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Assay Detail

CHEMBL673121

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

Binding
Ability to displace [125I]-sulpiride from human Dopamine receptor D3, expressed in CHO cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-[(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl)methyl]-1H-pyrroles with high affinity and selectivity for the dopamine D3 receptor
Bolton D, Boyfield I, Coldwell MC, Hadley MS, Johns A, Johnson CN, Markwell RE, Nash DJ, Riley GJ, Scott EE, Smith SA, Stemp G, Wadsworth HJ, Watts EA
Bioorg Med Chem Lett (1997) 7 : 485 -488
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.29 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1788258 1 9.10
CHEMBL22156 1 8.90
CHEMBL423198 1 8.80
CHEMBL280490 1 8.70
CHEMBL356526 1 8.70
CHEMBL145141 1 8.40
CHEMBL2093000 1 8.40
CHEMBL1788252 1 8.40
CHEMBL344531 1 8.30
CHEMBL145545 1 8.20
CHEMBL144055 1 8.20
CHEMBL145408 1 8.20
CHEMBL433552 1 8.00
CHEMBL2093001 1 7.80
CHEMBL144600 1 7.40
CHEMBL144141 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1788258 Ki = 0.7943 nM 9.10
CHEMBL22156 Ki = 1.259 nM 8.90
CHEMBL423198 Ki = 1.585 nM 8.80
CHEMBL280490 Ki = 1.995 nM 8.70
CHEMBL356526 Ki = 1.995 nM 8.70
CHEMBL145141 Ki = 3.981 nM 8.40
CHEMBL2093000 Ki = 3.981 nM 8.40
CHEMBL1788252 Ki = 3.981 nM 8.40
CHEMBL344531 Ki = 5.012 nM 8.30
CHEMBL145545 Ki = 6.31 nM 8.20
CHEMBL144055 Ki = 6.31 nM 8.20
CHEMBL145408 Ki = 6.31 nM 8.20
CHEMBL433552 Ki = 10.0 nM 8.00
CHEMBL2093001 Ki = 15.85 nM 7.80
CHEMBL144600 Ki = 39.81 nM 7.40
CHEMBL144141 Ki = 79.43 nM 7.10