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Assay Detail

CHEMBL691634

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

Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Cerebellum
Confidence 9 — Direct single protein target
Curated By Expert

Target

Histamine H1 receptor (CHEMBL3943)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and antiallergic activity of 11-(aminoalkylidene)-6,11-dihydrodibenz[b,e]oxepin derivatives.
Ohshima E, Otaki S, Sato H, Kumazawa T, Obase H, Ishii A, Ishii H, Ohmori K, Hirayama N.
J Med Chem (1992) 35 : 2074 -2084
PubMed 1350797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.23 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL366965 1 9.89
CHEMBL65612 1 9.32
CHEMBL293652 1 8.38
CHEMBL65822 1 8.38
CHEMBL304185 1 8.34
CHEMBL304223 1 8.30
CHEMBL65699 1 8.28
CHEMBL304042 1 8.20
CHEMBL65492 1 8.12
CHEMBL63596 1 8.00
CHEMBL63424 1 7.92
CHEMBL538750 1 7.85
CHEMBL1719 OLOPATADINE HYDROCHLORIDE 4.0 1 7.80
CHEMBL64067 1 7.70
CHEMBL302215 1 7.62
CHEMBL264979 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL366965 Ki = 0.13 nM 9.89
CHEMBL65612 Ki = 0.48 nM 9.32
CHEMBL293652 Ki = 4.2 nM 8.38
CHEMBL65822 Ki = 4.2 nM 8.38
CHEMBL304185 Ki = 4.6 nM 8.34
CHEMBL304223 Ki = 5.0 nM 8.30
CHEMBL65699 Ki = 5.2 nM 8.28
CHEMBL304042 Ki = 6.3 nM 8.20
CHEMBL65492 Ki = 7.6 nM 8.12
CHEMBL63596 Ki = 10.0 nM 8.00
CHEMBL63424 Ki = 12.0 nM 7.92
CHEMBL538750 Ki = 14.0 nM 7.85
CHEMBL1719 OLOPATADINE HYDROCHLORIDE Ki = 16.0 nM 7.80
CHEMBL64067 Ki = 20.0 nM 7.70
CHEMBL302215 Ki = 24.0 nM 7.62
CHEMBL264979 Ki = 29.0 nM 7.54