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Assay Detail

CHEMBL4729629

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Binding
Inhibition of human liver FBPase expressed in Escherichia coli BL21(DE3) using FBP as substrate in presence of PGI and G6PDH by spectrophotometric method
ChEMBL ↗
91
Total Activities
91
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

Fructose-1,6-bisphosphatase 1 (CHEMBL3975) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of N-Arylsulfonyl-Indole-2-Carboxamide Derivatives as Potent, Selective, and Orally Bioavailable Fructose-1,6-Bisphosphatase Inhibitors-Design, Synthesis, In Vivo Glucose Lowering Effects, and X-ray Crystal Complex Analysis.
Zhou J,Bie J,Wang X,Liu Q,Li R,Chen H,Hu J,Cao H,Ji W,Li Y,Liu S,Shen Z,Xu B
J Med Chem (2020) 63 : 10307 -10329
PubMed 32820629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 91 6.44 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4755209 — — 1 7.57
CHEMBL4759496 — — 1 7.54
CHEMBL4784745 — — 1 7.40
CHEMBL495498 MB-05032 2.0 1 7.36
CHEMBL4747278 — — 1 7.28
CHEMBL4762728 — — 1 7.25
CHEMBL4750118 — — 1 7.23
CHEMBL4764972 — — 1 7.20
CHEMBL4763100 — — 1 7.20
CHEMBL4760200 — — 1 7.16
CHEMBL4759549 — — 1 7.15
CHEMBL4745214 — — 1 7.07
CHEMBL4799382 — — 1 7.05
CHEMBL4776774 — — 1 7.00
CHEMBL4748284 — — 1 7.00
CHEMBL4791277 — — 1 6.92
CHEMBL4743304 — — 1 6.92
CHEMBL4792830 — — 1 6.89
CHEMBL4756632 — — 1 6.89
CHEMBL4790364 — — 1 6.85
CHEMBL4778169 — — 1 6.85
CHEMBL4786333 — — 1 6.85
CHEMBL4792589 — — 1 6.85
CHEMBL4747394 — — 1 6.85
CHEMBL4790616 — — 1 6.85
CHEMBL4748117 — — 1 6.82
CHEMBL4740367 — — 1 6.82
CHEMBL4749652 — — 1 6.82
CHEMBL4764458 — — 1 6.80
CHEMBL4744035 — — 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4755209 — IC50 = 27.0 nM 7.57
CHEMBL4759496 — IC50 = 29.0 nM 7.54
CHEMBL4784745 — IC50 = 40.0 nM 7.40
CHEMBL495498 MB-05032 IC50 = 44.0 nM 7.36
CHEMBL4747278 — IC50 = 52.0 nM 7.28
CHEMBL4762728 — IC50 = 56.0 nM 7.25
CHEMBL4750118 — IC50 = 59.0 nM 7.23
CHEMBL4764972 — IC50 = 63.0 nM 7.20
CHEMBL4763100 — IC50 = 63.0 nM 7.20
CHEMBL4760200 — IC50 = 70.0 nM 7.16
CHEMBL4759549 — IC50 = 71.0 nM 7.15
CHEMBL4745214 — IC50 = 85.0 nM 7.07
CHEMBL4799382 — IC50 = 90.0 nM 7.05
CHEMBL4776774 — IC50 = 100.0 nM 7.00
CHEMBL4748284 — IC50 = 100.0 nM 7.00
CHEMBL4791277 — IC50 = 120.0 nM 6.92
CHEMBL4743304 — IC50 = 120.0 nM 6.92
CHEMBL4792830 — IC50 = 130.0 nM 6.89
CHEMBL4756632 — IC50 = 130.0 nM 6.89
CHEMBL4790364 — IC50 = 140.0 nM 6.85
CHEMBL4778169 — IC50 = 140.0 nM 6.85
CHEMBL4786333 — IC50 = 140.0 nM 6.85
CHEMBL4792589 — IC50 = 140.0 nM 6.85
CHEMBL4747394 — IC50 = 140.0 nM 6.85
CHEMBL4790616 — IC50 = 140.0 nM 6.85
CHEMBL4748117 — IC50 = 150.0 nM 6.82
CHEMBL4749652 — IC50 = 150.0 nM 6.82
CHEMBL4740367 — IC50 = 150.0 nM 6.82
CHEMBL4764458 — IC50 = 160.0 nM 6.80
CHEMBL4744035 — IC50 = 160.0 nM 6.80
CHEMBL4756676 — IC50 = 160.0 nM 6.80
CHEMBL4752882 — IC50 = 180.0 nM 6.75
CHEMBL4759251 — IC50 = 190.0 nM 6.72
CHEMBL4787644 — IC50 = 200.0 nM 6.70
CHEMBL4751290 — IC50 = 210.0 nM 6.68
CHEMBL4749495 — IC50 = 210.0 nM 6.68
CHEMBL4749376 — IC50 = 220.0 nM 6.66
CHEMBL4784026 — IC50 = 230.0 nM 6.64
CHEMBL4795527 — IC50 = 230.0 nM 6.64
CHEMBL4741542 — IC50 = 240.0 nM 6.62
CHEMBL4784307 — IC50 = 260.0 nM 6.58
CHEMBL4795892 — IC50 = 270.0 nM 6.57
CHEMBL4746499 — IC50 = 280.0 nM 6.55
CHEMBL4776022 — IC50 = 310.0 nM 6.51
CHEMBL4755462 — IC50 = 320.0 nM 6.50
CHEMBL4786994 — IC50 = 350.0 nM 6.46
CHEMBL4792258 — IC50 = 360.0 nM 6.44
CHEMBL4741865 — IC50 = 400.0 nM 6.40
CHEMBL4745108 — IC50 = 400.0 nM 6.40
CHEMBL4760102 — IC50 = 430.0 nM 6.37