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Assay Detail

CHEMBL990372

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

Binding
Inhibition of CHK1
23
Total Activities
23
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

Synthesis and CHK1 inhibitory potency of Hymenialdisine analogues.
Parmentier JG, Portevin B, Golsteyn RM, Pierré A, Hickman J, Gloanec P, De Nanteuil G.
Bioorg Med Chem Lett (2009) 19 : 841 -844
PubMed 19111462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.59 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL507188 1 7.85
CHEMBL480187 1 7.54
CHEMBL480350 1 7.00
CHEMBL474608 1 6.85
CHEMBL519119 1 6.82
CHEMBL520929 1 6.82
CHEMBL511293 1 6.75
CHEMBL470758 1 6.72
CHEMBL512336 1 6.64
CHEMBL517241 1 6.58
CHEMBL470937 1 6.55
CHEMBL481495 1 6.52
CHEMBL255465 DEBROMOHYMENIALDISINE 1 6.48
CHEMBL514818 1 6.34
CHEMBL332551 1 6.33
CHEMBL475444 1 6.05
CHEMBL481332 1 5.89
CHEMBL480354 1 5.77
CHEMBL361708 HYMENIALDISINE 1 5.72
CHEMBL481494 1 -
CHEMBL519118 1 -
CHEMBL518466 1 -
CHEMBL480189 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL507188 IC50 = 14.0 nM 7.85
CHEMBL480187 IC50 = 29.0 nM 7.54
CHEMBL480350 IC50 = 100.0 nM 7.00
CHEMBL474608 IC50 = 140.0 nM 6.85
CHEMBL519119 IC50 = 150.0 nM 6.82
CHEMBL520929 IC50 = 150.0 nM 6.82
CHEMBL511293 IC50 = 180.0 nM 6.75
CHEMBL470758 IC50 = 190.0 nM 6.72
CHEMBL512336 IC50 = 230.0 nM 6.64
CHEMBL517241 IC50 = 260.0 nM 6.58
CHEMBL470937 IC50 = 280.0 nM 6.55
CHEMBL481495 IC50 = 300.0 nM 6.52
CHEMBL255465 DEBROMOHYMENIALDISINE IC50 = 330.0 nM 6.48
CHEMBL514818 IC50 = 460.0 nM 6.34
CHEMBL332551 IC50 = 470.0 nM 6.33
CHEMBL475444 IC50 = 890.0 nM 6.05
CHEMBL481332 IC50 = 1300.0 nM 5.89
CHEMBL480354 IC50 = 1700.0 nM 5.77
CHEMBL361708 HYMENIALDISINE IC50 = 1900.0 nM 5.72
CHEMBL481494 IC50 > 10000.0 nM -
CHEMBL519118 IC50 > 10000.0 nM -
CHEMBL518466 IC50 > 10000.0 nM -
CHEMBL480189 IC50 > 10000.0 nM -