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Assay Detail

CHEMBL5733738

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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.
60
Total Activities
14
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

Protein-tyrosine kinase 6 (CHEMBL4601)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Compounds
(2019)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.10 7.26
kon 20 - -
k_off 20 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3824089 6 7.26
CHEMBL3824233 6 7.26
CHEMBL3823104 6 7.26
CHEMBL3823543 6 7.26
CHEMBL3823620 6 7.26
CHEMBL3824279 3 7.26
CHEMBL1421 DASATINIB ANHYDROUS 4.0 6 7.26
CHEMBL3823556 3 7.26
CHEMBL3824116 3 7.26
CHEMBL5747601 3 7.26
CHEMBL3823255 3 6.26
CHEMBL3823711 3 6.26
CHEMBL3824228 3 6.26
CHEMBL3824021 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3823543 IC50 = 55.0 nM 7.26
CHEMBL1421 DASATINIB ANHYDROUS IC50 = 55.0 nM 7.26
CHEMBL1421 DASATINIB ANHYDROUS IC50 = 55.0 nM 7.26
CHEMBL3824233 IC50 = 55.0 nM 7.26
CHEMBL3823104 IC50 = 55.0 nM 7.26
CHEMBL5747601 IC50 = 55.0 nM 7.26
CHEMBL3823543 IC50 = 55.0 nM 7.26
CHEMBL3824089 IC50 = 55.0 nM 7.26
CHEMBL3823620 IC50 = 55.0 nM 7.26
CHEMBL3824116 IC50 = 55.0 nM 7.26
CHEMBL3824279 IC50 = 55.0 nM 7.26
CHEMBL3823556 IC50 = 55.0 nM 7.26
CHEMBL3823620 IC50 = 55.0 nM 7.26
CHEMBL3824089 IC50 = 55.0 nM 7.26
CHEMBL3824233 IC50 = 55.0 nM 7.26
CHEMBL3823104 IC50 = 55.0 nM 7.26
CHEMBL3823711 IC50 = 550.0 nM 6.26
CHEMBL3824228 IC50 = 550.0 nM 6.26
CHEMBL3823255 IC50 = 550.0 nM 6.26
CHEMBL1421 DASATINIB ANHYDROUS kon = - -
CHEMBL3823255 k_off = - s-1 -
CHEMBL3824279 kon = - -
CHEMBL3823620 k_off = - s-1 -
CHEMBL3823620 kon = - -
CHEMBL3823543 k_off = - s-1 -
CHEMBL3823543 kon = - -
CHEMBL3823104 k_off = - s-1 -
CHEMBL3823104 kon = - -
CHEMBL3824233 k_off = - s-1 -
CHEMBL3824233 kon = - -
CHEMBL3824089 k_off = - s-1 -
CHEMBL3824089 kon = - -
CHEMBL3824279 k_off = - s-1 -
CHEMBL3824116 kon = - -
CHEMBL3824021 k_off = - s-1 -
CHEMBL5747601 kon = - -
CHEMBL3824021 kon = - -
CHEMBL3824021 IC50 > 1000.0 nM -
CHEMBL1421 DASATINIB ANHYDROUS k_off = - s-1 -
CHEMBL3823620 k_off = - s-1 -
CHEMBL3823620 kon = - -
CHEMBL5747601 k_off = - s-1 -
CHEMBL3824116 k_off = - s-1 -
CHEMBL3824228 kon = - -
CHEMBL3823711 k_off = - s-1 -
CHEMBL3823711 kon = - -
CHEMBL1421 DASATINIB ANHYDROUS kon = - -
CHEMBL3823543 k_off = - s-1 -
CHEMBL3823543 kon = - -
CHEMBL3824228 k_off = - s-1 -