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Assay Detail

CHEMBL4037437

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

Binding
Inhibition of CHK1 (unknown origin)
31
Total Activities
31
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

Serine/threonine-protein kinase Chk1 (CHEMBL4630)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.
Yang B, Vasbinder MM, Hird AW, Su Q, Wang H, Yu Y, Toader D, Lyne PD, Read JA, Breed J, Ioannidis S, Deng C, Grondine M, DeGrace N, Whitston D, Brassil P, Janetka JW.
J Med Chem (2018) 61 : 1061 -1073
PubMed 29301085 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.44 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2041933 AZD-7762 1.0 1 8.30
CHEMBL4059912 1 8.22
CHEMBL4079910 1 8.22
CHEMBL4066751 1 8.22
CHEMBL487273 1 8.15
CHEMBL1287920 1 8.15
CHEMBL4067770 1 8.05
CHEMBL4082801 1 8.00
CHEMBL4098878 1 7.92
CHEMBL4093952 1 7.92
CHEMBL4071952 1 7.85
CHEMBL4097937 1 7.82
CHEMBL4105353 1 7.82
CHEMBL4094277 1 7.70
CHEMBL4104102 1 7.68
CHEMBL4088986 1 7.64
CHEMBL4104408 1 7.62
CHEMBL4097424 1 7.60
CHEMBL4096683 1 7.51
CHEMBL4079391 1 7.46
CHEMBL4068572 1 7.25
CHEMBL4100776 1 7.16
CHEMBL4076939 1 7.10
CHEMBL4066399 1 7.08
CHEMBL4089699 1 7.08
CHEMBL4081827 1 6.85
CHEMBL4078664 1 6.82
CHEMBL4081097 1 6.48
CHEMBL4098331 1 6.18
CHEMBL4082386 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2041933 AZD-7762 IC50 = 5.0 nM 8.30
CHEMBL4059912 IC50 = 6.0 nM 8.22
CHEMBL4079910 IC50 = 6.0 nM 8.22
CHEMBL4066751 IC50 = 6.0 nM 8.22
CHEMBL487273 IC50 = 7.0 nM 8.15
CHEMBL1287920 IC50 = 7.0 nM 8.15
CHEMBL4067770 IC50 = 9.0 nM 8.05
CHEMBL4082801 IC50 = 10.0 nM 8.00
CHEMBL4098878 IC50 = 12.0 nM 7.92
CHEMBL4093952 IC50 = 12.0 nM 7.92
CHEMBL4071952 IC50 = 14.0 nM 7.85
CHEMBL4097937 IC50 = 15.0 nM 7.82
CHEMBL4105353 IC50 = 15.0 nM 7.82
CHEMBL4094277 IC50 = 20.0 nM 7.70
CHEMBL4104102 IC50 = 21.0 nM 7.68
CHEMBL4088986 IC50 = 23.0 nM 7.64
CHEMBL4104408 IC50 = 24.0 nM 7.62
CHEMBL4097424 IC50 = 25.0 nM 7.60
CHEMBL4096683 IC50 = 31.0 nM 7.51
CHEMBL4079391 IC50 = 35.0 nM 7.46
CHEMBL4068572 IC50 = 56.0 nM 7.25
CHEMBL4100776 IC50 = 69.0 nM 7.16
CHEMBL4076939 IC50 = 79.0 nM 7.10
CHEMBL4066399 IC50 = 83.0 nM 7.08
CHEMBL4089699 IC50 = 83.0 nM 7.08
CHEMBL4081827 IC50 = 140.0 nM 6.85
CHEMBL4078664 IC50 = 150.0 nM 6.82
CHEMBL4081097 IC50 = 330.0 nM 6.48
CHEMBL4098331 IC50 = 660.0 nM 6.18
CHEMBL4082386 IC50 = 2600.0 nM 5.58
CHEMBL4083348 IC50 = 6800.0 nM 5.17