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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors UniProt IUPHAR Species p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
11141 331 46 DRD2 D2 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
120 331 46 DRD2 D2 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
135413504 331 46 DRD2 D2 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
43008 331 46 DRD2 D2 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
CHEMBL290194 331 46 DRD2 D2 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
DB01425 331 46 DRD2 D2 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 315 6 2 5 1.3 C=CCN1CCCC1CNC(=O)c1cc2[nH]nnc2cc1OC None
11140 2366 36 DRD2 D2 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C None
1784 2366 36 DRD2 D2 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C None
26388 2366 36 DRD2 D2 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C None
CHEMBL398615 2366 36 DRD2 D2 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C None
DB13591 2366 36 DRD2 D2 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C None
57383405 109205 0 DRD2 D2 receptor Human 6.0 pAC50 = 6.0 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
CHEMBL3234541 109205 0 DRD2 D2 receptor Human 6.0 pAC50 = 6.0 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
57383409 109153 0 DRD2 D2 receptor Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccc(OC)c3)cc21 10.1021/jm500126s
CHEMBL3234238 109153 0 DRD2 D2 receptor Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccc(OC)c3)cc21 10.1021/jm500126s
57383437 109179 0 DRD2 D2 receptor Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 420 4 1 4 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)N(C)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
CHEMBL3234511 109179 0 DRD2 D2 receptor Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 420 4 1 4 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)N(C)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
57383415 109192 0 DRD2 D2 receptor Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 411 4 1 4 2.7 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCN3CCCCC3)cc21 10.1021/jm500126s
CHEMBL3234524 109192 0 DRD2 D2 receptor Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 411 4 1 4 2.7 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCN3CCCCC3)cc21 10.1021/jm500126s
57383414 109200 0 DRD2 D2 receptor Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
CHEMBL3234537 109200 0 DRD2 D2 receptor Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
57383402 109188 0 DRD2 D2 receptor Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccn3)cc21 10.1021/jm500126s
CHEMBL3234520 109188 0 DRD2 D2 receptor Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccn3)cc21 10.1021/jm500126s
57383403 109195 1 DRD2 D2 receptor Human 5.9 pAC50 = 5.9 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234527 109195 1 DRD2 D2 receptor Human 5.9 pAC50 = 5.9 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383397 109201 0 DRD2 D2 receptor Human 5.9 pAC50 = 5.9 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
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 109201 0 DRD2 D2 receptor Human 5.9 pAC50 = 5.9 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
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
57377245 109170 0 DRD2 D2 receptor Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 472 4 1 3 4.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C(F)(F)F)cc3)cc21 10.1021/jm500126s
CHEMBL3234502 109170 0 DRD2 D2 receptor Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 472 4 1 3 4.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C(F)(F)F)cc3)cc21 10.1021/jm500126s
57377247 109171 0 DRD2 D2 receptor Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
CHEMBL3234503 109171 0 DRD2 D2 receptor Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
57383428 109176 0 DRD2 D2 receptor Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 420 4 1 4 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234508 109176 0 DRD2 D2 receptor Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 420 4 1 4 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383411 109185 0 DRD2 D2 receptor Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
CHEMBL3234517 109185 0 DRD2 D2 receptor Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
57383403 109195 1 DRD2 D2 receptor Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234527 109195 1 DRD2 D2 receptor Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383424 109181 0 DRD2 D2 receptor Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 376 2 1 3 3.7 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccccc3)cc21 10.1021/jm500126s
CHEMBL3234513 109181 0 DRD2 D2 receptor Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 376 2 1 3 3.7 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccccc3)cc21 10.1021/jm500126s
16007816 45189 5 DRD2 D2 receptor Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 4 1 3 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C)cc3)cc21 10.1021/jm500126s
CHEMBL1529544 45189 5 DRD2 D2 receptor Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 4 1 3 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C)cc3)cc21 10.1021/jm500126s
57383429 109173 0 DRD2 D2 receptor Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 494 7 1 6 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cc(OC)c(OC)c(OC)c3)cc21 10.1021/jm500126s
CHEMBL3234505 109173 0 DRD2 D2 receptor Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 494 7 1 6 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cc(OC)c(OC)c(OC)c3)cc21 10.1021/jm500126s
57383435 109168 0 DRD2 D2 receptor Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 450 5 1 4 4.5 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(SC)cc3)cc21 10.1021/jm500126s
CHEMBL3234500 109168 0 DRD2 D2 receptor Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 450 5 1 4 4.5 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(SC)cc3)cc21 10.1021/jm500126s
57383416 109183 0 DRD2 D2 receptor Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 390 3 1 3 3.4 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3)cc21 10.1021/jm500126s
CHEMBL3234515 109183 0 DRD2 D2 receptor Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 390 3 1 3 3.4 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3)cc21 10.1021/jm500126s
57383398 109198 0 DRD2 D2 receptor Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 4.2 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(NC(=O)Cc3ccc(F)cc3)cc21 10.1021/jm500126s
CHEMBL3234535 109198 0 DRD2 D2 receptor Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 4.2 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(NC(=O)Cc3ccc(F)cc3)cc21 10.1021/jm500126s
57383397 109201 0 DRD2 D2 receptor Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 496 4 1 3 5.1 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc(Br)cc3)cc21 10.1021/jm500126s
CHEMBL3234538 109201 0 DRD2 D2 receptor Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 496 4 1 3 5.1 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc(Br)cc3)cc21 10.1021/jm500126s
57383414 109200 0 DRD2 D2 receptor Human 6.6 pAC50 = 6.6 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
CHEMBL3234537 109200 0 DRD2 D2 receptor Human 6.6 pAC50 = 6.6 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
16007814 42454 4 DRD2 D2 receptor Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL1503220 42454 4 DRD2 D2 receptor Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383420 109204 0 DRD2 D2 receptor Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
CHEMBL3234540 109204 0 DRD2 D2 receptor Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
57383413 109186 0 DRD2 D2 receptor Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccc(Cl)c3)cc21 10.1021/jm500126s
CHEMBL3234518 109186 0 DRD2 D2 receptor Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccc(Cl)c3)cc21 10.1021/jm500126s
57383422 109189 0 DRD2 D2 receptor Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
CHEMBL3234521 109189 0 DRD2 D2 receptor Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
16007814 42454 4 DRD2 D2 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL1503220 42454 4 DRD2 D2 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383434 109202 0 DRD2 D2 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
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 109202 0 DRD2 D2 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 468 4 1 3 5.5 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc4ccccc4c3)cc21 10.1021/jm500126s
