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Assay Detail

CHEMBL5586782

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

Binding
Inhibition of URAT1 (unknown origin) by absorbance based assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Solute carrier family 22 member 12 (CHEMBL6120)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Potent and Orally Bioavailable Xanthine Oxidase/Urate Transporter 1 Dual Inhibitor as a Potential Treatment for Hyperuricemia and Gout.
Yang X, Li Y, Pan S, Ma F, Chen H, Deng J, Yue J, Gong Q, Zheng M, Zeng Y, Li J, Zhang Y, Wang X, Zhang X.
J Med Chem (2024) 67 : 14668 -14691
PubMed 39108024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.36 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5591047 1 7.51
CHEMBL5597034 1 7.43
CHEMBL5598112 1 7.35
CHEMBL388590 BENZBROMARONE 4.0 1 7.32
CHEMBL5597097 1 6.98
CHEMBL5596181 1 6.97
CHEMBL5598394 1 6.85
CHEMBL5597164 1 6.76
CHEMBL5597960 1 6.45
CHEMBL5598423 1 6.35
CHEMBL5597556 1 6.22
CHEMBL5596244 1 6.21
CHEMBL5598004 1 5.78
CHEMBL5596444 1 5.66
CHEMBL5598490 1 5.54
CHEMBL5590136 1 5.50
CHEMBL5590746 1 5.44
CHEMBL5596964 1 5.43
CHEMBL5590748 1 5.08
CHEMBL5597135 1 -
CHEMBL5598240 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5591047 IC50 = 31.0 nM 7.51
CHEMBL5597034 IC50 = 37.0 nM 7.43
CHEMBL5598112 IC50 = 45.0 nM 7.35
CHEMBL388590 BENZBROMARONE IC50 = 48.0 nM 7.32
CHEMBL5597097 IC50 = 104.0 nM 6.98
CHEMBL5596181 IC50 = 107.0 nM 6.97
CHEMBL5598394 IC50 = 140.0 nM 6.85
CHEMBL5597164 IC50 = 172.0 nM 6.76
CHEMBL5597960 IC50 = 352.0 nM 6.45
CHEMBL5598423 IC50 = 444.0 nM 6.35
CHEMBL5597556 IC50 = 598.0 nM 6.22
CHEMBL5596244 IC50 = 623.0 nM 6.21
CHEMBL5598004 IC50 = 1652.0 nM 5.78
CHEMBL5596444 IC50 = 2196.0 nM 5.66
CHEMBL5598490 IC50 = 2875.0 nM 5.54
CHEMBL5590136 IC50 = 3189.0 nM 5.50
CHEMBL5590746 IC50 = 3640.0 nM 5.44
CHEMBL5596964 IC50 = 3747.0 nM 5.43
CHEMBL5590748 IC50 = 8302.0 nM 5.08
CHEMBL5597135 IC50 > 10000.0 nM -
CHEMBL5598240 IC50 > 10000.0 nM -