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Assay Detail

CHEMBL672699

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

Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical antipsychotics.
Raviña E, Negreira J, Cid J, Masaguer CF, Rosa E, Rivas ME, Fontenla JA, Loza MI, Tristán H, Cadavid MI, Sanz F, Lozoya E, Carotti A, Carrieri A.
J Med Chem (1999) 42 : 2774 -2797
PubMed 10425088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.20 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL539544 1 6.89
CHEMBL541842 1 6.87
CHEMBL54 HALOPERIDOL 4.0 1 6.80
CHEMBL42 CLOZAPINE 4.0 1 6.77
CHEMBL543613 1 6.53
CHEMBL308480 1 6.49
CHEMBL310734 1 6.42
CHEMBL544319 1 6.37
CHEMBL558817 1 6.25
CHEMBL95098 1 5.88
CHEMBL96781 1 5.87
CHEMBL542428 1 5.87
CHEMBL310153 1 5.87
CHEMBL87717 1 5.55
CHEMBL545488 1 5.51
CHEMBL540822 1 5.27
CHEMBL544318 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL539544 Ki = 128.82 nM 6.89
CHEMBL541842 Ki = 134.9 nM 6.87
CHEMBL54 HALOPERIDOL Ki = 158.49 nM 6.80
CHEMBL42 CLOZAPINE Ki = 169.82 nM 6.77
CHEMBL543613 Ki = 295.12 nM 6.53
CHEMBL308480 Ki = 323.59 nM 6.49
CHEMBL310734 Ki = 380.19 nM 6.42
CHEMBL544319 Ki = 426.58 nM 6.37
CHEMBL558817 Ki = 562.34 nM 6.25
CHEMBL95098 Ki = 1318.26 nM 5.88
CHEMBL96781 Ki = 1348.96 nM 5.87
CHEMBL542428 Ki = 1348.96 nM 5.87
CHEMBL310153 Ki = 1348.96 nM 5.87
CHEMBL87717 Ki = 2818.38 nM 5.55
CHEMBL545488 Ki = 3090.3 nM 5.51
CHEMBL540822 Ki = 5370.32 nM 5.27
CHEMBL544318 Ki < 10000.0 nM -