57383420 109204 0 DRD2 D2 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
CHEMBL3234540 109204 0 DRD2 D2 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
57383436 109206 0 DRD2 D2 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
CHEMBL3234542 109206 0 DRD2 D2 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
57383400 109169 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 460 4 1 3 5.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C(C)(C)C)cc3)cc21 10.1021/jm500126s
CHEMBL3234501 109169 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 460 4 1 3 5.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(C(C)(C)C)cc3)cc21 10.1021/jm500126s
57383418 109172 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 482 5 1 5 3.2 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)cc21 10.1021/jm500126s
CHEMBL3234504 109172 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 482 5 1 5 3.2 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(S(C)(=O)=O)cc3)cc21 10.1021/jm500126s
20861039 109174 4 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 4 1 5 3.5 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc4c(c3)OCO4)cc21 10.1021/jm500126s
CHEMBL3234506 109174 4 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 4 1 5 3.5 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc4c(c3)OCO4)cc21 10.1021/jm500126s
57383427 109177 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 6 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234509 109177 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 6 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383404 109182 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 406 3 1 4 3.7 COc1ccc(NC(=O)c2ccc3c(c2)N(C)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
CHEMBL3234514 109182 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 406 3 1 4 3.7 COc1ccc(NC(=O)c2ccc3c(c2)N(C)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
57383433 109184 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 408 3 1 3 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
CHEMBL3234516 109184 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 408 3 1 3 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
57383434 109202 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 4 1 3 5.5 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc4ccccc4c3)cc21 10.1021/jm500126s
CHEMBL3234539 109202 0 DRD2 D2 receptor Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 4 1 3 5.5 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc4ccccc4c3)cc21 10.1021/jm500126s
57383401 109207 0 DRD2 D2 receptor Human 6.4 pAC50 = 6.4 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
CHEMBL3234543 109207 0 DRD2 D2 receptor Human 6.4 pAC50 = 6.4 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
57383399 109154 0 DRD2 D2 receptor Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 404 4 1 3 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3)cc21 10.1021/jm500126s
CHEMBL3234239 109154 0 DRD2 D2 receptor Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 404 4 1 3 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3)cc21 10.1021/jm500126s
57383436 109206 0 DRD2 D2 receptor Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
CHEMBL3234542 109206 0 DRD2 D2 receptor Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
16007818 59258 5 DRD2 D2 receptor Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3OC)cc21 10.1021/jm500126s
CHEMBL1726600 59258 5 DRD2 D2 receptor Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccccc3OC)cc21 10.1021/jm500126s
16007812 58952 5 DRD2 D2 receptor Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 438 4 1 3 4.4 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
CHEMBL1714249 58952 5 DRD2 D2 receptor Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 438 4 1 3 4.4 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
57383430 109199 0 DRD2 D2 receptor Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
CHEMBL3234536 109199 0 DRD2 D2 receptor Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
20861041 109167 1 DRD2 D2 receptor Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 4 1 3 4.3 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NC(C)c3ccccc3)cc21 10.1021/jm500126s
CHEMBL3234499 109167 1 DRD2 D2 receptor Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 4 1 3 4.3 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NC(C)c3ccccc3)cc21 10.1021/jm500126s
57383406 109193 0 DRD2 D2 receptor Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 385 5 1 4 2.1 CN(C)CCCNC(=O)c1ccc2c(c1)N(C)C(=O)c1ccccc1[S+]2[O-] 10.1021/jm500126s
CHEMBL3234525 109193 0 DRD2 D2 receptor Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 385 5 1 4 2.1 CN(C)CCCNC(=O)c1ccc2c(c1)N(C)C(=O)c1ccccc1[S+]2[O-] 10.1021/jm500126s
57383417 109196 0 DRD2 D2 receptor Human 4.3 pAC50 = 4.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 432 5 0 3 4.5 CCN(Cc1ccccc1)C(=O)c1ccc2c(c1)N(CC)C(=O)c1ccccc1[S+]2[O-] 10.1021/jm500126s
CHEMBL3234532 109196 0 DRD2 D2 receptor Human 4.3 pAC50 = 4.3 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 432 5 0 3 4.5 CCN(Cc1ccccc1)C(=O)c1ccc2c(c1)N(CC)C(=O)c1ccccc1[S+]2[O-] 10.1021/jm500126s
57383430 109199 0 DRD2 D2 receptor Human 6.2 pAC50 = 6.2 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
CHEMBL3234536 109199 0 DRD2 D2 receptor Human 6.2 pAC50 = 6.2 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
57377246 2415 0 DRD2 D2 receptor Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 410 4 1 4 3.5 O=C(c1ccc2c(c1)N(C)C(=O)c1c([S@@]2=O)cccc1)NCCc1cccs1 10.1021/jm500126s
8368 2415 0 DRD2 D2 receptor Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 410 4 1 4 3.5 O=C(c1ccc2c(c1)N(C)C(=O)c1c([S@@]2=O)cccc1)NCCc1cccs1 10.1021/jm500126s
CHEMBL3234544 2415 0 DRD2 D2 receptor Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 410 4 1 4 3.5 O=C(c1ccc2c(c1)N(C)C(=O)c1c([S@@]2=O)cccc1)NCCc1cccs1 10.1021/jm500126s
57383401 109207 0 DRD2 D2 receptor Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
CHEMBL3234543 109207 0 DRD2 D2 receptor Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
57383423 109180 0 DRD2 D2 receptor Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 6 1 4 4.2 CCCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234512 109180 0 DRD2 D2 receptor Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 448 6 1 4 4.2 CCCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383432 109194 0 DRD2 D2 receptor Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 5 1 4 4.8 CCN1C(=O)c2ccccc2Sc2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234526 109194 0 DRD2 D2 receptor Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 418 5 1 4 4.8 CCN1C(=O)c2ccccc2Sc2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383419 109197 0 DRD2 D2 receptor Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 4.0 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(NC(=O)Cc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234534 109197 0 DRD2 D2 receptor Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 434 5 1 4 4.0 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(NC(=O)Cc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383421 109187 0 DRD2 D2 receptor Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
CHEMBL3234519 109187 0 DRD2 D2 receptor Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
57377246 2415 0 DRD2 D2 receptor Human 6.1 pAC50 = 6.1 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
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 2415 0 DRD2 D2 receptor Human 6.1 pAC50 = 6.1 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
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 2415 0 DRD2 D2 receptor Human 6.1 pAC50 = 6.1 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 410 4 1 4 3.5 O=C(c1ccc2c(c1)N(C)C(=O)c1c([S@@]2=O)cccc1)NCCc1cccs1 10.1021/jm500126s
57383426 109175 0 DRD2 D2 receptor Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 390 3 1 3 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccccc3)cc21 10.1021/jm500126s
CHEMBL3234507 109175 0 DRD2 D2 receptor Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 390 3 1 3 4.1 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)Nc3ccccc3)cc21 10.1021/jm500126s
57383425 109178 0 DRD2 D2 receptor Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 406 4 2 4 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)NC(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
CHEMBL3234510 109178 0 DRD2 D2 receptor Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 406 4 2 4 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)NC(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
