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Assay Detail

CHEMBL1909140

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

DrugMatrix in vitro pharmacology data
Scott S. Auerbach, DrugMatrix¨ and ToxFX¨ Coordinator National Toxicology Program

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 871 6.60 8.83
Ki 871 7.08 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE 2 9.31
CHEMBL493 BROMOCRIPTINE 4.0 2 9.28
CHEMBL726 FLUPHENAZINE 4.0 2 9.27
CHEMBL1403281 ERGOCRYPTINE 2 9.19
CHEMBL1108 DROPERIDOL 4.0 2 9.10
CHEMBL219916 DOMPERIDONE 3.0 2 9.05
CHEMBL157138 LISURIDE 3.0 2 9.02
CHEMBL1909072 PIPAMAZINE 4.0 2 8.87
CHEMBL442 ERGOTAMINE 4.0 2 8.84
CHEMBL1385840 ERGOCORNINE 2 8.78
CHEMBL54 HALOPERIDOL 4.0 2 8.66
CHEMBL1732 DIHYDROERGOTAMINE 4.0 2 8.53
CHEMBL728 PROCHLORPERAZINE 4.0 2 8.44
CHEMBL85 RISPERIDONE 4.0 2 8.18
CHEMBL479 THIORIDAZINE 4.0 2 7.92
CHEMBL71 CHLORPROMAZINE 4.0 2 7.75
CHEMBL19215 METERGOLINE 2.0 2 7.68
CHEMBL531 PERGOLIDE 4.0 2 7.43
CHEMBL715 OLANZAPINE 4.0 2 7.41
CHEMBL86 METOCLOPRAMIDE 4.0 2 7.38
CHEMBL267044 LEVOSULPIRIDE 2.0 2 7.37
CHEMBL1626 CLEMASTINE 4.0 2 7.35
CHEMBL723 CARVEDILOL 4.0 2 7.31
CHEMBL1221512 2 7.28
CHEMBL516 CYPROHEPTADINE 4.0 2 7.26
CHEMBL1113 AMOXAPINE 4.0 2 7.17
CHEMBL26 SULPIRIDE 3.0 2 7.17
CHEMBL49 BUSPIRONE 4.0 2 6.97
CHEMBL30008 FLUNARIZINE 2.0 2 6.93
CHEMBL42 CLOZAPINE 4.0 2 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE Ki = 0.491 nM 9.31
CHEMBL493 BROMOCRIPTINE Ki = 0.527 nM 9.28
CHEMBL726 FLUPHENAZINE Ki = 0.539 nM 9.27
CHEMBL1403281 ERGOCRYPTINE Ki = 0.65 nM 9.19
CHEMBL1108 DROPERIDOL Ki = 0.802 nM 9.10
CHEMBL219916 DOMPERIDONE Ki = 0.882 nM 9.05
CHEMBL157138 LISURIDE Ki = 0.953 nM 9.02
CHEMBL1909072 PIPAMAZINE Ki = 1.35 nM 8.87
CHEMBL442 ERGOTAMINE Ki = 1.433 nM 8.84
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE IC50 = 1.474 nM 8.83
CHEMBL493 BROMOCRIPTINE IC50 = 1.582 nM 8.80
CHEMBL726 FLUPHENAZINE IC50 = 1.616 nM 8.79
CHEMBL1385840 ERGOCORNINE Ki = 1.677 nM 8.78
CHEMBL1403281 ERGOCRYPTINE IC50 = 1.95 nM 8.71
CHEMBL54 HALOPERIDOL Ki = 2.197 nM 8.66
CHEMBL1108 DROPERIDOL IC50 = 2.407 nM 8.62
CHEMBL219916 DOMPERIDONE IC50 = 2.647 nM 8.58
CHEMBL157138 LISURIDE IC50 = 2.86 nM 8.54
CHEMBL1732 DIHYDROERGOTAMINE Ki = 2.96 nM 8.53
CHEMBL728 PROCHLORPERAZINE Ki = 3.608 nM 8.44
CHEMBL1909072 PIPAMAZINE IC50 = 4.05 nM 8.39
CHEMBL442 ERGOTAMINE IC50 = 4.3 nM 8.37
CHEMBL1385840 ERGOCORNINE IC50 = 5.032 nM 8.30
CHEMBL54 HALOPERIDOL IC50 = 6.592 nM 8.18
CHEMBL85 RISPERIDONE Ki = 6.545 nM 8.18
CHEMBL1732 DIHYDROERGOTAMINE IC50 = 8.88 nM 8.05
CHEMBL728 PROCHLORPERAZINE IC50 = 11.0 nM 7.96
CHEMBL479 THIORIDAZINE Ki = 12.0 nM 7.92
CHEMBL71 CHLORPROMAZINE Ki = 18.0 nM 7.75
CHEMBL85 RISPERIDONE IC50 = 20.0 nM 7.70
CHEMBL19215 METERGOLINE Ki = 21.0 nM 7.68
CHEMBL479 THIORIDAZINE IC50 = 35.0 nM 7.46
CHEMBL531 PERGOLIDE Ki = 37.0 nM 7.43
CHEMBL715 OLANZAPINE Ki = 39.0 nM 7.41
CHEMBL86 METOCLOPRAMIDE Ki = 42.0 nM 7.38
CHEMBL267044 LEVOSULPIRIDE Ki = 43.0 nM 7.37
CHEMBL1626 CLEMASTINE Ki = 45.0 nM 7.35
CHEMBL723 CARVEDILOL Ki = 49.0 nM 7.31
CHEMBL1221512 Ki = 52.0 nM 7.28
CHEMBL71 CHLORPROMAZINE IC50 = 54.0 nM 7.27
CHEMBL516 CYPROHEPTADINE Ki = 55.0 nM 7.26
CHEMBL19215 METERGOLINE IC50 = 63.0 nM 7.20
CHEMBL26 SULPIRIDE Ki = 68.0 nM 7.17
CHEMBL1113 AMOXAPINE Ki = 67.0 nM 7.17
CHEMBL49 BUSPIRONE Ki = 108.0 nM 6.97
CHEMBL531 PERGOLIDE IC50 = 111.0 nM 6.96
CHEMBL715 OLANZAPINE IC50 = 118.0 nM 6.93
CHEMBL30008 FLUNARIZINE Ki = 117.0 nM 6.93
CHEMBL86 METOCLOPRAMIDE IC50 = 127.0 nM 6.90
CHEMBL42 CLOZAPINE Ki = 129.0 nM 6.89