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Assay Detail

CHEMBL3383111

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Binding
Inhibition of human dopamine D3 receptor
16
Total Activities
9
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity.
Berry CB, Bubser M, Jones CK, Hayes JP, Wepy JA, Locuson CW, Daniels JS, Lindsley CW, Hopkins CR.
ACS Med Chem Lett (2014) 5 : 1060 -1064
PubMed 25221667 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.23 5.56
IC50 7 4.76 5.09
INH 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3335538 2 5.56
CHEMBL3335539 2 5.56
CHEMBL3335554 2 5.56
CHEMBL3335555 2 5.56
CHEMBL3335535 2 4.97
CHEMBL3335537 2 4.80
CHEMBL3335536 2 4.59
CHEMBL3335556 1 -
CHEMBL3335540 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3335538 Ki = 2770.0 nM 5.56
CHEMBL3335539 Ki = 2770.0 nM 5.56
CHEMBL3335554 Ki = 2770.0 nM 5.56
CHEMBL3335555 Ki = 2770.0 nM 5.56
CHEMBL3335538 IC50 = 8170.0 nM 5.09
CHEMBL3335539 IC50 = 8170.0 nM 5.09
CHEMBL3335554 IC50 = 8170.0 nM 5.09
CHEMBL3335555 IC50 = 8170.0 nM 5.09
CHEMBL3335535 Ki = 10800.0 nM 4.97
CHEMBL3335537 Ki = 15700.0 nM 4.80
CHEMBL3335536 Ki = 25900.0 nM 4.59
CHEMBL3335535 IC50 = 31800.0 nM 4.50
CHEMBL3335537 IC50 = 46200.0 nM 4.33
CHEMBL3335536 IC50 = 76400.0 nM 4.12
CHEMBL3335556 INH > 20.0 uM -
CHEMBL3335540 INH > 20.0 uM -