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Assay Detail

CHEMBL3865474

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

Binding
Competitive inhibition of SETD8 (unknown origin) using biotin-labeled H4 (1 to 24 residues) as substrate after 1 hr in presence of varying levels of [3H]SAM by Lineweaver-Burk plot analysis
1
Total Activities
1
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-lysine methyltransferase KMT5A (CHEMBL1795176)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8.
Judge RA, Zhu H, Upadhyay AK, Bodelle PM, Hutchins CW, Torrent M, Marin VL, Yu W, Vedadi M, Li F, Brown PJ, Pappano WN, Sun C, Petros AM.
ACS Med Chem Lett (2016) 7 : 1102 -1106
PubMed 27994746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.70 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3318284 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3318284 Ki = 2000.0 nM 5.70