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Assay Detail

CHEMBL3380639

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

ADMET
Inhibition of CYP2C9 (unknown origin)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease.
Cioffi CL, Dobri N, Freeman EE, Conlon MP, Chen P, Stafford DG, Schwarz DM, Golden KC, Zhu L, Kitchen DB, Barnes KD, Racz B, Qin Q, Michelotti E, Cywin CL, Martin WH, Pearson PG, Johnson G, Petrukhin K.
J Med Chem (2014) 57 : 7731 -7757
PubMed 25210858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.53 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3359017 1 6.48
CHEMBL3359014 1 6.47
CHEMBL3359019 1 6.24
CHEMBL3359023 1 6.00
CHEMBL3359022 1 5.25
CHEMBL3359020 1 5.06
CHEMBL3359018 1 4.89
CHEMBL3359024 1 4.77
CHEMBL3359021 1 4.57
CHEMBL1230001 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3359017 IC50 = 330.0 nM 6.48
CHEMBL3359014 IC50 = 340.0 nM 6.47
CHEMBL3359019 IC50 = 580.0 nM 6.24
CHEMBL3359023 IC50 = 1000.0 nM 6.00
CHEMBL3359022 IC50 = 5600.0 nM 5.25
CHEMBL3359020 IC50 = 8700.0 nM 5.06
CHEMBL3359018 IC50 = 13000.0 nM 4.89
CHEMBL3359024 IC50 = 17000.0 nM 4.77
CHEMBL3359021 IC50 = 27000.0 nM 4.57
CHEMBL1230001 IC50 > 100000.0 nM -