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Assay Detail

CHEMBL5735121

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

Binding
In Vitro Activity Assay: The in vitro activity of the compounds described herein in inhibiting TAK1, HCK and other kinases were obtained using an Invitrogen Select Screening assay as known in the art.
ChEMBL ↗
51
Total Activities
16
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

Tyrosine-protein kinase HCK (CHEMBL3234) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Methods to treat lymphoplasmacytic lymphoma
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.85 7.75
kon 17 - -
k_off 17 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5887569 — — 3 7.75
CHEMBL6006139 — — 3 7.56
CHEMBL6038355 — — 3 7.55
CHEMBL5961742 — — 3 7.47
CHEMBL5962638 — — 3 7.42
CHEMBL5885824 — — 3 7.21
CHEMBL5860086 — — 3 6.94
CHEMBL6022481 — — 3 6.73
CHEMBL5929345 — — 3 6.60
CHEMBL5705821 — — 6 6.56
CHEMBL5950869 — — 3 6.42
CHEMBL5903220 — — 3 6.41
CHEMBL5829674 — — 3 5.16
CHEMBL5798659 — — 3 -
CHEMBL5744065 — — 3 -
CHEMBL5833736 — — 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5887569 — IC50 = 18.0 nM 7.75
CHEMBL6006139 — IC50 = 27.4 nM 7.56
CHEMBL6038355 — IC50 = 28.0 nM 7.55
CHEMBL5961742 — IC50 = 33.8 nM 7.47
CHEMBL5962638 — IC50 = 38.4 nM 7.42
CHEMBL5885824 — IC50 = 61.8 nM 7.21
CHEMBL5860086 — IC50 = 116.0 nM 6.94
CHEMBL6022481 — IC50 = 185.0 nM 6.73
CHEMBL5929345 — IC50 = 253.0 nM 6.60
CHEMBL5705821 — IC50 = 275.0 nM 6.56
CHEMBL5950869 — IC50 = 382.0 nM 6.42
CHEMBL5903220 — IC50 = 392.0 nM 6.41
CHEMBL5705821 — IC50 = 889.0 nM 6.05
CHEMBL5829674 — IC50 = 6980.0 nM 5.16
CHEMBL5705821 — k_off = - s-1 -
CHEMBL5798659 — kon = - — -
CHEMBL6038355 — kon = - — -
CHEMBL6038355 — k_off = - s-1 -
CHEMBL5929345 — kon = - — -
CHEMBL5929345 — k_off = - s-1 -
CHEMBL6022481 — kon = - — -
CHEMBL6022481 — k_off = - s-1 -
CHEMBL5950869 — kon = - — -
CHEMBL5950869 — k_off = - s-1 -
CHEMBL5744065 — IC50 > 10000.0 nM -
CHEMBL5885824 — k_off = - s-1 -
CHEMBL5962638 — kon = - — -
CHEMBL5962638 — k_off = - s-1 -
CHEMBL5961742 — kon = - — -
CHEMBL5961742 — k_off = - s-1 -
CHEMBL5705821 — k_off = - s-1 -
CHEMBL5798659 — IC50 > 10000.0 nM -
CHEMBL5887569 — kon = - — -
CHEMBL5744065 — kon = - — -
CHEMBL5829674 — k_off = - s-1 -
CHEMBL5829674 — kon = - — -
CHEMBL5833736 — IC50 > 10000.0 nM -
CHEMBL5744065 — k_off = - s-1 -
CHEMBL5705821 — kon = - — -
CHEMBL5833736 — kon = - — -
CHEMBL5833736 — k_off = - s-1 -
CHEMBL5705821 — kon = - — -
CHEMBL5887569 — k_off = - s-1 -
CHEMBL5903220 — kon = - — -
CHEMBL5903220 — k_off = - s-1 -
CHEMBL6006139 — kon = - — -
CHEMBL6006139 — k_off = - s-1 -
CHEMBL5860086 — kon = - — -
CHEMBL5860086 — k_off = - s-1 -
CHEMBL5885824 — kon = - — -