16007752 58728 5 DRD2 D2 receptor Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 496 6 1 4 5.0 COc1ccc(CNC(=O)c2ccc3c(c2)N(Cc2ccccc2)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
CHEMBL1703877 58728 5 DRD2 D2 receptor Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 496 6 1 4 5.0 COc1ccc(CNC(=O)c2ccc3c(c2)N(Cc2ccccc2)C(=O)c2ccccc2[S+]3[O-])cc1 10.1021/jm500126s
16007820 66927 2 DRD2 D2 receptor Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
CHEMBL1894173 66927 2 DRD2 D2 receptor Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
57383431 109190 0 DRD2 D2 receptor Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 410 4 1 4 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3cccs3)cc21 10.1021/jm500126s
CHEMBL3234522 109190 0 DRD2 D2 receptor Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 410 4 1 4 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3cccs3)cc21 10.1021/jm500126s
57383412 109191 0 DRD2 D2 receptor Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
CHEMBL3234523 109191 0 DRD2 D2 receptor Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
57383405 109205 0 DRD2 D2 receptor Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
CHEMBL3234541 109205 0 DRD2 D2 receptor Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
57383431 109190 0 DRD2 D2 receptor Human 6.0 pAC50 = 6.0 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 410 4 1 4 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3cccs3)cc21 10.1021/jm500126s
CHEMBL3234522 109190 0 DRD2 D2 receptor Human 6.0 pAC50 = 6.0 Binding
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 410 4 1 4 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3cccs3)cc21 10.1021/jm500126s
1588 2189 17 DRD2 D2 receptor Human 11.0 pEC50 = 11 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2189 17 DRD2 D2 receptor Human 11.0 pEC50 = 11 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2189 17 DRD2 D2 receptor Human 11.0 pEC50 = 11 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2189 17 DRD2 D2 receptor Human 11.0 pEC50 = 11 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2189 17 DRD2 D2 receptor Human 11.0 pEC50 = 11 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
10015731 201698 0 DRD2 D2 receptor Rat 10.9 pEC50 = 10.9 Functional
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from rat
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@H]21 10.1021/jm0000113
CHEMBL98305 201698 0 DRD2 D2 receptor Rat 10.9 pEC50 = 10.9 Functional
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from rat
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@H]21 10.1021/jm0000113
10378389 196825 1 DRD2 D2 receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 196825 1 DRD2 D2 receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 196825 1 DRD2 D2 receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
76325150 105702 0 DRD2 D2 receptor Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 105702 0 DRD2 D2 receptor Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 105702 0 DRD2 D2 receptor Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
167715 2702 11 DRD2 D2 receptor Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2702 11 DRD2 D2 receptor Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2702 11 DRD2 D2 receptor Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
167715 2702 11 DRD2 D2 receptor Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2702 11 DRD2 D2 receptor Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2702 11 DRD2 D2 receptor Human 10.4 pEC50 = 10.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
76325156 105670 1 DRD2 D2 receptor Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 105670 1 DRD2 D2 receptor Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 105670 1 DRD2 D2 receptor Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
137657882 158848 0 DRD2 D2 receptor Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 158848 0 DRD2 D2 receptor Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
137657882 158848 0 DRD2 D2 receptor Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 158848 0 DRD2 D2 receptor Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as increase in forskolin-mediated cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
56599011 145627 0 DRD2 D2 receptor Human 10.0 pEC50 = 10 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 449 9 1 5 4.7 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
CHEMBL3921903 145627 0 DRD2 D2 receptor Human 10.0 pEC50 = 10 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 449 9 1 5 4.7 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 nan
137643309 157592 0 DRD2 D2 receptor Human 10.0 pEC50 = 10.0 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4090208 157592 0 DRD2 D2 receptor Human 10.0 pEC50 = 10.0 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137643309 157592 0 DRD2 D2 receptor Human 10.0 pEC50 = 10.0 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4090208 157592 0 DRD2 D2 receptor Human 10.0 pEC50 = 10.0 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137660837 158256 0 DRD2 D2 receptor Human 10.0 pEC50 = 10.0 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 158256 0 DRD2 D2 receptor Human 10.0 pEC50 = 10.0 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137651936 156575 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 156575 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137640371 156001 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071185 156001 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137651936 156575 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 156575 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137640371 156001 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071185 156001 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137660837 158256 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 158256 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
44554472 105562 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099226 105562 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139040 105562 0 DRD2 D2 receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
76328715 105652 0 DRD2 D2 receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115582 105652 0 DRD2 D2 receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139265 105652 0 DRD2 D2 receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
137638973 156060 0 DRD2 D2 receptor Human 9.8 pEC50 = 9.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071868 156060 0 DRD2 D2 receptor Human 9.8 pEC50 = 9.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137659990 158406 0 DRD2 D2 receptor Human 9.8 pEC50 = 9.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4098859 158406 0 DRD2 D2 receptor Human 9.8 pEC50 = 9.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
13851595 173660 2 DRD2 D2 receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3098131 173660 2 DRD2 D2 receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL455497 173660 2 DRD2 D2 receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
137638973 156060 0 DRD2 D2 receptor Human 9.7 pEC50 = 9.7 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071868 156060 0 DRD2 D2 receptor Human 9.7 pEC50 = 9.7 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
66633659 152531 0 DRD2 D2 receptor Human 9.7 pEC50 = 9.7 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 452 9 1 6 4.1 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
CHEMBL3978288 152531 0 DRD2 D2 receptor Human 9.7 pEC50 = 9.7 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 452 9 1 6 4.1 CC(C)Oc1ccccc1N1CCCN(CCCCOc2ccc3c(n2)NC(=O)CC3)CC1 nan
137659990 158406 0 DRD2 D2 receptor Human 9.7 pEC50 = 9.7 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4098859 158406 0 DRD2 D2 receptor Human 9.7 pEC50 = 9.7 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
17449900 138747 8 DRD2 D2 receptor Human 9.7 pEC50 = 9.7 Functional
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 138747 8 DRD2 D2 receptor Human 9.7 pEC50 = 9.7 Functional
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
132578416 172961 0 DRD2 D2 receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human D2 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 383 9 3 4 4.8 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4538230 172961 0 DRD2 D2 receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human D2 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 383 9 3 4 4.8 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2016.08.021
17449900 138747 8 DRD2 D2 receptor Human 9.6 pEC50 = 9.6 Functional
Intrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 138747 8 DRD2 D2 receptor Human 9.6 pEC50 = 9.6 Functional
Intrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
3045992 175227 1 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4591021 175227 1 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
137651936 156575 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 156575 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137660837 158256 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 158256 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
127046922 138918 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at dopamine D2 receptor (unknown origin) by cAMP accumulation assayAgonist activity at dopamine D2 receptor (unknown origin) by cAMP accumulation assay
ChEMBL 417 7 3 4 2.9 CN(CCCCNC(=O)c1cc2ccccc2[nH]1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.8b00435
CHEMBL3798179 138918 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at dopamine D2 receptor (unknown origin) by cAMP accumulation assayAgonist activity at dopamine D2 receptor (unknown origin) by cAMP accumulation assay
ChEMBL 417 7 3 4 2.9 CN(CCCCNC(=O)c1cc2ccccc2[nH]1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.8b00435
90645289 111775 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assayAgonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assay
ChEMBL 519 8 2 6 5.5 Cc1cc(C)c2c(N)c(C(=O)NCCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)sc2n1 10.1021/jm500457x
CHEMBL3298895 111775 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assayAgonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assay
ChEMBL 519 8 2 6 5.5 Cc1cc(C)c2c(N)c(C(=O)NCCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)sc2n1 10.1021/jm500457x
10715828 53560 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 397 7 1 4 3.7 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4F)CC3)cc2N1 10.1021/jm300603y
CHEMBL160630 53560 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 397 7 1 4 3.7 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4F)CC3)cc2N1 10.1021/jm300603y
127046922 138918 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 417 7 3 4 2.9 CN(CCCCNC(=O)c1cc2ccccc2[nH]1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.6b01875
CHEMBL3798179 138918 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 417 7 3 4 2.9 CN(CCCCNC(=O)c1cc2ccccc2[nH]1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.6b01875
137640371 156001 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071185 156001 0 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
3045992 175227 1 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4591021 175227 1 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
2105 2869 27 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 2869 27 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 2869 27 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 2869 27 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 2869 27 DRD2 D2 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
219050 3171 15 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
52 3171 15 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
CHEMBL431367 3171 15 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
3033200 173682 3 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 173682 3 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
3033200 173682 3 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 173682 3 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
57420188 111795 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 349 6 1 5 2.7 COc1ccccc1N1CCN(CCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
CHEMBL3299094 111795 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 349 6 1 5 2.7 COc1ccccc1N1CCN(CCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
137638973 156060 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071868 156060 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137643309 157592 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4090208 157592 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
57420188 111795 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 349 6 1 5 2.7 COc1ccccc1N1CCN(CCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
CHEMBL3299094 111795 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 349 6 1 5 2.7 COc1ccccc1N1CCN(CCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
76325152 105651 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 105651 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 105651 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
12899503 53228 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 379 7 1 4 3.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm300603y
CHEMBL160357 53228 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 379 7 1 4 3.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm300603y
228 425 20 DRD2 D2 receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 425 20 DRD2 D2 receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 425 20 DRD2 D2 receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 425 20 DRD2 D2 receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 425 20 DRD2 D2 receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
56597940 153149 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 450 7 2 6 2.9 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCC(=O)N5)CC3)cc2N1 nan
CHEMBL3983588 153149 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 450 7 2 6 2.9 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCC(=O)N5)CC3)cc2N1 nan
228 425 20 DRD2 D2 receptor Rat 9.4 pEC50 = 9.4 Binding
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
33 425 20 DRD2 D2 receptor Rat 9.4 pEC50 = 9.4 Binding
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
6005 425 20 DRD2 D2 receptor Rat 9.4 pEC50 = 9.4 Binding
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL53 425 20 DRD2 D2 receptor Rat 9.4 pEC50 = 9.4 Binding
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
DB00714 425 20 DRD2 D2 receptor Rat 9.4 pEC50 = 9.4 Binding
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL4451797 169852 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Binding
Partial agonist activity at human D2L receptor expressed in HEK293T cells co-expressing Galpahi1/Gbeta1/GFP2-Ggamma2 assessed as Galphai1 dissociation after 15 mins in presence of coelenterazine 400a by luciferase reporter gene assayPartial agonist activity at human D2L receptor expressed in HEK293T cells co-expressing Galpahi1/Gbeta1/GFP2-Ggamma2 assessed as Galphai1 dissociation after 15 mins in presence of coelenterazine 400a by luciferase reporter gene 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
11154555 756 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
5037 756 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
7671 756 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
CHEMBL2028019 756 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
DB06016 756 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
21073553 144394 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 438 7 1 7 2.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)nc2N1 nan
CHEMBL3912435 144394 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 438 7 1 7 2.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)nc2N1 nan
137633863 155813 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 155813 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
137633863 155813 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 155813 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
71459660 83186 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 548 17 2 4 8.1 CCCN(CCCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
CHEMBL2206265 83186 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 548 17 2 4 8.1 CCCN(CCCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
11154555 756 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
5037 756 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
7671 756 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
CHEMBL2028019 756 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
DB06016 756 0 DRD2 D2 receptor Human 9.4 pEC50 = 9.4 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.9b00508
137659990 158406 0 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4098859 158406 0 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
44554649 103552 0 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099235 103552 0 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
10692886 53160 1 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
