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Assay Detail

CHEMBL617169

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

Binding
In vitro binding affinity against rat 5-hydroxytryptamine 2 receptor.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
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 7.27 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304902 CLOTHIAPINE 2.0 1 9.22
CHEMBL415300 ISOCLOZAPINE 1 8.74
CHEMBL71 CHLORPROMAZINE 4.0 1 8.48
CHEMBL42 CLOZAPINE 4.0 1 8.42
CHEMBL63756 FLUPERLAPINE 2.0 1 8.42
CHEMBL67284 ISOCLOTHIAPINE 1 8.39
CHEMBL63576 1 8.21
CHEMBL54 HALOPERIDOL 4.0 1 7.63
CHEMBL67298 1 7.54
CHEMBL304493 1 7.32
CHEMBL63329 1 7.03
CHEMBL63590 1 6.99
CHEMBL67355 1 6.99
CHEMBL303173 1 6.91
CHEMBL63347 1 6.91
CHEMBL66730 1 6.08
CHEMBL303435 1 5.73
CHEMBL65768 1 5.69
CHEMBL63390 1 5.54
CHEMBL292738 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304902 CLOTHIAPINE Ki = 0.6 nM 9.22
CHEMBL415300 ISOCLOZAPINE Ki = 1.8 nM 8.74
CHEMBL71 CHLORPROMAZINE Ki = 3.3 nM 8.48
CHEMBL42 CLOZAPINE Ki = 3.8 nM 8.42
CHEMBL63756 FLUPERLAPINE Ki = 3.8 nM 8.42
CHEMBL67284 ISOCLOTHIAPINE Ki = 4.1 nM 8.39
CHEMBL63576 Ki = 6.2 nM 8.21
CHEMBL54 HALOPERIDOL Ki = 23.4 nM 7.63
CHEMBL67298 Ki = 29.0 nM 7.54
CHEMBL304493 Ki = 48.0 nM 7.32
CHEMBL63329 Ki = 94.0 nM 7.03
CHEMBL63590 Ki = 103.0 nM 6.99
CHEMBL67355 Ki = 103.0 nM 6.99
CHEMBL303173 Ki = 124.0 nM 6.91
CHEMBL63347 Ki = 124.0 nM 6.91
CHEMBL66730 Ki = 837.0 nM 6.08
CHEMBL303435 Ki = 1870.0 nM 5.73
CHEMBL65768 Ki = 2053.0 nM 5.69
CHEMBL63390 Ki = 2900.0 nM 5.54
CHEMBL292738 Ki = 7120.0 nM 5.15