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Assay Detail

CHEMBL1663818

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Binding
Inhibition of CHK1 by DELFIA assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
Caldwell JJ, Welsh EJ, Matijssen C, Anderson VE, Antoni L, Boxall K, Urban F, Hayes A, Raynaud FI, Rigoreau LJ, Raynham T, Aherne GW, Pearl LH, Oliver AW, Garrett MD, Collins I.
J Med Chem (2011) 54 : 580 -590
PubMed 21186793 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 5.78 6.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1650128 1 6.98
CHEMBL1650126 1 6.85
CHEMBL1236782 1 6.72
CHEMBL1650125 1 6.70
CHEMBL1650129 1 6.64
CHEMBL1650127 1 6.58
CHEMBL1650124 1 6.48
CHEMBL1650121 1 6.07
CHEMBL1650119 1 6.06
CHEMBL1650123 1 6.06
CHEMBL1650105 1 6.00
CHEMBL1234108 1 5.97
CHEMBL1650122 1 5.96
CHEMBL1650109 1 5.88
CHEMBL1650130 1 5.77
CHEMBL1650115 1 5.76
CHEMBL1650110 1 5.72
CHEMBL1650117 1 5.58
CHEMBL1231179 1 5.35
CHEMBL1650131 1 5.33
CHEMBL1650120 1 5.30
CHEMBL1650113 1 4.69
CHEMBL1650093 1 4.58
CHEMBL1650114 1 4.56
CHEMBL1650055 1 4.55
CHEMBL1650116 1 4.25
CHEMBL1650118 1 -
CHEMBL1650056 1 -
CHEMBL1650112 1 -
CHEMBL1650111 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1650128 IC50 = 105.0 nM 6.98
CHEMBL1650126 IC50 = 140.0 nM 6.85
CHEMBL1236782 IC50 = 190.0 nM 6.72
CHEMBL1650125 IC50 = 200.0 nM 6.70
CHEMBL1650129 IC50 = 230.0 nM 6.64
CHEMBL1650127 IC50 = 260.0 nM 6.58
CHEMBL1650124 IC50 = 330.0 nM 6.48
CHEMBL1650121 IC50 = 850.0 nM 6.07
CHEMBL1650119 IC50 = 870.0 nM 6.06
CHEMBL1650123 IC50 = 870.0 nM 6.06
CHEMBL1650105 IC50 = 990.0 nM 6.00
CHEMBL1234108 IC50 = 1070.0 nM 5.97
CHEMBL1650122 IC50 = 1100.0 nM 5.96
CHEMBL1650109 IC50 = 1320.0 nM 5.88
CHEMBL1650130 IC50 = 1700.0 nM 5.77
CHEMBL1650115 IC50 = 1750.0 nM 5.76
CHEMBL1650110 IC50 = 1910.0 nM 5.72
CHEMBL1650117 IC50 = 2600.0 nM 5.58
CHEMBL1231179 IC50 = 4500.0 nM 5.35
CHEMBL1650131 IC50 = 4650.0 nM 5.33
CHEMBL1650120 IC50 = 5050.0 nM 5.30
CHEMBL1650113 IC50 = 20500.0 nM 4.69
CHEMBL1650093 IC50 = 26000.0 nM 4.58
CHEMBL1650114 IC50 = 27500.0 nM 4.56
CHEMBL1650055 IC50 = 28000.0 nM 4.55
CHEMBL1650116 IC50 = 56000.0 nM 4.25
CHEMBL1650118 IC50 - -
CHEMBL1650056 IC50 - -
CHEMBL1650112 IC50 = 104000.0 nM -
CHEMBL1650111 IC50 - -
CHEMBL1650108 IC50 - -
CHEMBL1650107 IC50 - -
CHEMBL1650106 IC50 - -