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Assay Detail

CHEMBL5733744

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

Binding
Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software.
63
Total Activities
21
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase Lck (CHEMBL258)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Compounds
(2019)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.93 7.26
kon 21 - -
k_off 21 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3824228 3 7.26
CHEMBL3823255 3 7.26
CHEMBL3823711 3 7.26
CHEMBL6018546 3 7.26
CHEMBL3823212 3 6.26
CHEMBL3823861 3 6.26
CHEMBL3823692 3 -
CHEMBL3823849 3 -
CHEMBL3822591 3 -
CHEMBL3823556 3 -
CHEMBL3824089 3 -
CHEMBL3824233 3 -
CHEMBL3823606 3 -
CHEMBL3823543 3 -
CHEMBL3823620 3 -
CHEMBL3824021 3 -
CHEMBL3824116 3 -
CHEMBL5747601 3 -
CHEMBL3824279 3 -
CHEMBL1421 DASATINIB ANHYDROUS 4.0 3 -
CHEMBL3823104 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6018546 IC50 = 55.0 nM 7.26
CHEMBL3824228 IC50 = 55.0 nM 7.26
CHEMBL3823711 IC50 = 55.0 nM 7.26
CHEMBL3823255 IC50 = 55.0 nM 7.26
CHEMBL3823212 IC50 = 550.0 nM 6.26
CHEMBL3823861 IC50 = 550.0 nM 6.26
CHEMBL3823692 IC50 > 1000.0 nM -
CHEMBL3824279 IC50 < 10.0 nM -
CHEMBL3823606 k_off = - s-1 -
CHEMBL3823606 kon = - -
CHEMBL3823861 k_off = - s-1 -
CHEMBL1421 DASATINIB ANHYDROUS k_off = - s-1 -
CHEMBL1421 DASATINIB ANHYDROUS kon = - -
CHEMBL1421 DASATINIB ANHYDROUS IC50 < 10.0 nM -
CHEMBL3824279 k_off = - s-1 -
CHEMBL3824279 kon = - -
CHEMBL3823104 k_off = - s-1 -
CHEMBL3823692 kon = - -
CHEMBL3823692 k_off = - s-1 -
CHEMBL3823212 kon = - -
CHEMBL3823212 k_off = - s-1 -
CHEMBL3823849 IC50 > 1000.0 nM -
CHEMBL3823849 kon = - -
CHEMBL3823849 k_off = - s-1 -
CHEMBL3822591 IC50 > 1000.0 nM -
CHEMBL3822591 kon = - -
CHEMBL3822591 k_off = - s-1 -
CHEMBL3823861 kon = - -
CHEMBL3823620 kon = - -
CHEMBL3823543 IC50 < 10.0 nM -
CHEMBL3823543 kon = - -
CHEMBL3823543 k_off = - s-1 -
CHEMBL3823255 k_off = - s-1 -
CHEMBL3823711 kon = - -
CHEMBL3823711 k_off = - s-1 -
CHEMBL3823255 kon = - -
CHEMBL3824228 kon = - -
CHEMBL3824228 k_off = - s-1 -
CHEMBL3823620 IC50 < 10.0 nM -
CHEMBL5747601 k_off = - s-1 -
CHEMBL3823620 k_off = - s-1 -
CHEMBL3824021 IC50 > 1000.0 nM -
CHEMBL3823104 kon = - -
CHEMBL3824021 kon = - -
CHEMBL3824021 k_off = - s-1 -
CHEMBL3824116 IC50 < 10.0 nM -
CHEMBL3824116 kon = - -
CHEMBL3824116 k_off = - s-1 -
CHEMBL5747601 IC50 < 10.0 nM -
CHEMBL5747601 kon = - -