CHEMBL160296 53160 1 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
CHEMBL1813590 53160 1 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 nan
10425024 6876 2 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
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 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1021/jm950721m
CHEMBL108531 6876 2 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
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 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1021/jm950721m
10357631 7726 0 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1021/jm950721m
CHEMBL109063 7726 0 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1021/jm950721m
31101 690 31 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 690 31 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 690 31 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 690 31 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 690 31 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assayAgonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
52937876 60625 0 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrsAgonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrs
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765633 60625 0 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrsAgonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrs
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
137640371 156001 0 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071185 156001 0 DRD2 D2 receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137638973 156060 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071868 156060 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
44554820 105565 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099222 105565 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139044 105565 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
21073553 144394 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 438 7 1 7 2.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)nc2N1 nan
CHEMBL3912435 144394 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 438 7 1 7 2.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)nc2N1 nan
11154555 756 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assayPartial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene 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 756 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assayPartial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene 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 756 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assayPartial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene 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 756 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assayPartial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene 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 756 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assayPartial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene 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
10692886 53160 1 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL160296 53160 1 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL1813590 53160 1 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
58765508 111796 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 363 7 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
CHEMBL3299095 111796 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 363 7 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
58765508 111796 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 363 7 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
CHEMBL3299095 111796 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 363 7 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
137660837 158256 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 158256 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137657882 158848 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 158848 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
681 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
940 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
947 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
CHEMBL59 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
DB00988 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
76321554 105683 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 105683 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 105683 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
11154555 756 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assayPartial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene 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 756 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assayPartial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene 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 756 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assayPartial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene 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 756 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assayPartial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene 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 756 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assayPartial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene 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
46882052 5981 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 287 4 0 2 2.8 O=C1N(CCN2CCCCCC2)CCN1c1ccccc1 10.1016/j.bmcl.2010.01.090
CHEMBL1081489 5981 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 287 4 0 2 2.8 O=C1N(CCN2CCCCCC2)CCN1c1ccccc1 10.1016/j.bmcl.2010.01.090
46881463 6958 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 293 3 1 2 2.7 O=C1N(CC2CCCCN2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1085672 6958 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 293 3 1 2 2.7 O=C1N(CC2CCCCN2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
137657882 158848 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 158848 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human dopamine D2L receptor expressed in F1pIn CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4526364 172473 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 355 4 1 3 4.0 N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.9b00508
137651936 156575 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 156575 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
21786101 154923 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 261 2 2 3 2.7 CCCN1CCC[C@@H]2Cc3c(ccc(O)c3O)C[C@H]21 10.1016/j.bmc.2007.06.036
CHEMBL405519 154923 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 261 2 2 3 2.7 CCCN1CCC[C@@H]2Cc3c(ccc(O)c3O)C[C@H]21 10.1016/j.bmc.2007.06.036
137659990 158406 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4098859 158406 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
681 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.6b01857
940 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.6b01857
947 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.6b01857
CHEMBL59 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.6b01857
DB00988 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.6b01857
681 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2016.07.038
940 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2016.07.038
947 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2016.07.038
CHEMBL59 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2016.07.038
DB00988 1368 56 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2016.07.038
2407 3170 63 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
59227 3170 63 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
941 3170 63 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
CHEMBL1303 3170 63 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
DB05271 3170 63 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
CHEMBL4526364 172473 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 355 4 1 3 4.0 N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1021/acs.jmedchem.9b00508
122167 11954 10 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Tested for intrinsic activity towards Dopamine receptor D2 in CHO cellsTested for intrinsic activity towards Dopamine receptor D2 in CHO cells
ChEMBL 263 5 2 3 3.1 CCCN(CCC)C1CCc2c(ccc(O)c2O)C1 10.1021/jm0307786
