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Assay Detail

CHEMBL748440

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

Binding
In vitro binding affinity against Muscarinic acetylcholine receptors in rat brain.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor (CHEMBL1907609)
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 6.64 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67284 ISOCLOTHIAPINE 1 8.25
CHEMBL415300 ISOCLOZAPINE 1 7.68
CHEMBL42 CLOZAPINE 4.0 1 7.60
CHEMBL63756 FLUPERLAPINE 2.0 1 7.60
CHEMBL63329 1 7.32
CHEMBL71 CHLORPROMAZINE 4.0 1 7.22
CHEMBL63576 1 7.19
CHEMBL304902 CLOTHIAPINE 2.0 1 6.87
CHEMBL63390 1 6.76
CHEMBL67355 1 6.52
CHEMBL303435 1 6.51
CHEMBL304493 1 6.44
CHEMBL63347 1 6.38
CHEMBL66730 1 6.37
CHEMBL63590 1 6.28
CHEMBL303173 1 6.18
CHEMBL67298 1 5.49
CHEMBL292738 1 5.47
CHEMBL65768 1 5.46
CHEMBL54 HALOPERIDOL 4.0 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67284 ISOCLOTHIAPINE Ki = 5.6 nM 8.25
CHEMBL415300 ISOCLOZAPINE Ki = 21.0 nM 7.68
CHEMBL42 CLOZAPINE Ki = 25.0 nM 7.60
CHEMBL63756 FLUPERLAPINE Ki = 25.0 nM 7.60
CHEMBL63329 Ki = 48.0 nM 7.32
CHEMBL71 CHLORPROMAZINE Ki = 60.7 nM 7.22
CHEMBL63576 Ki = 65.0 nM 7.19
CHEMBL304902 CLOTHIAPINE Ki = 136.0 nM 6.87
CHEMBL63390 Ki = 175.0 nM 6.76
CHEMBL67355 Ki = 303.0 nM 6.52
CHEMBL303435 Ki = 311.0 nM 6.51
CHEMBL304493 Ki = 366.0 nM 6.44
CHEMBL63347 Ki = 415.0 nM 6.38
CHEMBL66730 Ki = 430.0 nM 6.37
CHEMBL63590 Ki = 523.0 nM 6.28
CHEMBL303173 Ki = 665.0 nM 6.18
CHEMBL67298 Ki = 3260.0 nM 5.49
CHEMBL292738 Ki = 3415.0 nM 5.47
CHEMBL65768 Ki = 3450.0 nM 5.46
CHEMBL54 HALOPERIDOL Ki = 7466.0 nM 5.13