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Assay Detail

CHEMBL5158074

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

Binding
Inhibition of human recombinant NEK1 (1 to 505 residues) using ULight-p70 S6K peptide as substrate incubated for 30 mins by LANCE Ultra TR-FRET assay
19
Total Activities
19
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 Nek1 (CHEMBL5855)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Illuminating a Dark Kinase: Structure-Guided Design, Synthesis, and Evaluation of a Potent Nek1 Inhibitor and Its Effects on the Embryonic Zebrafish Pronephros.
Baumann G, Meckel T, Böhm K, Shih YH, Dickhaut M, Reichardt T, Pilakowski J, Pehl U, Schmidt B.
J Med Chem (2022) 65 : 1265 -1282
PubMed 35081715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.43 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5201686 1 6.48
CHEMBL5206874 1 6.00
CHEMBL5189609 1 5.89
CHEMBL5200819 1 5.80
CHEMBL5174141 1 5.72
CHEMBL5182208 1 5.70
CHEMBL5182549 1 5.57
CHEMBL5197597 1 5.50
CHEMBL5203616 1 5.24
CHEMBL5208840 1 5.18
CHEMBL520954 1 5.15
CHEMBL5197360 1 5.06
CHEMBL5181887 1 5.00
CHEMBL5197075 1 4.57
CHEMBL5180286 1 4.54
CHEMBL5198653 1 -
CHEMBL5180705 1 -
CHEMBL5172286 1 -
CHEMBL5175782 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5201686 IC50 = 330.0 nM 6.48
CHEMBL5206874 IC50 = 990.0 nM 6.00
CHEMBL5189609 IC50 = 1300.0 nM 5.89
CHEMBL5200819 IC50 = 1600.0 nM 5.80
CHEMBL5174141 IC50 = 1900.0 nM 5.72
CHEMBL5182208 IC50 = 2000.0 nM 5.70
CHEMBL5182549 IC50 = 2700.0 nM 5.57
CHEMBL5197597 IC50 = 3200.0 nM 5.50
CHEMBL5203616 IC50 = 5800.0 nM 5.24
CHEMBL5208840 IC50 = 6600.0 nM 5.18
CHEMBL520954 IC50 = 7100.0 nM 5.15
CHEMBL5197360 IC50 = 8800.0 nM 5.06
CHEMBL5181887 IC50 = 10000.0 nM 5.00
CHEMBL5197075 IC50 = 27000.0 nM 4.57
CHEMBL5180286 IC50 = 29000.0 nM 4.54
CHEMBL5198653 IC50 - -
CHEMBL5180705 IC50 > 30000.0 nM -
CHEMBL5172286 IC50 > 10000.0 nM -
CHEMBL5175782 IC50 - -