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Assay Detail

CHEMBL945391

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Functional
Inverse agonist activity at human H3 receptor expressed in CHOK1 cells by GTPgammaS binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel H3 receptor antagonists with improved pharmacokinetic profiles.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Semple G, Ren A, Pereira G, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Lorea J, Grottick AJ.
Bioorg Med Chem Lett (2008) 18 : 4133 -4136
PubMed 18554904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.70 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL408934 1 9.00
CHEMBL471555 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL408934 Ki = 1.0 nM 9.00
CHEMBL471555 Ki = 4.0 nM 8.40