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Assay Detail

CHEMBL673094

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

Binding
In vitro binding affinity against Dopamine D2 receptor 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(2) dopamine receptor (CHEMBL339)
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 6.37 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.06
CHEMBL71 CHLORPROMAZINE 4.0 1 8.70
CHEMBL304902 CLOTHIAPINE 2.0 1 8.36
CHEMBL415300 ISOCLOZAPINE 1 7.89
CHEMBL67284 ISOCLOTHIAPINE 1 7.52
CHEMBL42 CLOZAPINE 4.0 1 7.35
CHEMBL63576 1 6.93
CHEMBL63756 FLUPERLAPINE 2.0 1 6.88
CHEMBL63590 1 6.53
CHEMBL67298 1 6.36
CHEMBL63329 1 6.28
CHEMBL304493 1 5.99
CHEMBL63347 1 5.81
CHEMBL67355 1 5.71
CHEMBL303173 1 5.44
CHEMBL66730 1 5.40
CHEMBL65768 1 4.62
CHEMBL63390 1 4.57
CHEMBL303435 1 4.00
CHEMBL292738 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.88 nM 9.06
CHEMBL71 CHLORPROMAZINE Ki = 2.01 nM 8.70
CHEMBL304902 CLOTHIAPINE Ki = 4.4 nM 8.36
CHEMBL415300 ISOCLOZAPINE Ki = 13.0 nM 7.89
CHEMBL67284 ISOCLOTHIAPINE Ki = 30.0 nM 7.52
CHEMBL42 CLOZAPINE Ki = 45.0 nM 7.35
CHEMBL63576 Ki = 118.0 nM 6.93
CHEMBL63756 FLUPERLAPINE Ki = 133.0 nM 6.88
CHEMBL63590 Ki = 297.0 nM 6.53
CHEMBL67298 Ki = 442.0 nM 6.36
CHEMBL63329 Ki = 530.0 nM 6.28
CHEMBL304493 Ki = 1020.0 nM 5.99
CHEMBL63347 Ki = 1550.0 nM 5.81
CHEMBL67355 Ki = 1966.0 nM 5.71
CHEMBL303173 Ki = 3652.0 nM 5.44
CHEMBL66730 Ki = 3970.0 nM 5.40
CHEMBL65768 Ki = 23900.0 nM 4.62
CHEMBL63390 Ki = 27100.0 nM 4.57
CHEMBL303435 Ki = 100000.0 nM 4.00
CHEMBL292738 Ki = 100000.0 nM 4.00