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Assay Detail

CHEMBL1909141

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

Binding
DRUGMATRIX: Dopamine D3 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(3) dopamine receptor (CHEMBL234)
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 6.55 9.76
Ki 871 6.99 10.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 2 10.23
CHEMBL493 BROMOCRIPTINE 4.0 2 9.70
CHEMBL1403281 ERGOCRYPTINE 2 9.70
CHEMBL726 FLUPHENAZINE 4.0 2 9.70
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE 2 9.11
CHEMBL1108 DROPERIDOL 4.0 2 9.03
CHEMBL1385840 ERGOCORNINE 2 9.01
CHEMBL442 ERGOTAMINE 4.0 2 8.83
CHEMBL1909072 PIPAMAZINE 4.0 2 8.80
CHEMBL1732 DIHYDROERGOTAMINE 4.0 2 8.74
CHEMBL531 PERGOLIDE 4.0 2 8.74
CHEMBL1626 CLEMASTINE 4.0 2 8.60
CHEMBL19215 METERGOLINE 2.0 2 8.58
CHEMBL479 THIORIDAZINE 4.0 2 8.47
CHEMBL71 CHLORPROMAZINE 4.0 2 8.38
CHEMBL728 PROCHLORPERAZINE 4.0 2 8.35
CHEMBL219916 DOMPERIDONE 3.0 2 8.21
CHEMBL54 HALOPERIDOL 4.0 2 8.16
CHEMBL85 RISPERIDONE 4.0 2 8.10
CHEMBL1909065 MADURAMICIN ACID 2.0 2 8.03
CHEMBL1221512 2 8.02
CHEMBL49 BUSPIRONE 4.0 2 7.82
CHEMBL516 CYPROHEPTADINE 4.0 2 7.80
CHEMBL715 OLANZAPINE 4.0 2 7.57
CHEMBL508338 THIMEROSAL 3.0 2 7.54
CHEMBL30008 FLUNARIZINE 2.0 2 7.48
CHEMBL305660 EBASTINE 4.0 2 7.38
CHEMBL267044 LEVOSULPIRIDE 2.0 2 7.38
CHEMBL1113 AMOXAPINE 4.0 2 7.34
CHEMBL415 CLOMIPRAMINE 4.0 2 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Ki = 0.059 nM 10.23
CHEMBL157138 LISURIDE IC50 = 0.173 nM 9.76
CHEMBL1403281 ERGOCRYPTINE Ki = 0.2 nM 9.70
CHEMBL726 FLUPHENAZINE Ki = 0.202 nM 9.70
CHEMBL493 BROMOCRIPTINE Ki = 0.202 nM 9.70
CHEMBL1403281 ERGOCRYPTINE IC50 = 0.589 nM 9.23
CHEMBL726 FLUPHENAZINE IC50 = 0.594 nM 9.23
CHEMBL493 BROMOCRIPTINE IC50 = 0.596 nM 9.22
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE Ki = 0.777 nM 9.11
CHEMBL1108 DROPERIDOL Ki = 0.939 nM 9.03
CHEMBL1385840 ERGOCORNINE Ki = 0.971 nM 9.01
CHEMBL442 ERGOTAMINE Ki = 1.464 nM 8.83
CHEMBL1909072 PIPAMAZINE Ki = 1.586 nM 8.80
CHEMBL1732 DIHYDROERGOTAMINE Ki = 1.812 nM 8.74
CHEMBL531 PERGOLIDE Ki = 1.832 nM 8.74
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE IC50 = 2.288 nM 8.64
CHEMBL1626 CLEMASTINE Ki = 2.491 nM 8.60
CHEMBL19215 METERGOLINE Ki = 2.611 nM 8.58
CHEMBL1108 DROPERIDOL IC50 = 2.765 nM 8.56
CHEMBL1385840 ERGOCORNINE IC50 = 2.86 nM 8.54
CHEMBL479 THIORIDAZINE Ki = 3.36 nM 8.47
CHEMBL71 CHLORPROMAZINE Ki = 4.205 nM 8.38
CHEMBL442 ERGOTAMINE IC50 = 4.311 nM 8.37
CHEMBL728 PROCHLORPERAZINE Ki = 4.454 nM 8.35
CHEMBL1909072 PIPAMAZINE IC50 = 4.671 nM 8.33
CHEMBL1732 DIHYDROERGOTAMINE IC50 = 5.336 nM 8.27
CHEMBL531 PERGOLIDE IC50 = 5.393 nM 8.27
CHEMBL219916 DOMPERIDONE Ki = 6.243 nM 8.21
CHEMBL54 HALOPERIDOL Ki = 6.842 nM 8.16
CHEMBL1626 CLEMASTINE IC50 = 7.335 nM 8.13
CHEMBL19215 METERGOLINE IC50 = 7.689 nM 8.11
CHEMBL85 RISPERIDONE Ki = 8.036 nM 8.10
CHEMBL1909065 MADURAMICIN ACID Ki = 9.336 nM 8.03
CHEMBL1221512 Ki = 9.635 nM 8.02
CHEMBL479 THIORIDAZINE IC50 = 9.892 nM 8.01
CHEMBL71 CHLORPROMAZINE IC50 = 12.0 nM 7.92
CHEMBL728 PROCHLORPERAZINE IC50 = 13.0 nM 7.89
CHEMBL49 BUSPIRONE Ki = 15.0 nM 7.82
CHEMBL516 CYPROHEPTADINE Ki = 16.0 nM 7.80
CHEMBL219916 DOMPERIDONE IC50 = 18.0 nM 7.75
CHEMBL54 HALOPERIDOL IC50 = 20.0 nM 7.70
CHEMBL85 RISPERIDONE IC50 = 24.0 nM 7.62
CHEMBL715 OLANZAPINE Ki = 27.0 nM 7.57
CHEMBL1909065 MADURAMICIN ACID IC50 = 27.0 nM 7.57
CHEMBL1221512 IC50 = 28.0 nM 7.55
CHEMBL508338 THIMEROSAL Ki = 29.0 nM 7.54
CHEMBL30008 FLUNARIZINE Ki = 33.0 nM 7.48
CHEMBL267044 LEVOSULPIRIDE Ki = 42.0 nM 7.38
CHEMBL305660 EBASTINE Ki = 41.3 nM 7.38
CHEMBL49 BUSPIRONE IC50 = 44.0 nM 7.36