 196201 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 407 10 1 6 4.9 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)oc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5418748 196201 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 407 10 1 6 4.9 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)oc4c3)oc12 10.1021/acs.jmedchem.3c00098
172458432 196201 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 407 10 1 6 4.9 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)oc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5418748 196201 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 407 10 1 6 4.9 CCOc1cccc2cc(CNCCCCOc3ccc4ccc(=O)oc4c3)oc12 10.1021/acs.jmedchem.3c00098
137655735 159084 None 0 Human Functional pEC50 = 6.3 6.3 -12 2
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 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4096353 159084 None 0 Human Functional pEC50 = 6.3 6.3 -12 2
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 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
681 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
681.0 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
940 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
947 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
CHEMBL59 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
DB00988 1465 None 47 Human Functional pEC50 = 6.3 6.3 -19 15
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm5004039
122189392 123314 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613878 123314 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
118725995 117265 None 0 Human Functional pEC50 = 6.3 6.3 -13 2
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 708 19 4 13 4.0 CCCN(CCCNC(=O)CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394253 117265 None 0 Human Functional pEC50 = 6.3 6.3 -13 2
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 708 19 4 13 4.0 CCCN(CCCNC(=O)CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
164610211 185173 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 442 10 1 4 5.1 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4855583 185173 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 442 10 1 4 5.1 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
164624420 185596 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 394 10 2 4 4.1 COc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862301 185596 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 394 10 2 4 4.1 COc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
172460089 196332 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 383 10 1 6 4.5 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)OCO4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5421574 196332 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 383 10 1 6 4.5 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)OCO4)oc12 10.1021/acs.jmedchem.3c00098
45267373 14023 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
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 295 1 2 3 3.5 CCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1197201 14023 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
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 295 1 2 3 3.5 CCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL562460 14023 None 0 Rat Functional pEC50 = 6.3 6.3 - 1
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 295 1 2 3 3.5 CCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
118725995 117265 None 0 Human Functional pEC50 = 6.3 6.3 -13 2
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 708 19 4 13 4.0 CCCN(CCCNC(=O)CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394253 117265 None 0 Human Functional pEC50 = 6.3 6.3 -13 2
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 708 19 4 13 4.0 CCCN(CCCNC(=O)CCCC(=O)Oc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
172471633 197192 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 422 10 1 5 5.0 CCOc1cccc2cc(CN(C)CCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5440936 197192 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 422 10 1 5 5.0 CCOc1cccc2cc(CN(C)CCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
172471633 197192 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 422 10 1 5 5.0 CCOc1cccc2cc(CN(C)CCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5440936 197192 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 422 10 1 5 5.0 CCOc1cccc2cc(CN(C)CCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
71722295 102522 None 0 Human Functional pEC50 = 7.3 7.3 1 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397381 102522 None 0 Human Functional pEC50 = 7.3 7.3 1 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040115 102522 None 0 Human Functional pEC50 = 7.3 7.3 1 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
164624420 185596 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 394 10 2 4 4.1 COc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862301 185596 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 394 10 2 4 4.1 COc1ccccc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
172460089 196332 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 383 10 1 6 4.5 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)OCO4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5421574 196332 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 383 10 1 6 4.5 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)OCO4)oc12 10.1021/acs.jmedchem.3c00098
90467453 158935 None 0 Human Functional pEC50 = 7.3 7.3 -3 2
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 486 9 2 5 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4094794 158935 None 0 Human Functional pEC50 = 7.3 7.3 -3 2
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 486 9 2 5 4.5 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
15389743 184515 None 0 Rat Functional pEC50 = 7.3 7.3 -63 3
