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Assay Detail

CHEMBL4392453

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

ADMET
Inhibition of recombinant rat UGT1A1 using beta-estradiol as substrate preincubated for 5 mins followed by substrate addition and measured after 40 mins by LC-MS/MS analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

UDP-glucuronosyltransferase 1A1 (CHEMBL4523339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir.
A M Subbaiah M, Mandlekar S, Desikan S, Ramar T, Subramani L, Annadurai M, Desai SD, Sinha S, Jenkins SM, Krystal MR, Subramanian M, Sridhar S, Padmanabhan S, Bhutani P, Arla R, Singh S, Sinha J, Thakur M, Kadow JF, Meanwell NA.
J Med Chem (2019) 62 : 3553 -3574
PubMed 30938524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.14 5.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1163 ATAZANAVIR 4.0 1 5.38
CHEMBL4573907 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1163 ATAZANAVIR IC50 = 4200.0 nM 5.38
CHEMBL4573907 IC50 = 12600.0 nM 4.90