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Assay Detail

CHEMBL5734115

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Binding
Kinase Inhibiting Activity Assay: Chk-1 Kinase Inhibiting ActivityThe compounds of the invention were tested for activity against Chk-1 kinase using the materials and protocols set out below.Reaction Buffer:Base Reaction buffer: 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/ml BSA, 0.1 mM Na3VO4, 2 mM DTT, 1% DMSO*Required cofactors are added individually to each kinase reactionReaction Procedure:(i) Prepare indicated substrate in freshly prepared Base Reaction Buffer(ii) Deliver any required cofactors to the substrate solution above(iii) Deliver indicated kinase into the substrate solution and gently mix(iv) Deliver compounds in DMSO into the kinase reaction mixture(v) Deliver 33P-ATP (specific activity 0.01 μCi/μl final) into the reaction mixture to initiate the reaction.(vi) Incubate kinase reaction for 120 minutes at room temperature(vii) Reactions are spotted onto P81 ion exchange paper (Whatman #3698-915)(viii) Wash filters extensively in 0.1% phosphoric acid.(ix) Dry filters and measure counts in scintillation counterKinase Information:CHK-1 Genbank Accession # AF016582Recombinant full length construct, N-terminal GST tagged, purified from insect cells.No special measures were taken to activate this kinase.Final concentration in assay=0.5 nMSubstrate: CHKtidePeptide sequence: [KKKVSRSGLYRSPSMPENLNRPR]Final concentration in assay=20 μM
ChEMBL ↗
441
Total Activities
147
Compounds Tested
3
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

Pharmaceutical compounds
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 147 9.68 10.92
kon 147 - -
k_off 147 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5747621 — — 3 10.92
CHEMBL5812486 — — 3 10.80
CHEMBL5944770 — — 3 10.80
CHEMBL6027444 — — 3 10.80
CHEMBL5935192 — — 3 10.72
CHEMBL5861249 — — 3 10.68
CHEMBL5777143 — — 3 10.68
CHEMBL5773272 — — 3 10.66
CHEMBL5893031 — — 3 10.66
CHEMBL6047287 — — 3 10.64
CHEMBL5956681 — — 3 10.60
CHEMBL5842815 — — 3 10.59
CHEMBL5824984 — — 3 10.59
CHEMBL5855043 — — 3 10.59
CHEMBL5845949 — — 3 10.57
CHEMBL5931629 — — 3 10.57
CHEMBL6053351 — — 3 10.51
CHEMBL5995631 — — 3 10.47
CHEMBL5839557 — — 3 10.39
CHEMBL5750986 — — 3 10.37
CHEMBL5912614 — — 3 10.36
CHEMBL5796222 — — 3 10.34
CHEMBL6002144 — — 3 10.32
CHEMBL5956287 — — 3 10.32
CHEMBL5796100 — — 3 10.29
CHEMBL5772293 — — 3 10.28
CHEMBL5962917 — — 3 10.28
CHEMBL5802846 — — 3 10.28
CHEMBL5977891 — — 3 10.27
CHEMBL5907466 — — 3 10.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5747621 — IC50 = 0.012 nM 10.92
CHEMBL5812486 — IC50 = 0.016 nM 10.80
CHEMBL6027444 — IC50 = 0.016 nM 10.80
CHEMBL5944770 — IC50 = 0.016 nM 10.80
CHEMBL5935192 — IC50 = 0.019 nM 10.72
CHEMBL5861249 — IC50 = 0.021 nM 10.68
CHEMBL5777143 — IC50 = 0.021 nM 10.68
CHEMBL5773272 — IC50 = 0.022 nM 10.66
CHEMBL5893031 — IC50 = 0.022 nM 10.66
CHEMBL6047287 — IC50 = 0.023 nM 10.64
CHEMBL5956681 — IC50 = 0.025 nM 10.60
CHEMBL5855043 — IC50 = 0.026 nM 10.59
CHEMBL5842815 — IC50 = 0.026 nM 10.59
CHEMBL5824984 — IC50 = 0.026 nM 10.59
CHEMBL5931629 — IC50 = 0.027 nM 10.57
CHEMBL5845949 — IC50 = 0.027 nM 10.57
CHEMBL6053351 — IC50 = 0.031 nM 10.51
CHEMBL5995631 — IC50 = 0.034 nM 10.47
CHEMBL5839557 — IC50 = 0.041 nM 10.39
CHEMBL5750986 — IC50 = 0.043 nM 10.37
CHEMBL5912614 — IC50 = 0.044 nM 10.36
CHEMBL5796222 — IC50 = 0.046 nM 10.34
CHEMBL5956287 — IC50 = 0.048 nM 10.32
CHEMBL6002144 — IC50 = 0.048 nM 10.32
CHEMBL5796100 — IC50 = 0.051 nM 10.29
CHEMBL5802846 — IC50 = 0.053 nM 10.28
CHEMBL5962917 — IC50 = 0.053 nM 10.28
CHEMBL5772293 — IC50 = 0.052 nM 10.28
CHEMBL5907466 — IC50 = 0.054 nM 10.27
CHEMBL5977891 — IC50 = 0.054 nM 10.27
CHEMBL5904385 — IC50 = 0.055 nM 10.26
CHEMBL5847574 — IC50 = 0.056 nM 10.25
CHEMBL5936666 — IC50 = 0.058 nM 10.24
CHEMBL5959878 — IC50 = 0.058 nM 10.24
CHEMBL5750451 — IC50 = 0.059 nM 10.23
CHEMBL5785658 — IC50 = 0.068 nM 10.17
CHEMBL5926704 — IC50 = 0.071 nM 10.15
CHEMBL5983291 — IC50 = 0.071 nM 10.15
CHEMBL5836251 — IC50 = 0.074 nM 10.13
CHEMBL6057862 — IC50 = 0.077 nM 10.11
CHEMBL5772252 — IC50 = 0.077 nM 10.11
CHEMBL5916214 — IC50 = 0.079 nM 10.10
CHEMBL5905622 — IC50 = 0.081 nM 10.09
CHEMBL5815401 — IC50 = 0.082 nM 10.09
CHEMBL5901221 — IC50 = 0.084 nM 10.08
CHEMBL6034036 — IC50 = 0.085 nM 10.07
CHEMBL5941388 — IC50 = 0.087 nM 10.06
CHEMBL5986500 — IC50 = 0.095 nM 10.02
CHEMBL5954239 — IC50 = 0.097 nM 10.01
CHEMBL5838153 — IC50 = 0.1 nM 10.00