CHEMBL11845 11954 10 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Tested for intrinsic activity towards Dopamine receptor D2 in CHO cellsTested for intrinsic activity towards Dopamine receptor D2 in CHO cells
ChEMBL 263 5 2 3 3.1 CCCN(CCC)C1CCc2c(ccc(O)c2O)C1 10.1021/jm0307786
137643309 157592 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4090208 157592 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
131801153 169152 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at dopamine D2 receptor (unknown origin) assessed as increase in beta-arrestin-2 recruitment after 20 mins measured for 1 sec by BRET-based luciferase reporter gene assayAgonist activity at dopamine D2 receptor (unknown origin) assessed as increase in beta-arrestin-2 recruitment after 20 mins measured for 1 sec by BRET-based luciferase reporter gene assay
ChEMBL 418 7 2 4 4.0 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5[nH]ccc45)CC3)cc2N1 10.1021/acs.jmedchem.8b00435
CHEMBL4442260 169152 0 DRD2 D2 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at dopamine D2 receptor (unknown origin) assessed as increase in beta-arrestin-2 recruitment after 20 mins measured for 1 sec by BRET-based luciferase reporter gene assayAgonist activity at dopamine D2 receptor (unknown origin) assessed as increase in beta-arrestin-2 recruitment after 20 mins measured for 1 sec by BRET-based luciferase reporter gene assay
ChEMBL 418 7 2 4 4.0 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5[nH]ccc45)CC3)cc2N1 10.1021/acs.jmedchem.8b00435
137640371 156001 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071185 156001 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137643309 157592 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4090208 157592 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
25093832 155071 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155071 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
25093832 155071 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155071 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
681 1368 56 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.6b01857
940 1368 56 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.6b01857
947 1368 56 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.6b01857
CHEMBL59 1368 56 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.6b01857
DB00988 1368 56 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.6b01857
46882053 5982 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 305 4 0 2 2.9 O=C1N(CCN2CCCCCC2)CCN1c1cccc(F)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1081490 5982 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 305 4 0 2 2.9 O=C1N(CCN2CCCCCC2)CCN1c1cccc(F)c1 10.1016/j.bmcl.2010.01.090
10715828 53560 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 397 7 1 4 3.7 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4F)CC3)cc2N1 10.1021/jm300603y
CHEMBL160630 53560 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 397 7 1 4 3.7 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4F)CC3)cc2N1 10.1021/jm300603y
10763756 53925 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 404 7 1 5 3.4 N#Cc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL160921 53925 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 404 7 1 5 3.4 N#Cc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
10502413 168642 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 423 9 1 5 4.0 CCOc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
CHEMBL443034 168642 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 423 9 1 5 4.0 CCOc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1021/jm300603y
681 1368 56 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
940 1368 56 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
947 1368 56 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
CHEMBL59 1368 56 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
DB00988 1368 56 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
137651936 156575 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 156575 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
12899503 53228 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 379 7 1 4 3.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm300603y
CHEMBL160357 53228 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 379 7 1 4 3.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm300603y
44554468 105547 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099225 105547 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139011 105547 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
137660837 158256 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 158256 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
127047229 138770 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 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 138770 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay
ChEMBL 315 7 0 4 3.3 CCCN(CCC)[C@@H]1Cc2cccc3c2n(c(=O)n3CCC)C1 10.1021/acs.jmedchem.6b01875
66633662 151214 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 435 7 1 6 3.3 O=c1ccc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)cc2[nH]1 nan
CHEMBL3966956 151214 0 DRD2 D2 receptor Human 9.1 pEC50 = 9.1 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 435 7 1 6 3.3 O=c1ccc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)cc2[nH]1 nan
137638973 156060 0 DRD2 D2 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071868 156060 0 DRD2 D2 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137659990 158406 0 DRD2 D2 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4098859 158406 0 DRD2 D2 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
131801153 169152 0 DRD2 D2 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 1 hr by FLIPR assayAgonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 1 hr by FLIPR assay
ChEMBL 418 7 2 4 4.0 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5[nH]ccc45)CC3)cc2N1 10.1021/acs.jmedchem.8b00435
CHEMBL4442260 169152 0 DRD2 D2 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 1 hr by FLIPR assayAgonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 1 hr by FLIPR assay
ChEMBL 418 7 2 4 4.0 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5[nH]ccc45)CC3)cc2N1 10.1021/acs.jmedchem.8b00435
681 1368 56 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2019.04.014
940 1368 56 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2019.04.014
947 1368 56 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2019.04.014
CHEMBL59 1368 56 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2019.04.014
DB00988 1368 56 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assayAgonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2019.04.014
242 451 110 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
34 451 110 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
60795 451 110 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
CHEMBL1112 451 110 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
DB01238 451 110 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
44554984 103548 0 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099231 103548 0 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
127047229 138770 0 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 315 7 0 4 3.3 CCCN(CCC)[C@@H]1Cc2cccc3c2n(c(=O)n3CCC)C1 10.1021/acs.jmedchem.6b01875
CHEMBL3797209 138770 0 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
ChEMBL 315 7 0 4 3.3 CCCN(CCC)[C@@H]1Cc2cccc3c2n(c(=O)n3CCC)C1 10.1021/acs.jmedchem.6b01875
132955 167557 7 DRD2 D2 receptor Human 9.0 pEC50 = 9 Binding
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 231 3 2 4 1.7 CCCN[C@@H]1Cc2cccc3nc(O)n(c23)C1 10.1021/acs.jmedchem.5b01612
CHEMBL434665 167557 7 DRD2 D2 receptor Human 9.0 pEC50 = 9 Binding
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 231 3 2 4 1.7 CCCN[C@@H]1Cc2cccc3nc(O)n(c23)C1 10.1021/acs.jmedchem.5b01612
10684789 8941 1 DRD2 D2 receptor Human 9.0 pEC50 = 9 Binding
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
CHEMBL110489 8941 1 DRD2 D2 receptor Human 9.0 pEC50 = 9 Binding
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
242 451 110 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assayInverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.8b00435
34 451 110 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assayInverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.8b00435
60795 451 110 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assayInverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.8b00435
CHEMBL1112 451 110 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assayInverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.8b00435
