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Assay Detail

CHEMBL4618909

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

Binding
Inhibition of wild type human Naa50 (1852 to 2082 residues) expressed in Escherichia coli BL21(DE3) cells using MLGPEGGEGK peptide as substrate after 75 mins in presence of acetyl CoA by rapidfire mass spectrometry analysis
18
Total Activities
18
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

N-alpha-acetyltransferase 50 (CHEMBL4630854)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Characterization of Specific <i>N</i>-α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library.
Kung PP, Bingham P, Burke BJ, Chen Q, Cheng X, Deng YL, Dou D, Feng J, Gallego GM, Gehring MR, Grant SK, Greasley S, Harris AR, Maegley KA, Meier J, Meng X, Montano JL, Morgan BA, Naughton BS, Palde PB, Paul TA, Richardson P, Sakata S, Shaginian A, Sonnenburg WK, Subramanyam C, Timofeevski S, Wan J, Yan W, Stewart AE.
ACS Med Chem Lett (2020) 11 : 1175 -1184
PubMed 32550998 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.28 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4645901 1 8.15
CHEMBL4642788 1 7.89
CHEMBL4642700 1 7.89
CHEMBL4639216 1 7.85
CHEMBL4642911 1 7.52
CHEMBL4644527 1 7.06
CHEMBL4636177 1 6.77
CHEMBL4648534 1 6.37
CHEMBL4640907 1 6.00
CHEMBL4645967 1 5.80
CHEMBL4635926 1 5.70
CHEMBL4635301 1 5.57
CHEMBL4636574 1 5.54
CHEMBL4632414 1 5.41
CHEMBL4634916 1 4.98
CHEMBL4633201 1 4.92
CHEMBL4645057 1 4.89
CHEMBL4637072 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4645901 IC50 = 7.0 nM 8.15
CHEMBL4642788 IC50 = 13.0 nM 7.89
CHEMBL4642700 IC50 = 13.0 nM 7.89
CHEMBL4639216 IC50 = 14.0 nM 7.85
CHEMBL4642911 IC50 = 30.0 nM 7.52
CHEMBL4644527 IC50 = 88.0 nM 7.06
CHEMBL4636177 IC50 = 170.0 nM 6.77
CHEMBL4648534 IC50 = 430.0 nM 6.37
CHEMBL4640907 IC50 = 1000.0 nM 6.00
CHEMBL4645967 IC50 = 1600.0 nM 5.80
CHEMBL4635926 IC50 = 2000.0 nM 5.70
CHEMBL4635301 IC50 = 2700.0 nM 5.57
CHEMBL4636574 IC50 = 2900.0 nM 5.54
CHEMBL4632414 IC50 = 3900.0 nM 5.41
CHEMBL4634916 IC50 = 10500.0 nM 4.98
CHEMBL4633201 IC50 = 12000.0 nM 4.92
CHEMBL4645057 IC50 = 13000.0 nM 4.89
CHEMBL4637072 IC50 = 21000.0 nM 4.68