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Assay Detail

CHEMBL4193347

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Binding
Activation of recombinant human liver glucokinase 2 assessed as reduction in NADH production in presence of 5 mM glucose by G6PDH coupled assay
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Hexokinase-4 (CHEMBL3820) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation.
Wang Z, Shi X, Zhang H, Yu L, Cheng Y, Zhang H, Zhang H, Zhou J, Chen J, Shen X, Duan W.
Eur J Med Chem (2017) 139 : 128 -152
PubMed 28800453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 47 6.20 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4206856 — — 1 7.05
CHEMBL4204989 — — 1 7.00
CHEMBL4206729 — — 1 6.85
CHEMBL4203455 — — 1 6.80
CHEMBL4208677 — — 1 6.77
CHEMBL4206337 — — 1 6.77
CHEMBL4215660 — — 1 6.75
CHEMBL4202919 — — 1 6.70
CHEMBL4204808 — — 1 6.70
CHEMBL4203863 — — 1 6.68
CHEMBL4217013 — — 1 6.68
CHEMBL4207270 — — 1 6.64
CHEMBL4211616 — — 1 6.64
CHEMBL4214183 — — 1 6.54
CHEMBL4213613 — — 1 6.54
CHEMBL4204346 — — 1 6.52
CHEMBL4205913 — — 1 6.50
CHEMBL4207808 — — 1 6.48
CHEMBL4205786 — — 1 6.34
CHEMBL4209218 — — 1 6.31
CHEMBL4212156 — — 1 6.30
CHEMBL4210704 — — 1 6.26
CHEMBL4216606 — — 1 6.16
CHEMBL4209159 — — 1 6.09
CHEMBL4216383 — — 1 6.06
CHEMBL4202493 — — 1 6.05
CHEMBL4205489 — — 1 6.05
CHEMBL4212586 — — 1 6.05
CHEMBL2165615 NERIGLIATIN 2.0 1 6.03
CHEMBL4212033 — — 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4206856 — EC50 = 90.0 nM 7.05
CHEMBL4204989 — EC50 = 100.0 nM 7.00
CHEMBL4206729 — EC50 = 140.0 nM 6.85
CHEMBL4203455 — EC50 = 160.0 nM 6.80
CHEMBL4208677 — EC50 = 170.0 nM 6.77
CHEMBL4206337 — EC50 = 170.0 nM 6.77
CHEMBL4215660 — EC50 = 180.0 nM 6.75
CHEMBL4202919 — EC50 = 200.0 nM 6.70
CHEMBL4204808 — EC50 = 200.0 nM 6.70
CHEMBL4203863 — EC50 = 210.0 nM 6.68
CHEMBL4217013 — EC50 = 210.0 nM 6.68
CHEMBL4207270 — EC50 = 230.0 nM 6.64
CHEMBL4211616 — EC50 = 230.0 nM 6.64
CHEMBL4214183 — EC50 = 290.0 nM 6.54
CHEMBL4213613 — EC50 = 290.0 nM 6.54
CHEMBL4204346 — EC50 = 300.0 nM 6.52
CHEMBL4205913 — EC50 = 320.0 nM 6.50
CHEMBL4207808 — EC50 = 330.0 nM 6.48
CHEMBL4205786 — EC50 = 460.0 nM 6.34
CHEMBL4209218 — EC50 = 490.0 nM 6.31
CHEMBL4212156 — EC50 = 500.0 nM 6.30
CHEMBL4210704 — EC50 = 550.0 nM 6.26
CHEMBL4216606 — EC50 = 690.0 nM 6.16
CHEMBL4209159 — EC50 = 820.0 nM 6.09
CHEMBL4216383 — EC50 = 870.0 nM 6.06
CHEMBL4202493 — EC50 = 900.0 nM 6.05
CHEMBL4205489 — EC50 = 890.0 nM 6.05
CHEMBL4212586 — EC50 = 890.0 nM 6.05
CHEMBL2165615 NERIGLIATIN EC50 = 930.0 nM 6.03
CHEMBL4212033 — EC50 = 1090.0 nM 5.96
CHEMBL4211625 — EC50 = 1130.0 nM 5.95
CHEMBL4212948 — EC50 = 1300.0 nM 5.89
CHEMBL4210790 — EC50 = 2220.0 nM 5.65
CHEMBL4211227 — EC50 = 2230.0 nM 5.65
CHEMBL4215125 — EC50 = 2600.0 nM 5.58
CHEMBL4207312 — EC50 = 4600.0 nM 5.34
CHEMBL4213321 — EC50 = 5420.0 nM 5.27
CHEMBL4217491 — EC50 = 6080.0 nM 5.22
CHEMBL4215129 — EC50 = 7000.0 nM 5.16
CHEMBL4208388 — EC50 = 7080.0 nM 5.15
CHEMBL4212777 — EC50 = 8420.0 nM 5.08
CHEMBL4216481 — EC50 > 10000.0 nM -
CHEMBL4204287 — EC50 > 10000.0 nM -
CHEMBL4207681 — EC50 > 10000.0 nM -
CHEMBL4217728 — EC50 > 10000.0 nM -
CHEMBL4217208 — EC50 > 10000.0 nM -
CHEMBL4203459 — EC50 > 10000.0 nM -