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 274 3 1 3 1.9 CCCN1CCO[C@@H]2c3cc(C(N)=O)ccc3CC[C@H]21 10.1007/s00044-004-0006-x
CHEMBL484599 184515 None 0 Rat Functional pEC50 = 7.3 7.3 -63 3
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 274 3 1 3 1.9 CCCN1CCO[C@@H]2c3cc(C(N)=O)ccc3CC[C@H]21 10.1007/s00044-004-0006-x
164610211 185173 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 442 10 1 4 5.1 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
CHEMBL4855583 185173 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 442 10 1 4 5.1 CCN(CCCOc1ccc2c(c1)NC(=O)CC2)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.1c01327
681 1465 None 47 Rat Functional pEC50 = 8.3 8.3 -288 15
Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
681.0 1465 None 47 Rat Functional pEC50 = 8.3 8.3 -288 15
Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
940 1465 None 47 Rat Functional pEC50 = 8.3 8.3 -288 15
Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
947 1465 None 47 Rat Functional pEC50 = 8.3 8.3 -288 15
Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
CHEMBL59 1465 None 47 Rat Functional pEC50 = 8.3 8.3 -288 15
Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
DB00988 1465 None 47 Rat Functional pEC50 = 8.3 8.3 -288 15
Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
10811378 54231 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 407 7 1 4 4.2 Cc1cccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c1C 10.1021/jm300603y
CHEMBL160744 54231 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 407 7 1 4 4.2 Cc1cccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c1C 10.1021/jm300603y
10763756 54441 None 2 Human Functional pEC50 = 8.3 8.3 - 1
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 404 7 1 5 3.4 N#Cc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL160921 54441 None 2 Human Functional pEC50 = 8.3 8.3 - 1
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 404 7 1 5 3.4 N#Cc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
119570 3159 None 58 Human Functional pEC50 = 8.3 8.3 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmc.2007.06.036
119570.0 3159 None 58 Human Functional pEC50 = 8.3 8.3 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmc.2007.06.036
2233 3159 None 58 Human Functional pEC50 = 8.3 8.3 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmc.2007.06.036
953 3159 None 58 Human Functional pEC50 = 8.3 8.3 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmc.2007.06.036
CHEMBL301265 3159 None 58 Human Functional pEC50 = 8.3 8.3 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmc.2007.06.036
DB00413 3159 None 58 Human Functional pEC50 = 8.3 8.3 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmc.2007.06.036
172468596 197053 None 0 Human Functional pEC50 = 8.3 8.3 3 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 436 7 2 4 3.9 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)NC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5437660 197053 None 0 Human Functional pEC50 = 8.3 8.3 3 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 436 7 2 4 3.9 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)NC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
146025777 173063 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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](CCN2CCc3cc(Cl)ccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4517517 173063 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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](CCN2CCc3cc(Cl)ccc3C2)CC1 10.1021/acs.jmedchem.9b00508
172457140 196444 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 10 2 5 4.7 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5424038 196444 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 10 2 5 4.7 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
172468596 197053 None 0 Human Functional pEC50 = 8.3 8.3 3 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 436 7 2 4 3.9 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)NC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5437660 197053 None 0 Human Functional pEC50 = 8.3 8.3 3 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 436 7 2 4 3.9 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)NC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
172457140 196444 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 10 2 5 4.7 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5424038 196444 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 408 10 2 5 4.7 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
164622576 185608 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 412 10 2 4 4.3 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862439 185608 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 412 10 2 4 4.3 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
2 3261 None 19 Human Functional pEC50 = 8.3 8.3 -10 7
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2020.113151
54562 3261 None 19 Human Functional pEC50 = 8.3 8.3 -10 7
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2020.113151
CHEMBL240773 3261 None 19 Human Functional pEC50 = 8.3 8.3 -10 7
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2020.113151
71722293 102530 None 0 Human Functional pEC50 = 8.3 8.3 4 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL2397380 102530 None 0 Human Functional pEC50 = 8.3 8.3 4 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL3040164 102530 None 0 Human Functional pEC50 = 8.3 8.3 4 2
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
172460539 196501 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 9 2 5 4.3 COc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5425434 196501 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 9 2 5 4.3 COc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
