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Assay Detail

CHEMBL670442

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

Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
Liégeois JF, Bruhwyler J, Damas J, Nguyen TP, Chleide EM, Mercier MG, Rogister FA, Delarge JE.
J Med Chem (1993) 36 : 2107 -2114
PubMed 8101877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.20 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304902 CLOTHIAPINE 2.0 1 7.85
CHEMBL415300 ISOCLOZAPINE 1 7.55
CHEMBL71 CHLORPROMAZINE 4.0 1 7.46
CHEMBL54 HALOPERIDOL 4.0 1 7.12
CHEMBL42 CLOZAPINE 4.0 1 6.94
CHEMBL63756 FLUPERLAPINE 2.0 1 6.85
CHEMBL304493 1 6.67
CHEMBL67284 ISOCLOTHIAPINE 1 6.62
CHEMBL67298 1 6.52
CHEMBL63329 1 6.40
CHEMBL63347 1 6.17
CHEMBL67355 1 6.14
CHEMBL63590 1 5.95
CHEMBL63576 1 5.67
CHEMBL303173 1 5.62
CHEMBL65768 1 5.52
CHEMBL63390 1 5.22
CHEMBL66730 1 4.87
CHEMBL292738 1 4.52
CHEMBL303435 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304902 CLOTHIAPINE Ki = 14.0 nM 7.85
CHEMBL415300 ISOCLOZAPINE Ki = 28.0 nM 7.55
CHEMBL71 CHLORPROMAZINE Ki = 35.0 nM 7.46
CHEMBL54 HALOPERIDOL Ki = 76.0 nM 7.12
CHEMBL42 CLOZAPINE Ki = 115.0 nM 6.94
CHEMBL63756 FLUPERLAPINE Ki = 141.0 nM 6.85
CHEMBL304493 Ki = 214.0 nM 6.67
CHEMBL67284 ISOCLOTHIAPINE Ki = 240.0 nM 6.62
CHEMBL67298 Ki = 302.0 nM 6.52
CHEMBL63329 Ki = 398.0 nM 6.40
CHEMBL63347 Ki = 677.0 nM 6.17
CHEMBL67355 Ki = 726.0 nM 6.14
CHEMBL63590 Ki = 1135.0 nM 5.95
CHEMBL63576 Ki = 2140.0 nM 5.67
CHEMBL303173 Ki = 2400.0 nM 5.62
CHEMBL65768 Ki = 3020.0 nM 5.52
CHEMBL63390 Ki = 6020.0 nM 5.22
CHEMBL66730 Ki = 13500.0 nM 4.87
CHEMBL292738 Ki = 30200.0 nM 4.52
CHEMBL303435 Ki = 47900.0 nM 4.32