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Assay Detail

CHEMBL826108

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

Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.
Kitbunnadaj R, Hashimoto T, Poli E, Zuiderveld OP, Menozzi A, Hidaka R, de Esch IJ, Bakker RA, Menge WM, Yamatodani A, Coruzzi G, Timmerman H, Leurs R.
J Med Chem (2005) 48 : 2100 -2107
PubMed 15771452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 7.91 9.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18661 IMMEPIP 1 9.90
CHEMBL175782 METHIMEPIP 1 9.50
CHEMBL179302 1 8.60
CHEMBL356666 1 8.50
CHEMBL176178 1 8.40
CHEMBL176269 1 8.40
CHEMBL179873 1 8.10
CHEMBL176105 1 8.10
CHEMBL150701 1 7.90
CHEMBL179479 1 7.80
CHEMBL369819 1 7.80
CHEMBL175741 1 7.60
CHEMBL369096 1 7.50
CHEMBL175800 1 7.30
CHEMBL177612 1 7.30
CHEMBL368774 1 7.20
CHEMBL179747 1 7.10
CHEMBL180061 1 6.70
CHEMBL369158 1 6.50
CHEMBL176608 1 -
CHEMBL175771 1 -
CHEMBL176018 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18661 IMMEPIP EC50 = 0.1259 nM 9.90
CHEMBL175782 METHIMEPIP EC50 = 0.3162 nM 9.50
CHEMBL179302 EC50 = 2.512 nM 8.60
CHEMBL356666 EC50 = 3.162 nM 8.50
CHEMBL176178 EC50 = 3.981 nM 8.40
CHEMBL176269 EC50 = 3.981 nM 8.40
CHEMBL179873 EC50 = 7.943 nM 8.10
CHEMBL176105 EC50 = 7.943 nM 8.10
CHEMBL150701 EC50 = 12.59 nM 7.90
CHEMBL179479 EC50 = 15.85 nM 7.80
CHEMBL369819 EC50 = 15.85 nM 7.80
CHEMBL175741 EC50 = 25.12 nM 7.60
CHEMBL369096 EC50 = 31.62 nM 7.50
CHEMBL175800 EC50 = 50.12 nM 7.30
CHEMBL177612 EC50 = 50.12 nM 7.30
CHEMBL368774 EC50 = 63.1 nM 7.20
CHEMBL179747 EC50 = 79.43 nM 7.10
CHEMBL180061 EC50 = 199.53 nM 6.70
CHEMBL369158 EC50 = 316.23 nM 6.50
CHEMBL176608 EC50 < 10000.0 nM -
CHEMBL175771 EC50 < 10000.0 nM -
CHEMBL176018 EC50 < 10000.0 nM -