172465854 196539 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 392 9 2 5 4.2 CCOc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5426286 196539 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 392 9 2 5 4.2 CCOc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
172460539 196501 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 9 2 5 4.3 COc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5425434 196501 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 394 9 2 5 4.3 COc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
172465854 196539 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 392 9 2 5 4.2 CCOc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5426286 196539 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 392 9 2 5 4.2 CCOc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
172459790 196485 None 0 Human Functional pEC50 = 8.3 8.3 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5424897 196485 None 0 Human Functional pEC50 = 8.3 8.3 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
172459790 196485 None 0 Human Functional pEC50 = 8.3 8.3 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
CHEMBL5424897 196485 None 0 Human Functional pEC50 = 8.3 8.3 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 465 10 1 5 4.1 CCc1cc(Cl)c(OC)c(N2CCN(CC[C@H]3CC[C@H](NC(=O)CCOC)CC3)CC2)c1 10.1021/acs.jmedchem.2c01624
146025777 173063 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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](CCN2CCc3cc(Cl)ccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4517517 173063 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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](CCN2CCc3cc(Cl)ccc3C2)CC1 10.1021/acs.jmedchem.9b00508
145985295 165826 None 0 Human Functional pEC50 = 8.3 8.3 57 2
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 958 30 3 12 9.3 CCCN(CCc1ccc(NC(=O)CCc2cn(CCCCCCCCCCN(C)CCCCCNC(=O)COc3cncc(C#Cc4csc(C)n4)c3)nn2)cc1)C1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.8b00671
CHEMBL4246185 165826 None 0 Human Functional pEC50 = 8.3 8.3 57 2
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 958 30 3 12 9.3 CCCN(CCc1ccc(NC(=O)CCc2cn(CCCCCCCCCCN(C)CCCCCNC(=O)COc3cncc(C#Cc4csc(C)n4)c3)nn2)cc1)C1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.8b00671
66559587 81997 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 447 6 1 4 4.3 O=C1NCCc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc21 nan
CHEMBL2165118 81997 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 447 6 1 4 4.3 O=C1NCCc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc21 nan
5311346 206612 None 20 Rat Functional pEC50 = 8.2 8.2 -660 5
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 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL1256778 206612 None 20 Rat Functional pEC50 = 8.2 8.2 -660 5
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 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL70565 206612 None 20 Rat Functional pEC50 = 8.2 8.2 -660 5
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 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
9904074 110691 None 3 Rat Functional pEC50 = 8.2 8.2 - 1
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2cc3nc(N)sc3cc2C1 10.1021/jm000087z
CHEMBL325710 110691 None 3 Rat Functional pEC50 = 8.2 8.2 - 1
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2cc3nc(N)sc3cc2C1 10.1021/jm000087z
66559507 82009 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 481 5 1 4 6.0 O=C1CCc2ccc(Oc3ccc(CN4CCN(c5cccc(Cl)c5Cl)CC4)cc3)cc2N1 nan
CHEMBL2165132 82009 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 481 5 1 4 6.0 O=C1CCc2ccc(Oc3ccc(CN4CCN(c5cccc(Cl)c5Cl)CC4)cc3)cc2N1 nan
56597091 82011 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 418 7 1 4 4.9 Clc1cccc(N2CCN(CCCCOc3ccc4cn[nH]c4c3)CC2)c1Cl nan
CHEMBL2165134 82011 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 418 7 1 4 4.9 Clc1cccc(N2CCN(CCCCOc3ccc4cn[nH]c4c3)CC2)c1Cl nan
164622576 185608 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 412 10 2 4 4.3 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862439 185608 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 412 10 2 4 4.3 COc1ccc(F)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
228 445 None 20 Human Functional pEC50 = 8.2 8.2 -3 20
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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
33 445 None 20 Human Functional pEC50 = 8.2 8.2 -3 20
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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 445 None 20 Human Functional pEC50 = 8.2 8.2 -3 20
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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
6005.0 445 None 20 Human Functional pEC50 = 8.2 8.2 -3 20
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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 445 None 20 Human Functional pEC50 = 8.2 8.2 -3 20
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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 445 None 20 Human Functional pEC50 = 8.2 8.2 -3 20
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human 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
25072941 156565 None 0 Human Functional pEC50 = 8.2 8.2 1 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 156565 None 0 Human Functional pEC50 = 8.2 8.2 1 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
25072941 156565 None 0 Human Functional pEC50 = 8.2 8.2 1 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 156565 None 0 Human Functional pEC50 = 8.2 8.2 1 2
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 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
172454491 195657 None 0 Human Functional pEC50 = 8.2 8.2 -3 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 8 1 4 3.7 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)COC)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
