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Assay Detail

CHEMBL696443

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

Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
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
EC50 11 5.63 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18661 IMMEPIP 1 7.25
CHEMBL90019 IMBUTAMINE 1 7.05
CHEMBL82298 IMMETHRIDINE 1 6.04
CHEMBL78497 1 5.90
CHEMBL311473 1 5.82
CHEMBL309654 1 5.81
CHEMBL79126 1 5.50
CHEMBL81644 1 4.98
CHEMBL78838 1 4.82
CHEMBL82244 1 4.49
CHEMBL310360 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18661 IMMEPIP EC50 = 56.23 nM 7.25
CHEMBL90019 IMBUTAMINE EC50 = 89.13 nM 7.05
CHEMBL82298 IMMETHRIDINE EC50 = 912.01 nM 6.04
CHEMBL78497 EC50 = 1258.93 nM 5.90
CHEMBL311473 EC50 = 1513.56 nM 5.82
CHEMBL309654 EC50 = 1548.82 nM 5.81
CHEMBL79126 EC50 = 3162.28 nM 5.50
CHEMBL81644 EC50 = 10471.29 nM 4.98
CHEMBL78838 EC50 = 15135.61 nM 4.82
CHEMBL82244 EC50 = 32359.37 nM 4.49
CHEMBL310360 EC50 = 58884.37 nM 4.23