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Assay Detail

CHEMBL904746

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Binding
Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidation
ChEMBL ↗
49
Total Activities
48
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

UDP-glucuronosyltransferase 2B7 (CHEMBL4370) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Isoform-selective inhibition of the human UDP-glucuronosyltransferase 2B7 by isolongifolol derivatives.
Bichlmaier I, Kurkela M, Joshi T, Siiskonen A, Rüffer T, Lang H, Suchanova B, Vahermo M, Finel M, Yli-Kauhaluoma J.
J Med Chem (2007) 50 : 2655 -2664
PubMed 17474732 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 5.84 7.27
Ki 1 7.74 7.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376840 — — 2 7.74
CHEMBL388140 ISOLONGIFOLOL — 1 7.00
CHEMBL374179 — — 1 6.70
CHEMBL226514 — — 1 6.70
CHEMBL388191 — — 1 6.70
CHEMBL226038 — — 1 6.70
CHEMBL376839 — — 1 6.70
CHEMBL226344 — — 1 6.52
CHEMBL389041 — — 1 6.52
CHEMBL226088 — — 1 6.52
CHEMBL225767 — — 1 6.40
CHEMBL225768 — — 1 6.40
CHEMBL225769 — — 1 6.40
CHEMBL390574 — — 1 6.40
CHEMBL389256 — — 1 6.30
CHEMBL226039 — — 1 6.30
CHEMBL449400 — — 1 6.30
CHEMBL225520 — — 1 6.30
CHEMBL374178 — — 1 6.22
CHEMBL390748 — — 1 6.16
CHEMBL389042 — — 1 6.16
CHEMBL225521 — — 1 6.10
CHEMBL2448549 — — 1 6.10
CHEMBL226343 — — 1 6.05
CHEMBL390747 — — 1 6.05
CHEMBL225822 — — 1 6.05
CHEMBL390573 — — 1 6.00
CHEMBL388542 ISOLONGIFOLIC ACID — 1 5.70
CHEMBL439010 — — 1 5.70
CHEMBL225576 — — 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376840 — Ki = 18.4 nM 7.74
CHEMBL376840 — IC50 = 54.0 nM 7.27
CHEMBL388140 ISOLONGIFOLOL IC50 = 100.0 nM 7.00
CHEMBL376839 — IC50 = 200.0 nM 6.70
CHEMBL226514 — IC50 = 200.0 nM 6.70
CHEMBL388191 — IC50 = 200.0 nM 6.70
CHEMBL226038 — IC50 = 200.0 nM 6.70
CHEMBL374179 — IC50 = 200.0 nM 6.70
CHEMBL226344 — IC50 = 300.0 nM 6.52
CHEMBL389041 — IC50 = 300.0 nM 6.52
CHEMBL226088 — IC50 = 300.0 nM 6.52
CHEMBL225767 — IC50 = 400.0 nM 6.40
CHEMBL390574 — IC50 = 400.0 nM 6.40
CHEMBL225768 — IC50 = 400.0 nM 6.40
CHEMBL225769 — IC50 = 400.0 nM 6.40
CHEMBL389256 — IC50 = 500.0 nM 6.30
CHEMBL225520 — IC50 = 500.0 nM 6.30
CHEMBL449400 — IC50 = 500.0 nM 6.30
CHEMBL226039 — IC50 = 500.0 nM 6.30
CHEMBL374178 — IC50 = 600.0 nM 6.22
CHEMBL390748 — IC50 = 700.0 nM 6.16
CHEMBL389042 — IC50 = 700.0 nM 6.16
CHEMBL225521 — IC50 = 800.0 nM 6.10
CHEMBL2448549 — IC50 = 800.0 nM 6.10
CHEMBL225822 — IC50 = 900.0 nM 6.05
CHEMBL226343 — IC50 = 900.0 nM 6.05
CHEMBL390747 — IC50 = 900.0 nM 6.05
CHEMBL390573 — IC50 = 1000.0 nM 6.00
CHEMBL388542 ISOLONGIFOLIC ACID IC50 = 2000.0 nM 5.70
CHEMBL439010 — IC50 = 2000.0 nM 5.70
CHEMBL225576 — IC50 = 3000.0 nM 5.52
CHEMBL226225 — IC50 = 3000.0 nM 5.52
CHEMBL387764 — IC50 = 3000.0 nM 5.52
CHEMBL387981 — IC50 = 3000.0 nM 5.52
CHEMBL226513 — IC50 = 4000.0 nM 5.40
CHEMBL226459 — IC50 = 4000.0 nM 5.40
CHEMBL1203943 — IC50 = 5000.0 nM 5.30
CHEMBL226460 — IC50 = 5000.0 nM 5.30
CHEMBL387765 — IC50 = 8000.0 nM 5.10
CHEMBL375253 — IC50 = 10000.0 nM 5.00
CHEMBL375252 — IC50 = 10000.0 nM 5.00
CHEMBL226276 — IC50 = 12000.0 nM 4.92
CHEMBL226030 — IC50 = 13000.0 nM 4.89
CHEMBL226226 — IC50 = 16000.0 nM 4.80
CHEMBL226078 — IC50 = 18000.0 nM 4.75
CHEMBL376349 — IC50 = 18000.0 nM 4.75
CHEMBL226031 — IC50 = 28000.0 nM 4.55
CHEMBL226277 — IC50 = 32000.0 nM 4.50
CHEMBL226284 — IC50 = 41000.0 nM 4.39