CHEMBL5408223 195657 None 0 Human Functional pEC50 = 8.2 8.2 -3 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 8 1 4 3.7 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)COC)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
56599142 3942 None 7 Human Functional pEC50 = 7.3 7.3 - 1
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 420 6 0 4 6.3 Clc1cccc(c1Cl)C1CCN(CC1)CCCOc1ccc2c(c1)ncs2 10.1021/jm300603y
7652 3942 None 7 Human Functional pEC50 = 7.3 7.3 - 1
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 420 6 0 4 6.3 Clc1cccc(c1Cl)C1CCN(CC1)CCCOc1ccc2c(c1)ncs2 10.1021/jm300603y
CHEMBL2165138 3942 None 7 Human Functional pEC50 = 7.3 7.3 - 1
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 420 6 0 4 6.3 Clc1cccc(c1Cl)C1CCN(CC1)CCCOc1ccc2c(c1)ncs2 10.1021/jm300603y
71460601 82002 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 CCOc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1021/jm300603y
CHEMBL2165124 82002 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 CCOc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1021/jm300603y
46882006 5849 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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)CCN1c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.090
CHEMBL1079191 5849 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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)CCN1c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.090
172465854 196539 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 392 9 2 5 4.2 CCOc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5426286 196539 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 392 9 2 5 4.2 CCOc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
118726001 117269 None 0 Human Functional pEC50 = 6.3 6.3 -12 2
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 821 27 5 13 5.6 CCCN(CCCNC(=O)CCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394258 117269 None 0 Human Functional pEC50 = 6.3 6.3 -12 2
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 821 27 5 13 5.6 CCCN(CCCNC(=O)CCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
66559507 82009 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 481 5 1 4 6.0 O=C1CCc2ccc(Oc3ccc(CN4CCN(c5cccc(Cl)c5Cl)CC4)cc3)cc2N1 10.1021/jm300603y
CHEMBL2165132 82009 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 481 5 1 4 6.0 O=C1CCc2ccc(Oc3ccc(CN4CCN(c5cccc(Cl)c5Cl)CC4)cc3)cc2N1 10.1021/jm300603y
118726001 117269 None 0 Human Functional pEC50 = 6.3 6.3 -12 2
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 821 27 5 13 5.6 CCCN(CCCNC(=O)CCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
CHEMBL3394258 117269 None 0 Human Functional pEC50 = 6.3 6.3 -12 2
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 821 27 5 13 5.6 CCCN(CCCNC(=O)CCCCCCCNC(=O)CCCOc1ccc(CCNc2nc(N)n3nc(-c4ccco4)nc3n2)cc1)CCc1cccc2c1CC(=O)N2 10.1021/jm501254d
46881467 5593 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 260 3 1 3 1.5 O=C1N(CC2CCCCN2)CCN1c1cccnc1 10.1016/j.bmcl.2010.01.090
CHEMBL1077197 5593 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 260 3 1 3 1.5 O=C1N(CC2CCCCN2)CCN1c1cccnc1 10.1016/j.bmcl.2010.01.090
45271622 14036 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
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 357 2 2 3 4.9 CCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1197278 14036 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
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 357 2 2 3 4.9 CCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL564909 14036 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
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 357 2 2 3 4.9 CCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
172465854 196539 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 392 9 2 5 4.2 CCOc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5426286 196539 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 392 9 2 5 4.2 CCOc1cccc2cc(CNCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
77461254 191333 None 0 Human Functional pEC50 = 7.3 7.3 1 2
Agonist activity at dopamine D2 receptor (unknown origin)Agonist activity at dopamine D2 receptor (unknown origin)
ChEMBL 477 8 1 8 3.6 CCCN(CCN1CCN(c2ccc(-c3ccccn3)nc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
CHEMBL5189785 191333 None 0 Human Functional pEC50 = 7.3 7.3 1 2
Agonist activity at dopamine D2 receptor (unknown origin)Agonist activity at dopamine D2 receptor (unknown origin)
ChEMBL 477 8 1 8 3.6 CCCN(CCN1CCN(c2ccc(-c3ccccn3)nc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
56597094 148145 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 420 6 2 4 3.8 O=c1[nH]c2ccc(OCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
CHEMBL3934712 148145 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 420 6 2 4 3.8 O=c1[nH]c2ccc(OCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
169753704 195382 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 402 7 0 5 5.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2cccnc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5402456 195382 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 402 7 0 5 5.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2cccnc2c1)CC3 10.1021/acs.jmedchem.3c00098
15696482 79590 None 0 Rat Functional pEC50 = 5.3 5.3 -21 2
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
CHEMBL2114209 79590 None 0 Rat Functional pEC50 = 5.3 5.3 -21 2
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
169753704 195382 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 402 7 0 5 5.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2cccnc2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5402456 195382 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 402 7 0 5 5.2 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2cccnc2c1)CC3 10.1021/acs.jmedchem.3c00098
