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Assay Detail

CHEMBL672210

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Binding
Affinity towards Dopamine receptor D2
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

CoMFA-based prediction of agonist affinities at recombinant D1 vs D2 dopamine receptors.
Wilcox RE, Tseng T, Brusniak MY, Ginsburg B, Pearlman RS, Teeter M, DuRand C, Starr S, Neve KA.
J Med Chem (1998) 41 : 4385 -4399
PubMed 9784114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.45 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 1 9.10
CHEMBL609151 1 8.70
CHEMBL612083 1 7.70
CHEMBL531 PERGOLIDE 4.0 1 7.30
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE 1 7.30
CHEMBL611801 1 6.47
CHEMBL34095 1 6.46
CHEMBL317741 1 6.29
CHEMBL588 FENOLDOPAM 4.0 1 6.09
CHEMBL25856 DIHYDREXIDINE 2.0 1 5.77
CHEMBL240773 QUINPIROLE 2.0 1 5.59
CHEMBL59 DOPAMINE 4.0 1 5.10
CHEMBL1160787 1 5.10
CHEMBL24077 (R)-SKF-38393 1 5.02
CHEMBL145584 1 4.70
CHEMBL11608 TYRAMINE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Ki = 0.8 nM 9.10
CHEMBL609151 Ki = 2.0 nM 8.70
CHEMBL612083 Ki = 20.0 nM 7.70
CHEMBL531 PERGOLIDE Ki = 50.0 nM 7.30
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE Ki = 50.0 nM 7.30
CHEMBL611801 Ki = 340.0 nM 6.47
CHEMBL34095 Ki = 350.0 nM 6.46
CHEMBL317741 Ki = 510.0 nM 6.29
CHEMBL588 FENOLDOPAM Ki = 810.0 nM 6.09
CHEMBL25856 DIHYDREXIDINE Ki = 1700.0 nM 5.77
CHEMBL240773 QUINPIROLE Ki = 2570.0 nM 5.59
CHEMBL59 DOPAMINE Ki = 7940.0 nM 5.10
CHEMBL1160787 Ki = 8000.0 nM 5.10
CHEMBL24077 (R)-SKF-38393 Ki = 9550.0 nM 5.02
CHEMBL145584 Ki = 20000.0 nM 4.70
CHEMBL11608 TYRAMINE Ki = 160000.0 nM -