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Assay Detail

CHEMBL5732489

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Binding
Enzyme Inhibition Assay: c-Src and Syk Enzyme InhibitionThe inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), are evaluated in a similar fashion to that described hereinabove. The relevant enzyme (3000 ng/mL or 2000 ng/mL respectively, 2.5 μL) is incubated with the test compound (either 4 μg/mL, 0.4 μg/mL, 0.04 μg/mL, or 0.004 μg/mL, 2.5 μL each) for 2 hr at RT. The FRET peptides (8 μM, 2.5 μL), and appropriate ATP solutions (2.5 μL, 800 μM for c-Src, and 60 μM ATP for Syk) are then added to the enzymes/compound mixtures and incubated for 1 hr. Development reagent (protease, 5 μL) is added for 1 hr prior to detection in a fluorescence microplate reader (Varioskan® Flash, ThermoFisher Scientific).
ChEMBL ↗
126
Total Activities
42
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proto-oncogene tyrosine-protein kinase Src (CHEMBL267) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Kinase inhibitors
(2017)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 7.74 8.52
kon 42 - -
k_off 42 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5822857 — — 3 8.52
CHEMBL5991930 — — 3 8.40
CHEMBL5963080 — — 3 8.40
CHEMBL5935125 — — 3 8.30
CHEMBL5910007 — — 3 8.22
CHEMBL5919556 — — 3 8.15
CHEMBL6040369 — — 3 8.10
CHEMBL5943347 — — 3 8.10
CHEMBL5990759 — — 3 8.00
CHEMBL5820101 — — 3 8.00
CHEMBL5864913 — — 3 8.00
CHEMBL6036559 — — 3 8.00
CHEMBL5840394 — — 3 7.96
CHEMBL5823917 — — 3 7.96
CHEMBL6030562 — — 3 7.92
CHEMBL5750422 — — 3 7.89
CHEMBL5768749 — — 3 7.85
CHEMBL6014157 — — 3 7.82
CHEMBL5933911 — — 3 7.80
CHEMBL5750627 — — 3 7.77
CHEMBL5835423 — — 3 7.72
CHEMBL6040301 — — 3 7.70
CHEMBL5841040 — — 3 7.66
CHEMBL5802500 — — 3 7.64
CHEMBL5819054 — — 3 7.64
CHEMBL5981366 — — 3 7.64
CHEMBL5872801 — — 3 7.57
CHEMBL5752694 — — 3 7.55
CHEMBL6026207 — — 3 7.55
CHEMBL5988272 — — 3 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5822857 — IC50 = 3.0 nM 8.52
CHEMBL5963080 — IC50 = 4.0 nM 8.40
CHEMBL5991930 — IC50 = 4.0 nM 8.40
CHEMBL5935125 — IC50 = 5.0 nM 8.30
CHEMBL5910007 — IC50 = 6.0 nM 8.22
CHEMBL5919556 — IC50 = 7.0 nM 8.15
CHEMBL6040369 — IC50 = 8.0 nM 8.10
CHEMBL5943347 — IC50 = 8.0 nM 8.10
CHEMBL5864913 — IC50 = 10.0 nM 8.00
CHEMBL5990759 — IC50 = 10.0 nM 8.00
CHEMBL5820101 — IC50 = 10.0 nM 8.00
CHEMBL6036559 — IC50 = 10.0 nM 8.00
CHEMBL5823917 — IC50 = 11.0 nM 7.96
CHEMBL5840394 — IC50 = 11.0 nM 7.96
CHEMBL6030562 — IC50 = 12.0 nM 7.92
CHEMBL5750422 — IC50 = 13.0 nM 7.89
CHEMBL5768749 — IC50 = 14.0 nM 7.85
CHEMBL6014157 — IC50 = 15.0 nM 7.82
CHEMBL5933911 — IC50 = 16.0 nM 7.80
CHEMBL5750627 — IC50 = 17.0 nM 7.77
CHEMBL5835423 — IC50 = 19.0 nM 7.72
CHEMBL6040301 — IC50 = 20.0 nM 7.70
CHEMBL5841040 — IC50 = 22.0 nM 7.66
CHEMBL5802500 — IC50 = 23.0 nM 7.64
CHEMBL5981366 — IC50 = 23.0 nM 7.64
CHEMBL5819054 — IC50 = 23.0 nM 7.64
CHEMBL5872801 — IC50 = 27.0 nM 7.57
CHEMBL5988272 — IC50 = 28.0 nM 7.55
CHEMBL5752694 — IC50 = 28.0 nM 7.55
CHEMBL6026207 — IC50 = 28.0 nM 7.55
CHEMBL6059696 — IC50 = 39.0 nM 7.41
CHEMBL6037362 — IC50 = 39.0 nM 7.41
CHEMBL6009171 — IC50 = 46.0 nM 7.34
CHEMBL5810491 — IC50 = 47.0 nM 7.33
CHEMBL6011006 — IC50 = 48.0 nM 7.32
CHEMBL5855478 — IC50 = 53.0 nM 7.28
CHEMBL5909900 — IC50 = 61.0 nM 7.21
CHEMBL5769990 — IC50 = 73.0 nM 7.14
CHEMBL5896433 — IC50 = 137.0 nM 6.86
CHEMBL5888113 — IC50 = 154.0 nM 6.81
CHEMBL5981366 — k_off = - s-1 -
CHEMBL6009171 — k_off = - s-1 -
CHEMBL5820101 — k_off = - s-1 -
CHEMBL6037362 — kon = - — -
CHEMBL5820101 — kon = - — -
CHEMBL6037362 — k_off = - s-1 -
CHEMBL6011006 — kon = - — -
CHEMBL6011006 — k_off = - s-1 -
CHEMBL5819054 — k_off = - s-1 -
CHEMBL5835423 — kon = - — -