122177641 121273 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human dopamine D2L 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 D2L 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 121273 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human dopamine D2L 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 D2L 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
52941006 17106 None 0 Human Functional pEC50 = 7.3 7.3 -208 2
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)C1CCc2c(O)cccc2C1 10.1016/j.bmc.2010.06.025
CHEMBL1254947 17106 None 0 Human Functional pEC50 = 7.3 7.3 -208 2
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)C1CCc2c(O)cccc2C1 10.1016/j.bmc.2010.06.025
90466716 161097 None 0 Human Functional pEC50 = 7.3 7.3 -1 2
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 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099236 161097 None 0 Human Functional pEC50 = 7.3 7.3 -1 2
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 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4116199 161097 None 0 Human Functional pEC50 = 7.3 7.3 -1 2
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 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
228 445 None 20 Rat Functional pEC50 = 7.3 7.3 -4 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
33 445 None 20 Rat Functional pEC50 = 7.3 7.3 -4 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
6005 445 None 20 Rat Functional pEC50 = 7.3 7.3 -4 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
6005.0 445 None 20 Rat Functional pEC50 = 7.3 7.3 -4 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
CHEMBL53 445 None 20 Rat Functional pEC50 = 7.3 7.3 -4 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
DB00714 445 None 20 Rat Functional pEC50 = 7.3 7.3 -4 20
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
164609592 184522 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 472 11 1 3 6.5 CCCN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.1c01327
CHEMBL4846101 184522 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 472 11 1 3 6.5 CCCN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.1c01327
164609592 184522 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 472 11 1 3 6.5 CCCN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.1c01327
CHEMBL4846101 184522 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 472 11 1 3 6.5 CCCN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.1c01327
172452871 196003 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 364 8 2 4 4.3 O=C1CCc2ccc(OCCCCNCc3cc4ccccc4o3)cc2N1 10.1021/acs.jmedchem.3c00098
CHEMBL5414943 196003 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 364 8 2 4 4.3 O=C1CCc2ccc(OCCCCNCc3cc4ccccc4o3)cc2N1 10.1021/acs.jmedchem.3c00098
137631807 156655 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 487 11 2 5 4.5 CCCN(CCC)[C@@H]1Cc2cccc3c2n(c(=O)n3CCCCNC(=O)c2cc3ccccc3[nH]2)C1 10.1021/acs.jmedchem.6b01875
CHEMBL4068455 156655 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 487 11 2 5 4.5 CCCN(CCC)[C@@H]1Cc2cccc3c2n(c(=O)n3CCCCNC(=O)c2cc3ccccc3[nH]2)C1 10.1021/acs.jmedchem.6b01875
122177644 121276 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Intrinsic activity at human dopamine D2L 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 D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577345 121276 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Intrinsic activity at human dopamine D2L 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 D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
90644227 111843 None 0 Human Functional pEC50 = 6.3 6.3 -91 2
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 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287396 111843 None 0 Human Functional pEC50 = 6.3 6.3 -91 2
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 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
164624107 185828 None 0 Human Functional pEC50 = 5.3 5.3 -52 3
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 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4865765 185828 None 0 Human Functional pEC50 = 5.3 5.3 -52 3
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 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
71151588 118322 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAgonist activity at human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409256 118322 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAgonist activity at human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
72736197 103804 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 300 4 1 2 3.1 CC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL3088210 103804 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 300 4 1 2 3.1 CC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
90467024 157781 None 0 Human Functional pEC50 = 7.3 7.3 -10 2
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 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4081780 157781 None 0 Human Functional pEC50 = 7.3 7.3 -10 2
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 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
137651936 157484 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 157484 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
10854042 121595 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 332 10 1 4 2.8 CCCN(CCCC(=O)OCC)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585364 121595 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 332 10 1 4 2.8 CCCN(CCCC(=O)OCC)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
72736197 103804 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 300 4 1 2 3.1 CC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL3088210 103804 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 300 4 1 2 3.1 CC(=O)N[C@H]1CC[C@H](CCN2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.9b00508
