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Assay Detail

CHEMBL931094

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Functional
Antagonist activity at dopamine D3 receptor by GTPgammaS binding assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systems.
Micheli F, Bonanomi G, Braggio S, Capelli AM, Damiani F, Di Fabio R, Donati D, Gentile G, Hamprecht D, Perini O, Petrone M, Tedesco G, Terreni S, Worby A, Heidbreder C.
Bioorg Med Chem Lett (2008) 18 : 908 -912
PubMed 18178090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 7.89 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL402215 1 9.10
CHEMBL437792 1 9.10
CHEMBL271034 1 9.00
CHEMBL244946 1 8.80
CHEMBL271449 1 8.80
CHEMBL256488 1 8.70
CHEMBL256442 1 8.70
CHEMBL272775 1 8.60
CHEMBL270387 1 8.50
CHEMBL85606 1 8.40
CHEMBL272150 1 8.40
CHEMBL404404 1 8.40
CHEMBL402853 1 8.40
CHEMBL404363 1 8.30
CHEMBL270376 1 8.30
CHEMBL270602 1 8.20
CHEMBL403804 1 8.20
CHEMBL442456 1 8.10
CHEMBL427836 1 7.90
CHEMBL255158 1 7.80
CHEMBL256659 1 7.70
CHEMBL272297 1 7.60
CHEMBL271909 1 7.50
CHEMBL272511 1 7.20
CHEMBL402422 1 7.00
CHEMBL257717 1 6.80
CHEMBL271729 1 6.80
CHEMBL272588 1 6.70
CHEMBL411293 1 6.60
CHEMBL403815 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL402215 Ki = 0.7943 nM 9.10
CHEMBL437792 Ki = 0.7943 nM 9.10
CHEMBL271034 Ki = 1.0 nM 9.00
CHEMBL244946 Ki = 1.585 nM 8.80
CHEMBL271449 Ki = 1.585 nM 8.80
CHEMBL256488 Ki = 1.995 nM 8.70
CHEMBL256442 Ki = 1.995 nM 8.70
CHEMBL272775 Ki = 2.512 nM 8.60
CHEMBL270387 Ki = 3.162 nM 8.50
CHEMBL272150 Ki = 3.981 nM 8.40
CHEMBL402853 Ki = 3.981 nM 8.40
CHEMBL404404 Ki = 3.981 nM 8.40
CHEMBL85606 Ki = 3.981 nM 8.40
CHEMBL404363 Ki = 5.012 nM 8.30
CHEMBL270376 Ki = 5.012 nM 8.30
CHEMBL270602 Ki = 6.31 nM 8.20
CHEMBL403804 Ki = 6.31 nM 8.20
CHEMBL442456 Ki = 7.943 nM 8.10
CHEMBL427836 Ki = 12.59 nM 7.90
CHEMBL255158 Ki = 15.85 nM 7.80
CHEMBL256659 Ki = 19.95 nM 7.70
CHEMBL272297 Ki = 25.12 nM 7.60
CHEMBL271909 Ki = 31.62 nM 7.50
CHEMBL272511 Ki = 63.1 nM 7.20
CHEMBL402422 Ki = 100.0 nM 7.00
CHEMBL257717 Ki = 158.49 nM 6.80
CHEMBL271729 Ki = 158.49 nM 6.80
CHEMBL272588 Ki = 199.53 nM 6.70
CHEMBL411293 Ki = 251.19 nM 6.60
CHEMBL403815 Ki = 316.23 nM 6.50
CHEMBL271511 Ki = 398.11 nM 6.40
CHEMBL271702 Ki = 794.33 nM 6.10
CHEMBL256658 Ki < 251.19 nM -
CHEMBL257716 Ki < 251.19 nM -
CHEMBL255220 Ki < 125.89 nM -
CHEMBL406678 Ki < 251.19 nM -