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Assay Detail

CHEMBL674347

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

Binding
Binding affinity towards human Dopamine receptor D2 expressed in CHO cells by [125I]iodosulpiride displacement.
17
Total Activities
17
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(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 2,5-disubstituted-1H-pyrroles with high affinity for the dopamine D3 receptor
Bolton D, Boyfield I, Coldwell MC, Hadley MS, Healy MA, Johnson CN, Markwell RE, Nash DJ, Riley GJ, Stemp G, Wadsworth HJ
Bioorg Med Chem Lett (1996) 6 : 1233 -1236
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.23 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21967 1 9.10
CHEMBL277945 SULTOPRIDE 2.0 1 8.20
CHEMBL280177 1 8.10
CHEMBL20763 1 8.10
CHEMBL281177 1 7.90
CHEMBL280961 1 7.80
CHEMBL277631 1 7.60
CHEMBL22156 1 7.40
CHEMBL22022 1 7.10
CHEMBL21118 1 6.80
CHEMBL279039 1 6.80
CHEMBL21280 1 6.60
CHEMBL20395 1 6.50
CHEMBL20785 1 6.50
CHEMBL277684 1 6.50
CHEMBL282287 1 6.40
CHEMBL20407 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21967 Ki = 0.7943 nM 9.10
CHEMBL277945 SULTOPRIDE Ki = 6.31 nM 8.20
CHEMBL280177 Ki = 7.943 nM 8.10
CHEMBL20763 Ki = 7.943 nM 8.10
CHEMBL281177 Ki = 12.59 nM 7.90
CHEMBL280961 Ki = 15.85 nM 7.80
CHEMBL277631 Ki = 25.12 nM 7.60
CHEMBL22156 Ki = 39.81 nM 7.40
CHEMBL22022 Ki = 79.43 nM 7.10
CHEMBL21118 Ki = 158.49 nM 6.80
CHEMBL279039 Ki = 158.49 nM 6.80
CHEMBL21280 Ki = 251.19 nM 6.60
CHEMBL20395 Ki = 316.23 nM 6.50
CHEMBL20785 Ki = 316.23 nM 6.50
CHEMBL277684 Ki = 316.23 nM 6.50
CHEMBL282287 Ki = 398.11 nM 6.40
CHEMBL20407 Ki = 3162.28 nM 5.50