90644227 111843 None 0 Human Functional pEC50 = 6.3 6.3 -91 2
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 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287396 111843 None 0 Human Functional pEC50 = 6.3 6.3 -91 2
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 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
162672054 183071 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 1249 41 2 16 10.9 CCCN(CCCCNC(=O)c1ccc(-c2ccc(OCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc(-c6ccc(C(=O)NCCCCN(CCC)C7Cc8ccccc8C7)cc6)cc5)nn4)nn3)cc2)cc1)C1Cc2ccccc2C1 10.1016/j.ejmech.2020.113151
CHEMBL4792999 183071 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assayAgonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay
ChEMBL 1249 41 2 16 10.9 CCCN(CCCCNC(=O)c1ccc(-c2ccc(OCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc(-c6ccc(C(=O)NCCCCN(CCC)C7Cc8ccccc8C7)cc6)cc5)nn4)nn3)cc2)cc1)C1Cc2ccccc2C1 10.1016/j.ejmech.2020.113151
122189391 123313 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613877 123313 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
137651936 157484 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 157484 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
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 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
10854042 121595 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 332 10 1 4 2.8 CCCN(CCCC(=O)OCC)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585364 121595 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 332 10 1 4 2.8 CCCN(CCCC(=O)OCC)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
44567587 178340 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
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 311 2 2 4 3.2 CCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
CHEMBL465055 178340 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
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 311 2 2 4 3.2 CCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
71733932 91086 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human dopamine D2L 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 D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2397389 91086 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human dopamine D2L 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 D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
90466425 159408 None 0 Human Functional pEC50 = 7.3 7.3 -10 2
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 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099798 159408 None 0 Human Functional pEC50 = 7.3 7.3 -10 2
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 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
6453963 71563 None 7 Human Functional pEC50 = 4.3 4.3 -10000 2
Antagonist activity at dopamine D2 receptorAntagonist activity at dopamine D2 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmcl.2012.01.005
CHEMBL1950491 71563 None 7 Human Functional pEC50 = 4.3 4.3 -10000 2
Antagonist activity at dopamine D2 receptorAntagonist activity at dopamine D2 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmcl.2012.01.005
CHEMBL1962947 71563 None 7 Human Functional pEC50 = 4.3 4.3 -10000 2
Antagonist activity at dopamine D2 receptorAntagonist activity at dopamine D2 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmcl.2012.01.005
681 1465 None 47 Human Functional pEC50 = 7.2 7.2 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
681.0 1465 None 47 Human Functional pEC50 = 7.2 7.2 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
940 1465 None 47 Human Functional pEC50 = 7.2 7.2 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
947 1465 None 47 Human Functional pEC50 = 7.2 7.2 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
CHEMBL59 1465 None 47 Human Functional pEC50 = 7.2 7.2 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
DB00988 1465 None 47 Human Functional pEC50 = 7.2 7.2 -19 15
Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysisAgonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.3c00734
172459921 196115 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 396 10 1 6 5.4 CCOc1cccc2cc(CNCCCCOc3ccc4scnc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5417227 196115 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 396 10 1 6 5.4 CCOc1cccc2cc(CNCCCCOc3ccc4scnc4c3)oc12 10.1021/acs.jmedchem.3c00098
172459921 196115 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 396 10 1 6 5.4 CCOc1cccc2cc(CNCCCCOc3ccc4scnc4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5417227 196115 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 396 10 1 6 5.4 CCOc1cccc2cc(CNCCCCOc3ccc4scnc4c3)oc12 10.1021/acs.jmedchem.3c00098
90467322 156901 None 0 Human Functional pEC50 = 7.2 7.2 6 2
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 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4071121 156901 None 0 Human Functional pEC50 = 7.2 7.2 6 2
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 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
146025820 173325 None 0 Human Functional pEC50 = 6.2 6.2 -6 2
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 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4523054 173325 None 0 Human Functional pEC50 = 6.2 6.2 -6 2
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 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
45269974 13627 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
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 371 3 2 3 5.3 CCCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1194307 13627 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
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 371 3 2 3 5.3 CCCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL550792 13627 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
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 371 3 2 3 5.3 CCCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
