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Assay Detail

CHEMBL1767808

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Binding
Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting
ChEMBL ↗
42
Total Activities
42
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

Developing potent human uric acid transporter 1 (hURAT1) inhibitors.
Wempe MF, Jutabha P, Quade B, Iwen TJ, Frick MM, Ross IR, Rice PJ, Anzai N, Endou H.
J Med Chem (2011) 54 : 2701 -2713
PubMed 21449597 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 5.95 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388590 BENZBROMARONE 4.0 1 7.58
CHEMBL1767106 — — 1 7.38
CHEMBL1767109 — — 1 7.08
CHEMBL1767112 — — 1 6.96
CHEMBL1767079 — — 1 6.86
CHEMBL1767114 — — 1 6.75
CHEMBL1767107 — — 1 6.72
CHEMBL1767111 — — 1 6.54
CHEMBL1767108 — — 1 6.45
CHEMBL1767116 — — 1 6.18
CHEMBL1767117 — — 1 6.11
CHEMBL1767099 — — 1 5.95
CHEMBL1767110 — — 1 5.84
CHEMBL1767113 — — 1 5.78
CHEMBL1767088 — — 1 5.61
CHEMBL1767090 — — 1 5.60
CHEMBL1474963 BENZARONE 4.0 1 5.55
CHEMBL1767097 — — 1 5.41
CHEMBL1767105 — — 1 5.41
CHEMBL1767091 — — 1 5.17
CHEMBL1767100 — — 1 4.71
CHEMBL1767115 — — 1 4.63
CHEMBL1767094 — — 1 4.47
CHEMBL897 PROBENECID 4.0 1 4.06
CHEMBL1767089 — — 1 -
CHEMBL1767095 — — 1 -
CHEMBL1767087 — — 1 -
CHEMBL1767086 — — 1 -
CHEMBL1767085 — — 1 -
CHEMBL1767084 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388590 BENZBROMARONE IC50 = 26.0 nM 7.58
CHEMBL1767106 — IC50 = 42.0 nM 7.38
CHEMBL1767109 — IC50 = 83.0 nM 7.08
CHEMBL1767112 — IC50 = 111.0 nM 6.96
CHEMBL1767079 — IC50 = 138.0 nM 6.86
CHEMBL1767114 — IC50 = 177.0 nM 6.75
CHEMBL1767107 — IC50 = 189.0 nM 6.72
CHEMBL1767111 — IC50 = 287.0 nM 6.54
CHEMBL1767108 — IC50 = 358.0 nM 6.45
CHEMBL1767116 — IC50 = 667.0 nM 6.18
CHEMBL1767117 — IC50 = 772.0 nM 6.11
CHEMBL1767099 — IC50 = 1130.0 nM 5.95
CHEMBL1767110 — IC50 = 1440.0 nM 5.84
CHEMBL1767113 — IC50 = 1650.0 nM 5.78
CHEMBL1767088 — IC50 = 2460.0 nM 5.61
CHEMBL1767090 — IC50 = 2490.0 nM 5.60
CHEMBL1474963 BENZARONE IC50 = 2800.0 nM 5.55
CHEMBL1767097 — IC50 = 3920.0 nM 5.41
CHEMBL1767105 — IC50 = 3940.0 nM 5.41
CHEMBL1767091 — IC50 = 6680.0 nM 5.17
CHEMBL1767100 — IC50 = 19690.0 nM 4.71
CHEMBL1767115 — IC50 = 23460.0 nM 4.63
CHEMBL1767094 — IC50 = 33650.0 nM 4.47
CHEMBL897 PROBENECID IC50 = 86390.0 nM 4.06
CHEMBL1767096 — IC50 - — -
CHEMBL1767098 — IC50 - — -
CHEMBL1767093 — IC50 - — -
CHEMBL1767101 — IC50 - — -
CHEMBL1767102 — IC50 - — -
CHEMBL1767103 — IC50 - — -
CHEMBL1767104 — IC50 - — -
CHEMBL1767092 — IC50 - — -
CHEMBL1767080 — IC50 - — -
CHEMBL1767081 — IC50 - — -
CHEMBL1767082 — IC50 - — -
CHEMBL1767083 — IC50 - — -
CHEMBL1767084 — IC50 - — -
CHEMBL1767085 — IC50 - — -
CHEMBL1767086 — IC50 - — -
CHEMBL1767087 — IC50 - — -
CHEMBL1767095 — IC50 - — -
CHEMBL1767089 — IC50 - — -