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Assay Detail

CHEMBL671910

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 receptor D1 in rat striatal membrane.
10
Total Activities
10
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 10 5.88 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL554199 1 6.90
CHEMBL95112 1 6.49
CHEMBL87026 1 5.89
CHEMBL544091 1 5.86
CHEMBL92145 1 5.83
CHEMBL87943 1 5.81
CHEMBL545727 1 5.81
CHEMBL92673 1 5.60
CHEMBL542181 1 5.43
CHEMBL544089 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL554199 Ki = 125.89 nM 6.90
CHEMBL95112 Ki = 323.59 nM 6.49
CHEMBL87026 Ki = 1288.25 nM 5.89
CHEMBL544091 Ki = 1380.38 nM 5.86
CHEMBL92145 Ki = 1479.11 nM 5.83
CHEMBL87943 Ki = 1548.82 nM 5.81
CHEMBL545727 Ki = 1548.82 nM 5.81
CHEMBL92673 Ki = 2511.89 nM 5.60
CHEMBL542181 Ki = 3715.35 nM 5.43
CHEMBL544089 Ki = 7079.46 nM 5.15