DB01238 451 110 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assayInverse agonist activity at dopamine D2 receptor (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 20 mins by radiometric assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.8b00435
46882004 5346 0 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 321 4 0 2 3.5 O=C1N(CCN2CCCCCC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1077344 5346 0 DRD2 D2 receptor Human 9.0 pEC50 = 9 Functional
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
ChEMBL 321 4 0 2 3.5 O=C1N(CCN2CCCCCC2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
66559588 81319 0 DRD2 D2 receptor Human 9.0 pEC50 = 9 Binding
pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).
ChEMBL 459 7 1 4 5.2 O=c1ccc2ccc(OCCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
CHEMBL2165120 81319 0 DRD2 D2 receptor Human 9.0 pEC50 = 9 Binding
pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).
ChEMBL 459 7 1 4 5.2 O=c1ccc2ccc(OCCCCN3CCCN(c4cccc(Cl)c4Cl)CC3)cc2[nH]1 nan
44554474 105564 0 DRD2 D2 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099227 105564 0 DRD2 D2 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139043 105564 0 DRD2 D2 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
127046922 138918 0 DRD2 D2 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 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 138918 0 DRD2 D2 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 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
681 1368 56 DRD2 D2 receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
940 1368 56 DRD2 D2 receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
947 1368 56 DRD2 D2 receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
CHEMBL59 1368 56 DRD2 D2 receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
DB00988 1368 56 DRD2 D2 receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
681 1368 56 DRD2 D2 receptor Rat 9.0 pEC50 = 9.0 Binding
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
940 1368 56 DRD2 D2 receptor Rat 9.0 pEC50 = 9.0 Binding
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
947 1368 56 DRD2 D2 receptor Rat 9.0 pEC50 = 9.0 Binding
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
CHEMBL59 1368 56 DRD2 D2 receptor Rat 9.0 pEC50 = 9.0 Binding
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
DB00988 1368 56 DRD2 D2 receptor Rat 9.0 pEC50 = 9.0 Binding
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 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
167715 2702 11 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2702 11 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2702 11 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
167715 2702 11 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2702 11 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2702 11 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
2 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.6b01857
54562 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.6b01857
CHEMBL240773 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.6b01857
2 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.6b01857
54562 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.6b01857
CHEMBL240773 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.6b01857
2 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 ADMET
Agonist activity at recombinant human D2 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D2 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00412
54562 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 ADMET
Agonist activity at recombinant human D2 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D2 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00412
CHEMBL240773 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 ADMET
Agonist activity at recombinant human D2 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D2 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00412
137651936 156575 0 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assayAgonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 156575 0 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assayAgonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
2 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
54562 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
CHEMBL240773 3062 14 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
10086348 7788 0 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1021/jm950721m
CHEMBL109101 7788 0 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1021/jm950721m
2470 3432 34 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Functional
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 nan
3300 3432 34 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Functional
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 nan
5265 3432 34 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Functional
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 nan
99 3432 34 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Functional
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 nan
CHEMBL267930 3432 34 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Functional
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 nan
122177645 120444 0 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence 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 120444 0 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
71528204 86301 0 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Partial agonist activity at human D2 receptor transfected in HTLA cells measured after overnight incubation by luminescence counter analysisPartial agonist activity at human D2 receptor transfected in HTLA cells measured after overnight incubation by luminescence counter analysis
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323579 86301 0 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Partial agonist activity at human D2 receptor transfected in HTLA cells measured after overnight incubation by luminescence counter analysisPartial agonist activity at human D2 receptor transfected in HTLA cells measured after overnight incubation by luminescence counter analysis
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
90645297 111797 0 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 377 8 1 5 3.5 COc1ccccc1N1CCN(CCCCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
CHEMBL3299096 111797 0 DRD2 D2 receptor Human 8.9 pEC50 = 8.9 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 377 8 1 5 3.5 COc1ccccc1N1CCN(CCCCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
90645297 111797 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 377 8 1 5 3.5 COc1ccccc1N1CCN(CCCCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
CHEMBL3299096 111797 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
ChEMBL 377 8 1 5 3.5 COc1ccccc1N1CCN(CCCCCNC(=O)OC(C)(C)C)CC1 10.1021/jm500457x
137638973 156060 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assayAgonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071868 156060 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assayAgonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137655451 158029 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4094869 158029 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
25072633 158397 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 158397 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
44554982 103547 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099230 103547 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
56597227 153005 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 437 7 1 6 3.3 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)cc2N1 nan
CHEMBL3982360 153005 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
ChEMBL 437 7 1 6 3.3 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCCO5)CC3)cc2N1 nan
24754400 153795 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 423 8 1 5 3.8 CCCN(CCN1CCN(c2ccccc2OC)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
CHEMBL399164 153795 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 423 8 1 5 3.8 CCCN(CCN1CCN(c2ccccc2OC)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
228 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
76321556 105657 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 105657 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 105657 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assayAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by LANCE assay
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
