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Assay Detail

CHEMBL5384424

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Functional
Antagonist activity at human H3 receptor
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Advances in Epilepsy: Mechanisms, Clinical Trials, and Drug Therapies.
Hu T, Zhang J, Wang J, Sha L, Xia Y, Ortyl TC, Tian X, Chen L.
J Med Chem (2023) 66 : 4434 -4467
PubMed 37012671 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.58 8.08
IC50 1 8.23 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5434282 1 8.23
CHEMBL4173079 1 8.08
CHEMBL4162433 1 7.80
CHEMBL1789558 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5434282 IC50 = 5.92 nM 8.23
CHEMBL4173079 Ki = 8.4 nM 8.08
CHEMBL4162433 Ki = 16.0 nM 7.80
CHEMBL1789558 Ki = 141.25 nM 6.85