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Assay Detail

CHEMBL944207

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

Binding
Inhibition of Chk1
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.
Janetka JW, Almeida L, Ashwell S, Brassil PJ, Daly K, Deng C, Gero T, Glynn RE, Horn CL, Ioannidis S, Lyne P, Newcombe NJ, Oza VB, Pass M, Springer SK, Su M, Toader D, Vasbinder MM, Yu D, Yu Y, Zabludoff SD.
Bioorg Med Chem Lett (2008) 18 : 4242 -4248
PubMed 18547806 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 75 7.12 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL519913 1 8.52
CHEMBL471096 1 8.52
CHEMBL488231 1 8.40
CHEMBL519248 1 8.30
CHEMBL470289 1 8.30
CHEMBL469481 1 8.22
CHEMBL520902 1 8.22
CHEMBL520734 1 8.22
CHEMBL488230 1 8.22
CHEMBL488044 1 8.15
CHEMBL487273 1 8.15
CHEMBL459428 1 8.15
CHEMBL504542 1 8.10
CHEMBL459631 1 8.05
CHEMBL516784 1 8.05
CHEMBL527881 1 8.05
CHEMBL487622 1 8.05
CHEMBL471549 1 8.00
CHEMBL513191 1 8.00
CHEMBL488835 1 8.00
CHEMBL518661 1 8.00
CHEMBL470288 1 8.00
CHEMBL486234 1 7.96
CHEMBL517553 1 7.96
CHEMBL487437 1 7.89
CHEMBL513377 1 7.85
CHEMBL460685 1 7.77
CHEMBL469686 1 7.72
CHEMBL510101 1 7.54
CHEMBL508982 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL519913 IC50 = 3.0 nM 8.52
CHEMBL471096 IC50 = 3.0 nM 8.52
CHEMBL488231 IC50 = 4.0 nM 8.40
CHEMBL519248 IC50 = 5.0 nM 8.30
CHEMBL470289 IC50 = 5.0 nM 8.30
CHEMBL469481 IC50 = 6.0 nM 8.22
CHEMBL520902 IC50 = 6.0 nM 8.22
CHEMBL520734 IC50 = 6.0 nM 8.22
CHEMBL488230 IC50 = 6.0 nM 8.22
CHEMBL488044 IC50 = 7.0 nM 8.15
CHEMBL487273 IC50 = 7.0 nM 8.15
CHEMBL459428 IC50 = 7.0 nM 8.15
CHEMBL504542 IC50 = 8.0 nM 8.10
CHEMBL527881 IC50 = 9.0 nM 8.05
CHEMBL516784 IC50 = 9.0 nM 8.05
CHEMBL459631 IC50 = 9.0 nM 8.05
CHEMBL487622 IC50 = 9.0 nM 8.05
CHEMBL471549 IC50 = 10.0 nM 8.00
CHEMBL513191 IC50 = 10.0 nM 8.00
CHEMBL488835 IC50 = 10.0 nM 8.00
CHEMBL518661 IC50 = 10.0 nM 8.00
CHEMBL470288 IC50 = 10.0 nM 8.00
CHEMBL486234 IC50 = 11.0 nM 7.96
CHEMBL517553 IC50 = 11.0 nM 7.96
CHEMBL487437 IC50 = 13.0 nM 7.89
CHEMBL513377 IC50 = 14.0 nM 7.85
CHEMBL460685 IC50 = 17.0 nM 7.77
CHEMBL469686 IC50 = 19.0 nM 7.72
CHEMBL510101 IC50 = 29.0 nM 7.54
CHEMBL508982 IC50 = 30.0 nM 7.52
CHEMBL452274 IC50 = 31.0 nM 7.51
CHEMBL461294 IC50 = 35.0 nM 7.46
CHEMBL507700 IC50 = 37.0 nM 7.43
CHEMBL453053 IC50 = 39.0 nM 7.41
CHEMBL488039 IC50 = 41.0 nM 7.39
CHEMBL516478 IC50 = 41.0 nM 7.39
CHEMBL488287 IC50 = 41.0 nM 7.39
CHEMBL452020 IC50 = 50.0 nM 7.30
CHEMBL452273 IC50 = 72.0 nM 7.14
CHEMBL471094 IC50 = 100.0 nM 7.00
CHEMBL471095 IC50 = 100.0 nM 7.00
CHEMBL459650 IC50 = 100.0 nM 7.00
CHEMBL460888 IC50 = 100.0 nM 7.00
CHEMBL460889 IC50 = 100.0 nM 7.00
CHEMBL488239 IC50 = 110.0 nM 6.96
CHEMBL459651 IC50 = 110.0 nM 6.96
CHEMBL471365 IC50 = 110.0 nM 6.96
CHEMBL471548 IC50 = 130.0 nM 6.89
CHEMBL452021 IC50 = 150.0 nM 6.82
CHEMBL486233 IC50 = 160.0 nM 6.80