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Assay Detail

CHEMBL4728315

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

Binding
Inhibition of CLK1 V324A mutant (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity.
Schröder M,Bullock AN,Fedorov O,Bracher F,Chaikuad A,Knapp S
J Med Chem (2020) 63 : 10224 -10234
PubMed 32787076 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 5.86 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1349996 1 6.17
CHEMBL1945559 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1349996 Ki = 670.0 nM 6.17
CHEMBL1945559 Ki = 2810.0 nM 5.55