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Assay Detail

CHEMBL692579

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

Binding
In vitro binding affinity for human Histamine H3 receptor by displacing N-[3H]-methylhistamine in SK-N-MC cells was determined
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type SK-N-MC
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
Apodaca R, Dvorak CA, Xiao W, Barbier AJ, Boggs JD, Wilson SJ, Lovenberg TW, Carruthers NI.
J Med Chem (2003) 46 : 3938 -3944
PubMed 12930154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.48 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129411 1 9.29
CHEMBL129542 JNJ-5207852 1 9.24
CHEMBL129306 1 9.13
CHEMBL126321 1 9.08
CHEMBL339867 1 9.06
CHEMBL339324 1 9.03
CHEMBL421624 1 9.02
CHEMBL340688 1 8.91
CHEMBL126829 1 8.87
CHEMBL340023 1 8.82
CHEMBL129785 1 8.77
CHEMBL341491 1 8.64
CHEMBL337942 1 8.41
CHEMBL129820 1 8.08
CHEMBL126904 1 8.05
CHEMBL128190 1 7.87
CHEMBL129133 1 7.30
CHEMBL339215 1 7.30
CHEMBL126495 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129411 Ki = 0.5129 nM 9.29
CHEMBL129542 JNJ-5207852 Ki = 0.5754 nM 9.24
CHEMBL129306 Ki = 0.7413 nM 9.13
CHEMBL126321 Ki = 0.8318 nM 9.08
CHEMBL339867 Ki = 0.871 nM 9.06
CHEMBL339324 Ki = 0.9333 nM 9.03
CHEMBL421624 Ki = 0.955 nM 9.02
CHEMBL340688 Ki = 1.23 nM 8.91
CHEMBL126829 Ki = 1.349 nM 8.87
CHEMBL340023 Ki = 1.514 nM 8.82
CHEMBL129785 Ki = 1.698 nM 8.77
CHEMBL341491 Ki = 2.291 nM 8.64
CHEMBL337942 Ki = 3.89 nM 8.41
CHEMBL129820 Ki = 8.318 nM 8.08
CHEMBL126904 Ki = 8.913 nM 8.05
CHEMBL128190 Ki = 13.49 nM 7.87
CHEMBL129133 Ki = 50.12 nM 7.30
CHEMBL339215 Ki = 50.12 nM 7.30
CHEMBL126495 Ki = 630.96 nM 6.20