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Assay Detail

CHEMBL695758

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

Binding
Binding affinity towards histamine H3 receptor using [3H](R)-alpha-methylhistamine as radioligand in guinea pig cortical homogenates
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Histamine H3 receptor (CHEMBL5076)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.
Tozer MJ, Harper EA, Kalindjian SB, Pether MJ, Shankley NP, Watt GF.
Bioorg Med Chem Lett (1999) 9 : 1825 -1830
PubMed 10406649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.60 10.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268229 1 10.07
CHEMBL90 HISTAMINE 4.0 1 9.84
CHEMBL299589 1 8.99
CHEMBL301176 1 7.85
CHEMBL55836 1 7.85
CHEMBL53361 1 7.83
CHEMBL300704 1 7.79
CHEMBL55018 1 7.64
CHEMBL417017 1 7.60
CHEMBL52090 1 7.30
CHEMBL54858 1 7.07
CHEMBL52080 1 6.94
CHEMBL53412 1 6.86
CHEMBL301838 1 6.31
CHEMBL298581 1 5.99
CHEMBL53056 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268229 Ki = 0.08511 nM 10.07
CHEMBL90 HISTAMINE Ki = 0.1445 nM 9.84
CHEMBL299589 Ki = 1.023 nM 8.99
CHEMBL301176 Ki = 14.13 nM 7.85
CHEMBL55836 Ki = 14.13 nM 7.85
CHEMBL53361 Ki = 14.79 nM 7.83
CHEMBL300704 Ki = 16.22 nM 7.79
CHEMBL55018 Ki = 22.91 nM 7.64
CHEMBL417017 Ki = 25.12 nM 7.60
CHEMBL52090 Ki = 50.12 nM 7.30
CHEMBL54858 Ki = 85.11 nM 7.07
CHEMBL52080 Ki = 114.82 nM 6.94
CHEMBL53412 Ki = 138.04 nM 6.86
CHEMBL301838 Ki = 489.78 nM 6.31
CHEMBL298581 Ki = 1023.29 nM 5.99
CHEMBL53056 Ki = 1862.09 nM 5.73