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Assay Detail

CHEMBL5225679

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

ADMET
Inhibition of human CYP2C9 expressed in insect cell microsomes in presence of NADP+ by fluorescence based analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2C9 (CHEMBL3397)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist.
Zhao J, Wang S, Markison S, Kim SH, Han S, Chen M, Kusnetzow AK, Rico-Bautista E, Johns M, Luo R, Struthers RS, Madan A, Zhu Y, Betz SF.
ACS Med Chem Lett (2023) 14 : 66 -74
PubMed 36655128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.15 5.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5276605 1 5.20
CHEMBL5267842 PALTUSOTINE 3.0 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5276605 IC50 = 6309.57 nM 5.20
CHEMBL5267842 PALTUSOTINE IC50 = 7943.28 nM 5.10