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Assay Detail

CHEMBL696448

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

Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
11
Total Activities
11
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 H4 receptor (CHEMBL3759)
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 11 6.17 7.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL90019 IMBUTAMINE 1 7.84
CHEMBL18661 IMMEPIP 1 7.66
CHEMBL82298 IMMETHRIDINE 1 6.61
CHEMBL78497 1 6.32
CHEMBL78838 1 6.16
CHEMBL309654 1 6.00
CHEMBL79126 1 5.90
CHEMBL311473 1 5.88
CHEMBL81644 1 5.34
CHEMBL82244 1 5.29
CHEMBL310360 1 4.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL90019 IMBUTAMINE Ki = 14.45 nM 7.84
CHEMBL18661 IMMEPIP Ki = 21.88 nM 7.66
CHEMBL82298 IMMETHRIDINE Ki = 245.47 nM 6.61
CHEMBL78497 Ki = 478.63 nM 6.32
CHEMBL78838 Ki = 691.83 nM 6.16
CHEMBL309654 Ki = 1000.0 nM 6.00
CHEMBL79126 Ki = 1258.93 nM 5.90
CHEMBL311473 Ki = 1318.26 nM 5.88
CHEMBL81644 Ki = 4570.88 nM 5.34
CHEMBL82244 Ki = 5128.61 nM 5.29
CHEMBL310360 Ki = 12302.69 nM 4.91