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Assay Detail

CHEMBL672573

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Binding
Binding affinity for human Dopamine receptor D2 (short) by [3H]- spiperone displacement.
19
Total Activities
19
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

Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.
Bettinetti L, Schlotter K, Hübner H, Gmeiner P.
J Med Chem (2002) 45 : 4594 -4597
PubMed 12361386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.96 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140612 1 8.41
CHEMBL139600 1 7.60
CHEMBL141419 1 7.41
CHEMBL337531 1 7.32
CHEMBL424294 1 7.28
CHEMBL423735 1 7.19
CHEMBL140968 1 7.12
CHEMBL139926 1 7.10
CHEMBL336930 1 7.08
CHEMBL124444 1 7.08
CHEMBL344677 1 7.01
CHEMBL342060 1 6.92
CHEMBL141845 1 6.85
CHEMBL143352 1 6.75
CHEMBL25236 BP-897 1 6.68
CHEMBL142020 1 6.51
CHEMBL139722 1 6.32
CHEMBL357684 1 6.01
CHEMBL59725 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140612 Ki = 3.9 nM 8.41
CHEMBL139600 Ki = 25.0 nM 7.60
CHEMBL141419 Ki = 39.0 nM 7.41
CHEMBL337531 Ki = 48.0 nM 7.32
CHEMBL424294 Ki = 52.0 nM 7.28
CHEMBL423735 Ki = 65.0 nM 7.19
CHEMBL140968 Ki = 76.0 nM 7.12
CHEMBL139926 Ki = 80.0 nM 7.10
CHEMBL336930 Ki = 84.0 nM 7.08
CHEMBL124444 Ki = 84.0 nM 7.08
CHEMBL344677 Ki = 98.0 nM 7.01
CHEMBL342060 Ki = 120.0 nM 6.92
CHEMBL141845 Ki = 140.0 nM 6.85
CHEMBL143352 Ki = 180.0 nM 6.75
CHEMBL25236 BP-897 Ki = 210.0 nM 6.68
CHEMBL142020 Ki = 310.0 nM 6.51
CHEMBL139722 Ki = 480.0 nM 6.32
CHEMBL357684 Ki = 970.0 nM 6.01
CHEMBL59725 Ki = 2600.0 nM 5.58