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Assay Detail

CHEMBL840219

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

Binding
Displacement of [3H]N-R-methylhistamine binding to SK-N-MC cell membranes expressing human H3 receptor
22
Total Activities
22
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

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
Ki 22 7.56 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18661 IMMEPIP 1 9.30
CHEMBL175782 METHIMEPIP 1 9.00
CHEMBL356666 1 8.20
CHEMBL179302 1 8.20
CHEMBL179873 1 8.00
CHEMBL176269 1 7.80
CHEMBL176178 1 7.80
CHEMBL150701 1 7.70
CHEMBL177612 1 7.50
CHEMBL369096 1 7.40
CHEMBL176018 1 7.40
CHEMBL175741 1 7.30
CHEMBL175800 1 7.30
CHEMBL369819 1 7.30
CHEMBL176105 1 7.20
CHEMBL368774 1 7.20
CHEMBL176608 1 7.20
CHEMBL179479 1 7.20
CHEMBL175771 1 7.10
CHEMBL180061 1 7.00
CHEMBL369158 1 6.80
CHEMBL179747 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18661 IMMEPIP Ki = 0.5012 nM 9.30
CHEMBL175782 METHIMEPIP Ki = 1.0 nM 9.00
CHEMBL356666 Ki = 6.31 nM 8.20
CHEMBL179302 Ki = 6.31 nM 8.20
CHEMBL179873 Ki = 10.0 nM 8.00
CHEMBL176269 Ki = 15.85 nM 7.80
CHEMBL176178 Ki = 15.85 nM 7.80
CHEMBL150701 Ki = 19.95 nM 7.70
CHEMBL177612 Ki = 31.62 nM 7.50
CHEMBL369096 Ki = 39.81 nM 7.40
CHEMBL176018 Ki = 39.81 nM 7.40
CHEMBL175741 Ki = 50.12 nM 7.30
CHEMBL175800 Ki = 50.12 nM 7.30
CHEMBL369819 Ki = 50.12 nM 7.30
CHEMBL176105 Ki = 63.1 nM 7.20
CHEMBL368774 Ki = 63.1 nM 7.20
CHEMBL176608 Ki = 63.1 nM 7.20
CHEMBL179479 Ki = 63.1 nM 7.20
CHEMBL175771 Ki = 79.43 nM 7.10
CHEMBL180061 Ki = 100.0 nM 7.00
CHEMBL369158 Ki = 158.49 nM 6.80
CHEMBL179747 Ki = 398.11 nM 6.40