146025820 173325 None 0 Human Functional pEC50 = 6.2 6.2 -6 2
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 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4523054 173325 None 0 Human Functional pEC50 = 6.2 6.2 -6 2
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 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
44567594 172736 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
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 339 4 2 4 4.0 CCCCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
CHEMBL449461 172736 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
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 339 4 2 4 4.0 CCCCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
66559506 82008 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 481 5 1 4 6.0 O=C1CCc2ccc(Oc3cccc(CN4CCN(c5cccc(Cl)c5Cl)CC4)c3)cc2N1 nan
CHEMBL2165131 82008 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 481 5 1 4 6.0 O=C1CCc2ccc(Oc3cccc(CN4CCN(c5cccc(Cl)c5Cl)CC4)c3)cc2N1 nan
172447622 195955 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 11 2 5 5.0 CCOc1cccc2cc(CNCCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5414152 195955 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 420 11 2 5 5.0 CCOc1cccc2cc(CNCCCCCOc3ccc4ccc(=O)[nH]c4c3)oc12 10.1021/acs.jmedchem.3c00098
44438186 147296 None 2 Human Functional pEC50 = 6.2 6.2 - 1
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 340 3 2 2 4.3 OC1(c2ccccc2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL392822 147296 None 2 Human Functional pEC50 = 6.2 6.2 - 1
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 340 3 2 2 4.3 OC1(c2ccccc2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
164626153 186484 None 0 Human Functional pEC50 = 6.2 6.2 -9 3
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 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
CHEMBL4875600 186484 None 0 Human Functional pEC50 = 6.2 6.2 -9 3
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 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
56597939 81995 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 404 6 1 4 4.5 Clc1cccc(N2CCN(CCCOc3ccc4cn[nH]c4c3)CC2)c1Cl nan
CHEMBL2165116 81995 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 404 6 1 4 4.5 Clc1cccc(N2CCN(CCCOc3ccc4cn[nH]c4c3)CC2)c1Cl nan
71474024 144556 None 0 Human Functional pEC50 = 6.2 6.2 2 2
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 327 2 2 5 2.8 COc1cc2c(cc1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
CHEMBL3906676 144556 None 0 Human Functional pEC50 = 6.2 6.2 2 2
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 327 2 2 5 2.8 COc1cc2c(cc1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
172454491 195657 None 0 Human Functional pEC50 = 8.2 8.2 -3 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 8 1 4 3.7 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)COC)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
CHEMBL5408223 195657 None 0 Human Functional pEC50 = 8.2 8.2 -3 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 421 8 1 4 3.7 CCc1cccc(N2CCN(CC[C@H]3CC[C@H](NC(=O)COC)CC3)CC2)c1Cl 10.1021/acs.jmedchem.2c01624
56598877 147483 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 424 8 1 6 3.3 COc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
CHEMBL3929710 147483 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 424 8 1 6 3.3 COc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
56597937 146129 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 447 6 1 4 4.9 O=C1CCc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2N1 nan
CHEMBL3918805 146129 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 447 6 1 4 4.9 O=C1CCc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2N1 nan
101885477 121602 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 801 33 4 6 8.4 CCCN(CCCNC(=O)CCCCCCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585371 121602 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 801 33 4 6 8.4 CCCN(CCCNC(=O)CCCCCCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
172469879 197088 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 413 8 2 4 4.7 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N4CCCC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5438433 197088 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 413 8 2 4 4.7 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N4CCCC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
101885477 121602 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 801 33 4 6 8.4 CCCN(CCCNC(=O)CCCCCCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
CHEMBL3585371 121602 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 801 33 4 6 8.4 CCCN(CCCNC(=O)CCCCCCCCCCCCCCC(=O)NCCCN(CCC)CCc1cccc2c1CC(=O)N2)CCc1cccc2c1CC(=O)N2 10.1039/C4MD00066H
56598210 149282 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 461 7 1 4 4.7 O=C1NCCc2ccc(OCCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc21 nan
CHEMBL3943838 149282 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 461 7 1 4 4.7 O=C1NCCc2ccc(OCCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc21 nan
172469879 197088 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 413 8 2 4 4.7 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N4CCCC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5438433 197088 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T coexpressing beta-arrestin-2 assessed as increase in cAMP accumulation incubated for 5 mins by beta-arrestin recruitment based BRET assay
ChEMBL 413 8 2 4 4.7 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)N4CCCC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
172464337 196969 None 0 Human Functional pEC50 = 8.2 8.2 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5435745 196969 None 0 Human Functional pEC50 = 8.2 8.2 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
