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Assay Detail

CHEMBL4022684

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

Binding
Inhibition of GSK3 expressed in in CHO-IR cells expressing human insulin receptor assessed as glycogen synthase activation after 30 mins by filter paper assay
ChEMBL ↗
99
Total Activities
99
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.
Wagman AS, Boyce RS, Brown SP, Fang E, Goff D, Jansen JM, Le VP, Levine BH, Ng SC, Ni ZJ, Nuss JM, Pfister KB, Ramurthy S, Renhowe PA, Ring DB, Shu W, Subramanian S, Zhou XA, Shafer CM, Harrison SD, Johnson KW, Bussiere DE.
J Med Chem (2017) 60 : 8482 -8514
PubMed 29016121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 99 6.09 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4083757 — — 1 8.00
CHEMBL427882 — — 1 7.52
CHEMBL4094020 — — 1 7.40
CHEMBL4101752 — — 1 7.30
CHEMBL4072146 — — 1 7.30
CHEMBL4062322 — — 1 7.16
CHEMBL3185148 — — 1 7.10
CHEMBL4095193 — — 1 7.10
CHEMBL4102206 — — 1 7.05
CHEMBL4089838 — — 1 7.00
CHEMBL4078153 — — 1 6.96
CHEMBL4086044 — — 1 6.96
CHEMBL4072858 — — 1 6.92
CHEMBL4094465 — — 1 6.89
CHEMBL4069913 — — 1 6.82
CHEMBL4061876 — — 1 6.77
CHEMBL4094072 — — 1 6.72
CHEMBL4083649 — — 1 6.66
CHEMBL4080195 — — 1 6.62
CHEMBL4064262 — — 1 6.60
CHEMBL1080901 — — 1 6.58
CHEMBL4100641 — — 1 6.58
CHEMBL4080593 — — 1 6.55
CHEMBL4064514 — — 1 6.55
CHEMBL4072386 — — 1 6.54
CHEMBL4085164 — — 1 6.54
CHEMBL4064990 — — 1 6.52
CHEMBL4079611 — — 1 6.52
CHEMBL4060435 — — 1 6.50
CHEMBL4102940 — — 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4083757 — EC50 = 10.0 nM 8.00
CHEMBL427882 — EC50 = 30.0 nM 7.52
CHEMBL4094020 — EC50 = 40.0 nM 7.40
CHEMBL4101752 — EC50 = 50.0 nM 7.30
CHEMBL4072146 — EC50 = 50.0 nM 7.30
CHEMBL4062322 — EC50 = 70.0 nM 7.16
CHEMBL3185148 — EC50 = 80.0 nM 7.10
CHEMBL4095193 — EC50 = 80.0 nM 7.10
CHEMBL4102206 — EC50 = 90.0 nM 7.05
CHEMBL4089838 — EC50 = 100.0 nM 7.00
CHEMBL4078153 — EC50 = 110.0 nM 6.96
CHEMBL4086044 — EC50 = 110.0 nM 6.96
CHEMBL4072858 — EC50 = 120.0 nM 6.92
CHEMBL4094465 — EC50 = 130.0 nM 6.89
CHEMBL4069913 — EC50 = 150.0 nM 6.82
CHEMBL4061876 — EC50 = 170.0 nM 6.77
CHEMBL4094072 — EC50 = 190.0 nM 6.72
CHEMBL4083649 — EC50 = 220.0 nM 6.66
CHEMBL4080195 — EC50 = 240.0 nM 6.62
CHEMBL4064262 — EC50 = 250.0 nM 6.60
CHEMBL1080901 — EC50 = 260.0 nM 6.58
CHEMBL4100641 — EC50 = 260.0 nM 6.58
CHEMBL4080593 — EC50 = 280.0 nM 6.55
CHEMBL4064514 — EC50 = 280.0 nM 6.55
CHEMBL4085164 — EC50 = 290.0 nM 6.54
CHEMBL4072386 — EC50 = 290.0 nM 6.54
CHEMBL4064990 — EC50 = 300.0 nM 6.52
CHEMBL4079611 — EC50 = 300.0 nM 6.52
CHEMBL4060435 — EC50 = 320.0 nM 6.50
CHEMBL4102940 — EC50 = 350.0 nM 6.46
CHEMBL461262 — EC50 = 370.0 nM 6.43
CHEMBL4078661 — EC50 = 370.0 nM 6.43
CHEMBL4066536 — EC50 = 390.0 nM 6.41
CHEMBL4089009 — EC50 = 420.0 nM 6.38
CHEMBL4082639 — EC50 = 430.0 nM 6.37
CHEMBL4073905 — EC50 = 440.0 nM 6.36
CHEMBL4071127 — EC50 = 500.0 nM 6.30
CHEMBL4084039 — EC50 = 510.0 nM 6.29
CHEMBL4099272 — EC50 = 510.0 nM 6.29
CHEMBL4075148 — EC50 = 670.0 nM 6.17
CHEMBL4096710 — EC50 = 730.0 nM 6.14
CHEMBL412142 LADUVIGLUSIB EC50 = 770.0 nM 6.11
CHEMBL4086973 — EC50 = 790.0 nM 6.10
CHEMBL4092907 — EC50 = 810.0 nM 6.09
CHEMBL4104825 — EC50 = 840.0 nM 6.08
CHEMBL4071363 — EC50 = 860.0 nM 6.07
CHEMBL4089907 — EC50 = 900.0 nM 6.05
CHEMBL4097136 — EC50 = 1010.0 nM 6.00
CHEMBL4102872 — EC50 = 1000.0 nM 6.00
CHEMBL4098183 — EC50 = 1020.0 nM 5.99