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Assay Detail

CHEMBL3802094

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

Binding
Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assay
33
Total Activities
33
Compounds Tested
1
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 17B (CHEMBL3980)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.
Jung ME, Byun BJ, Kim HM, Lee JY, Park JH, Lee N, Son YH, Choi SU, Yang KM, Kim SJ, Lee K, Kim YC, Choi G.
Bioorg Med Chem Lett (2016) 26 : 2719 -2723
PubMed 27106709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.66 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3797480 1 8.52
CHEMBL3799389 1 8.10
CHEMBL3799585 1 8.00
CHEMBL3799505 1 7.85
CHEMBL3797466 1 7.85
CHEMBL513703 1 7.68
CHEMBL3798563 1 7.11
CHEMBL3798680 1 6.92
CHEMBL3798579 1 6.92
CHEMBL3797732 1 6.70
CHEMBL604263 1 6.60
CHEMBL3797817 1 6.54
CHEMBL3797582 1 6.48
CHEMBL1077291 1 6.21
CHEMBL3798736 1 6.16
CHEMBL216543 1 6.15
CHEMBL3799218 1 6.02
CHEMBL3798747 1 5.92
CHEMBL3799256 1 5.89
CHEMBL3798927 1 5.89
CHEMBL594192 1 5.85
CHEMBL3799269 1 5.82
CHEMBL3797619 1 5.50
CHEMBL1083838 1 5.21
CHEMBL1276127 INDIRUBIN 2.0 1 -
CHEMBL1084939 1 -
CHEMBL1077286 1 -
CHEMBL1084938 1 -
CHEMBL3799919 1 -
CHEMBL3798674 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3797480 IC50 = 3.0 nM 8.52
CHEMBL3799389 IC50 = 8.0 nM 8.10
CHEMBL3799585 IC50 = 10.0 nM 8.00
CHEMBL3799505 IC50 = 14.0 nM 7.85
CHEMBL3797466 IC50 = 14.0 nM 7.85
CHEMBL513703 IC50 = 21.0 nM 7.68
CHEMBL3798563 IC50 = 77.0 nM 7.11
CHEMBL3798680 IC50 = 120.0 nM 6.92
CHEMBL3798579 IC50 = 120.0 nM 6.92
CHEMBL3797732 IC50 = 200.0 nM 6.70
CHEMBL604263 IC50 = 250.0 nM 6.60
CHEMBL3797817 IC50 = 290.0 nM 6.54
CHEMBL3797582 IC50 = 330.0 nM 6.48
CHEMBL1077291 IC50 = 620.0 nM 6.21
CHEMBL3798736 IC50 = 700.0 nM 6.16
CHEMBL216543 IC50 = 710.0 nM 6.15
CHEMBL3799218 IC50 = 950.0 nM 6.02
CHEMBL3798747 IC50 = 1200.0 nM 5.92
CHEMBL3799256 IC50 = 1300.0 nM 5.89
CHEMBL3798927 IC50 = 1300.0 nM 5.89
CHEMBL594192 IC50 = 1400.0 nM 5.85
CHEMBL3799269 IC50 = 1500.0 nM 5.82
CHEMBL3797619 IC50 = 3200.0 nM 5.50
CHEMBL1083838 IC50 = 6200.0 nM 5.21
CHEMBL1276127 INDIRUBIN IC50 > 10000.0 nM -
CHEMBL1084939 IC50 > 10000.0 nM -
CHEMBL1077286 IC50 > 10000.0 nM -
CHEMBL1084938 IC50 > 10000.0 nM -
CHEMBL3799919 IC50 > 10000.0 nM -
CHEMBL3798674 IC50 > 10000.0 nM -
CHEMBL3799549 IC50 > 10000.0 nM -
CHEMBL3799765 IC50 > 10000.0 nM -
CHEMBL1095686 IC50 > 10000.0 nM -