56593482 3695 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
7650 3695 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
CHEMBL2165119 3695 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
2 3062 14 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
54562 3062 14 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
CHEMBL240773 3062 14 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
228 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
45140376 194243 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm901618d
CHEMBL599635 194243 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm901618d
137659990 158406 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assayAgonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4098859 158406 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assayAgonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assay
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137657153 158731 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4102616 158731 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137655451 158029 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4094869 158029 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
71459659 83185 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 534 16 2 4 7.7 CCCN(CCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
CHEMBL2206264 83185 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 534 16 2 4 7.7 CCCN(CCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
44554818 103551 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099234 103551 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
11761412 116206 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporationAgonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporation
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
CHEMBL338606 116206 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporationAgonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporation
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
228 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1039/C3MD00154G
33 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1039/C3MD00154G
6005 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1039/C3MD00154G
CHEMBL53 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1039/C3MD00154G
DB00714 425 20 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1039/C3MD00154G
119570 2967 79 DRD2 D2 receptor Rat 8.8 pEC50 = 8.8 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 2967 79 DRD2 D2 receptor Rat 8.8 pEC50 = 8.8 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 2967 79 DRD2 D2 receptor Rat 8.8 pEC50 = 8.8 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 2967 79 DRD2 D2 receptor Rat 8.8 pEC50 = 8.8 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 2967 79 DRD2 D2 receptor Rat 8.8 pEC50 = 8.8 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
10827222 6726 1 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
CHEMBL108463 6726 1 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Binding
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
11983282 138149 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 138149 0 DRD2 D2 receptor Human 8.8 pEC50 = 8.8 Functional
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
25093832 155071 0 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155071 0 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
228 425 20 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 425 20 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 425 20 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 425 20 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 425 20 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
2 3062 14 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assayAgonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.8b00671
54562 3062 14 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assayAgonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.8b00671
CHEMBL240773 3062 14 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assayAgonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.8b00671
228 425 20 DRD2 D2 receptor Rat 8.7 pEC50 = 8.7 Binding
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
33 425 20 DRD2 D2 receptor Rat 8.7 pEC50 = 8.7 Binding
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
6005 425 20 DRD2 D2 receptor Rat 8.7 pEC50 = 8.7 Binding
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL53 425 20 DRD2 D2 receptor Rat 8.7 pEC50 = 8.7 Binding
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
DB00714 425 20 DRD2 D2 receptor Rat 8.7 pEC50 = 8.7 Binding
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 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
2 3062 14 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
54562 3062 14 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
CHEMBL240773 3062 14 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
56597940 153149 0 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 450 7 2 6 2.9 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCC(=O)N5)CC3)cc2N1 nan
CHEMBL3983588 153149 0 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
ChEMBL 450 7 2 6 2.9 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4OCC(=O)N5)CC3)cc2N1 nan
2 3062 14 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
54562 3062 14 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
CHEMBL240773 3062 14 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assayPartial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00508
11957566 178 18 DRD2 D2 receptor Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1007/s00044-004-0006-x
1219 178 18 DRD2 D2 receptor Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1007/s00044-004-0006-x
3296 178 18 DRD2 D2 receptor Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1007/s00044-004-0006-x
950 178 18 DRD2 D2 receptor Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1007/s00044-004-0006-x
CHEMBL285755 178 18 DRD2 D2 receptor Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1007/s00044-004-0006-x
25072633 158397 0 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 158397 0 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assayAgonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4526364 172473 0 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 ADMET
Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assayPartial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene 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
183812 199295 15 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assayAgonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assay
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1021/ml4005232
CHEMBL82663 199295 15 DRD2 D2 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assayAgonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assay
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1021/ml4005232
228 425 20 DRD2 D2 receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 425 20 DRD2 D2 receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 425 20 DRD2 D2 receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 425 20 DRD2 D2 receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 425 20 DRD2 D2 receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
66559778 81322 0 DRD2 D2 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 423 9 1 5 4.0 CCOc1cccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c1 10.1021/jm300603y
CHEMBL2165123 81322 0 DRD2 D2 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
ChEMBL 423 9 1 5 4.0 CCOc1cccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c1 10.1021/jm300603y
121418538 170753 0 DRD2 D2 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at dopamine D2long receptor (unknown origin) assessed as increased in cAMP accumulationAgonist activity at dopamine D2long receptor (unknown origin) assessed as increased in cAMP accumulation
ChEMBL 345 6 0 3 4.7 CC1(Oc2ccc(Cl)cc2)CCN(CCOc2ccccc2)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL4465147 170753 0 DRD2 D2 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at dopamine D2long receptor (unknown origin) assessed as increased in cAMP accumulationAgonist activity at dopamine D2long receptor (unknown origin) assessed as increased in cAMP accumulation
ChEMBL 345 6 0 3 4.7 CC1(Oc2ccc(Cl)cc2)CCN(CCOc2ccccc2)CC1 10.1021/acs.jmedchem.8b00435
76336623 105387 0 DRD2 D2 receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
ChEMBL 324 4 2 4 2.9 CN1CCc2cccc3c2[C@H]1Cc1ccc(OCCCN)c(O)c1-3 10.1039/C3MD00154G