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Assay Detail

CHEMBL3106116

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

Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
9
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H2 receptor (CHEMBL1941)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.
Rajagopalan R, Bandyopadhyaya A, Rajagopalan DR, Rajagopalan P.
Bioorg Med Chem Lett (2014) 24 : 576 -579
PubMed 24365159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.13 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3544974 ASENAPINE MALEATE 4.0 2 8.24
CHEMBL30 CIMETIDINE 4.0 2 7.16
CHEMBL3104091 2 7.09
CHEMBL3104093 2 6.03
CHEMBL3104092 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3544974 ASENAPINE MALEATE Ki = 5.754 nM 8.24
CHEMBL3544974 ASENAPINE MALEATE Ki = 5.7 nM 8.24
CHEMBL30 CIMETIDINE Ki = 70.0 nM 7.16
CHEMBL30 CIMETIDINE Ki = 70.79 nM 7.15
CHEMBL3104091 Ki = 81.0 nM 7.09
CHEMBL3104091 Ki = 81.28 nM 7.09
CHEMBL3104093 Ki = 943.0 nM 6.03
CHEMBL3104093 Ki = 933.25 nM 6.03
CHEMBL3104092 Ki > 10000.0 nM -