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Assay Detail

CHEMBL692576

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

Binding
Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-N-MC
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.
Kitbunnadaj R, Zuiderveld OP, Christophe B, Hulscher S, Menge WM, Gelens E, Snip E, Bakker RA, Celanire S, Gillard M, Talaga P, Timmerman H, Leurs R.
J Med Chem (2004) 47 : 2414 -2417
PubMed 15115383 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.57 9.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18661 IMMEPIP 1 9.32
CHEMBL82298 IMMETHRIDINE 1 9.07
CHEMBL90019 IMBUTAMINE 1 8.39
CHEMBL78498 1 8.35
CHEMBL311473 1 8.16
CHEMBL309654 1 7.81
CHEMBL78497 1 7.48
CHEMBL78838 1 7.28
CHEMBL82244 1 6.85
CHEMBL81644 1 6.23
CHEMBL79126 1 5.98
CHEMBL310360 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18661 IMMEPIP Ki = 0.4786 nM 9.32
CHEMBL82298 IMMETHRIDINE Ki = 0.8511 nM 9.07
CHEMBL90019 IMBUTAMINE Ki = 4.074 nM 8.39
CHEMBL78498 Ki = 4.467 nM 8.35
CHEMBL311473 Ki = 6.918 nM 8.16
CHEMBL309654 Ki = 15.49 nM 7.81
CHEMBL78497 Ki = 33.11 nM 7.48
CHEMBL78838 Ki = 52.48 nM 7.28
CHEMBL82244 Ki = 141.25 nM 6.85
CHEMBL81644 Ki = 588.84 nM 6.23
CHEMBL79126 Ki = 1047.13 nM 5.98
CHEMBL310360 Ki = 1174.9 nM 5.93