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Assay Detail

CHEMBL4022683

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

Binding
Inhibition of human GSK3 using biotin-CREB peptide substrate after 1 hr by scintillation counting method
137
Total Activities
137
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
IC50 137 7.35 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1080901 1 9.00
CHEMBL4064262 1 9.00
CHEMBL4094465 1 9.00
CHEMBL3185148 1 9.00
CHEMBL4072858 1 8.70
CHEMBL4073905 1 8.52
CHEMBL427882 1 8.40
CHEMBL4094020 1 8.40
CHEMBL461262 1 8.40
CHEMBL4099272 1 8.40
CHEMBL4083649 1 8.40
CHEMBL4082639 1 8.40
CHEMBL4072146 1 8.40
CHEMBL412142 LADUVIGLUSIB 1.0 1 8.30
CHEMBL4071127 1 8.30
CHEMBL4098183 1 8.30
CHEMBL4079611 1 8.22
CHEMBL4094072 1 8.22
CHEMBL4099541 1 8.22
CHEMBL4101752 1 8.22
CHEMBL4100641 1 8.22
CHEMBL4069913 1 8.15
CHEMBL4062322 1 8.15
CHEMBL4083757 1 8.15
CHEMBL4094913 1 8.15
CHEMBL4080195 1 8.15
CHEMBL4089009 1 8.15
CHEMBL4085164 1 8.10
CHEMBL4089838 1 8.05
CHEMBL4066536 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3185148 IC50 = 1.0 nM 9.00
CHEMBL1080901 IC50 = 1.0 nM 9.00
CHEMBL4094465 IC50 = 1.0 nM 9.00
CHEMBL4064262 IC50 = 1.0 nM 9.00
CHEMBL4072858 IC50 = 2.0 nM 8.70
CHEMBL4073905 IC50 = 3.0 nM 8.52
CHEMBL4094020 IC50 = 4.0 nM 8.40
CHEMBL4083649 IC50 = 4.0 nM 8.40
CHEMBL461262 IC50 = 4.0 nM 8.40
CHEMBL427882 IC50 = 4.0 nM 8.40
CHEMBL4082639 IC50 = 4.0 nM 8.40
CHEMBL4099272 IC50 = 4.0 nM 8.40
CHEMBL4072146 IC50 = 4.0 nM 8.40
CHEMBL412142 LADUVIGLUSIB IC50 = 5.0 nM 8.30
CHEMBL4071127 IC50 = 5.0 nM 8.30
CHEMBL4098183 IC50 = 5.0 nM 8.30
CHEMBL4079611 IC50 = 6.0 nM 8.22
CHEMBL4099541 IC50 = 6.0 nM 8.22
CHEMBL4094072 IC50 = 6.0 nM 8.22
CHEMBL4100641 IC50 = 6.0 nM 8.22
CHEMBL4101752 IC50 = 6.0 nM 8.22
CHEMBL4062322 IC50 = 7.0 nM 8.15
CHEMBL4083757 IC50 = 7.0 nM 8.15
CHEMBL4089009 IC50 = 7.0 nM 8.15
CHEMBL4094913 IC50 = 7.0 nM 8.15
CHEMBL4080195 IC50 = 7.0 nM 8.15
CHEMBL4069913 IC50 = 7.0 nM 8.15
CHEMBL4085164 IC50 = 8.0 nM 8.10
CHEMBL4104432 IC50 = 9.0 nM 8.05
CHEMBL4066536 IC50 = 9.0 nM 8.05
CHEMBL4089838 IC50 = 9.0 nM 8.05
CHEMBL4072386 IC50 = 10.0 nM 8.00
CHEMBL4078591 IC50 = 11.0 nM 7.96
CHEMBL4096710 IC50 = 12.0 nM 7.92
CHEMBL4061880 IC50 = 13.0 nM 7.89
CHEMBL4062490 IC50 = 13.0 nM 7.89
CHEMBL4071363 IC50 = 14.0 nM 7.85
CHEMBL4089404 IC50 = 15.0 nM 7.82
CHEMBL4080593 IC50 = 15.0 nM 7.82
CHEMBL4064514 IC50 = 15.0 nM 7.82
CHEMBL4097117 IC50 = 16.0 nM 7.80
CHEMBL4104825 IC50 = 17.0 nM 7.77
CHEMBL4084039 IC50 = 18.0 nM 7.75
CHEMBL4092907 IC50 = 19.0 nM 7.72
CHEMBL4095107 IC50 = 19.0 nM 7.72
CHEMBL4102872 IC50 = 19.0 nM 7.72
CHEMBL4090468 IC50 = 19.0 nM 7.72
CHEMBL4102206 IC50 = 21.0 nM 7.68
CHEMBL4060435 IC50 = 22.0 nM 7.66
CHEMBL4095193 IC50 = 22.0 nM 7.66