10114519 55258 None 46 Human Functional pEC50 = 8.2 8.2 - 1
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 445 7 1 5 5.2 Oc1ccc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2n1 10.1021/jm300603y
CHEMBL161792 55258 None 46 Human Functional pEC50 = 8.2 8.2 - 1
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 445 7 1 5 5.2 Oc1ccc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2n1 10.1021/jm300603y
66559587 81997 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 447 6 1 4 4.3 O=C1NCCc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc21 10.1021/jm300603y
CHEMBL2165118 81997 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 447 6 1 4 4.3 O=C1NCCc2ccc(OCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc21 10.1021/jm300603y
172464337 196969 None 0 Human Functional pEC50 = 8.2 8.2 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
CHEMBL5435745 196969 None 0 Human Functional pEC50 = 8.2 8.2 1 2
Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysisPartial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
ChEMBL 427 7 0 4 3.8 COCCC(=O)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.2c01624
164619127 185631 None 0 Human Functional pEC50 = 8.2 8.2 8 3
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 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185631 None 0 Human Functional pEC50 = 8.2 8.2 8 3
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 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
119570 3159 None 58 Human Functional pEC50 = 8.2 8.2 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
119570.0 3159 None 58 Human Functional pEC50 = 8.2 8.2 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
2233 3159 None 58 Human Functional pEC50 = 8.2 8.2 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
953 3159 None 58 Human Functional pEC50 = 8.2 8.2 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
CHEMBL301265 3159 None 58 Human Functional pEC50 = 8.2 8.2 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
DB00413 3159 None 58 Human Functional pEC50 = 8.2 8.2 -28 11
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 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
164619127 185631 None 0 Human Functional pEC50 = 8.2 8.2 8 3
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 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185631 None 0 Human Functional pEC50 = 8.2 8.2 8 3
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 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
172457140 196444 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 10 2 5 4.7 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5424038 196444 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 10 2 5 4.7 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
172457140 196444 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 10 2 5 4.7 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5424038 196444 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 408 10 2 5 4.7 CCOc1cccc2cc(CNCCCCOc3ccc4c(c3)NC(=O)CC4)oc12 10.1021/acs.jmedchem.3c00098
164628423 186379 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4874021 186379 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164628423 186379 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4874021 186379 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 396 9 2 4 3.8 COc1ccc(F)cc1C1CC1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164616008 185418 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 428 10 2 4 4.8 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4859410 185418 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 428 10 2 4 4.8 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
172454187 195871 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 384 9 2 4 4.4 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)C4CC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5412359 195871 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 384 9 2 4 4.4 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)C4CC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
146025765 172025 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 386 7 1 3 3.6 CN(C)C(=O)NCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.9b00508
CHEMBL4470060 172025 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 386 7 1 3 3.6 CN(C)C(=O)NCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.9b00508
164616008 185418 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 428 10 2 4 4.8 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4859410 185418 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 428 10 2 4 4.8 COc1ccc(Cl)cc1C1CC1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
172454187 195871 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 384 9 2 4 4.4 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)C4CC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
CHEMBL5412359 195871 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at Dopamine D2 receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 384 9 2 4 4.4 CCOc1cccc2cc(CNCC[C@H]3CC[C@H](NC(=O)C4CC4)CC3)oc12 10.1021/acs.jmedchem.3c00098
164617999 185182 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 392 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4855775 185182 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 392 9 2 4 3.9 COc1ccccc1C1CC1CNC/C=C/COc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
137633705 156709 None 0 Human Functional pEC50 = 6.2 6.2 -158 2
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 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4069091 156709 None 0 Human Functional pEC50 = 6.2 6.2 -158 2
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 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
121418491 171889 None 4 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at dopamine D2long r