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Assay Detail

CHEMBL874139

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

Binding
Binding affinity towards human Histamine H3 receptor using [3H]N-methyl-histamine as radioligand
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Non-imidazole heterocyclic histamine H3 receptor antagonists.
Chai W, Breitenbucher JG, Kwok A, Li X, Wong V, Carruthers NI, Lovenberg TW, Mazur C, Wilson SJ, Axe FU, Jones TK.
Bioorg Med Chem Lett (2003) 13 : 1767 -1770
PubMed 12729661 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.64 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294962 1 8.70
CHEMBL49532 1 8.70
CHEMBL51462 1 8.30
CHEMBL48982 1 8.22
CHEMBL49156 1 7.96
CHEMBL51123 1 7.96
CHEMBL52160 1 7.89
CHEMBL51877 1 7.80
CHEMBL50138 1 7.80
CHEMBL49919 1 7.72
CHEMBL299356 1 7.55
CHEMBL299192 1 7.43
CHEMBL48523 1 7.40
CHEMBL51873 1 7.40
CHEMBL299075 1 7.40
CHEMBL51418 1 7.34
CHEMBL48512 1 7.33
CHEMBL299223 1 6.82
CHEMBL49723 1 6.63
CHEMBL300716 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294962 Ki = 2.0 nM 8.70
CHEMBL49532 Ki = 2.0 nM 8.70
CHEMBL51462 Ki = 5.0 nM 8.30
CHEMBL48982 Ki = 6.0 nM 8.22
CHEMBL49156 Ki = 11.0 nM 7.96
CHEMBL51123 Ki = 11.0 nM 7.96
CHEMBL52160 Ki = 13.0 nM 7.89
CHEMBL51877 Ki = 16.0 nM 7.80
CHEMBL50138 Ki = 16.0 nM 7.80
CHEMBL49919 Ki = 19.0 nM 7.72
CHEMBL299356 Ki = 28.0 nM 7.55
CHEMBL299192 Ki = 37.0 nM 7.43
CHEMBL48523 Ki = 40.0 nM 7.40
CHEMBL51873 Ki = 40.0 nM 7.40
CHEMBL299075 Ki = 40.0 nM 7.40
CHEMBL51418 Ki = 46.0 nM 7.34
CHEMBL48512 Ki = 47.0 nM 7.33
CHEMBL299223 Ki = 152.0 nM 6.82
CHEMBL49723 Ki = 236.0 nM 6.63
CHEMBL300716 Ki = 308.0 nM 6.51