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Assay Detail

CHEMBL5650085

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

Binding
Inhibition of recombinant human 6His-(Tev)-G-SUV420H1 (69 to 335 residues) using Biotin-tagged H4K20me1 and [3H-SAM] as substrate incubated for 2 hrs by scintillation proximity assay
6
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone-lysine N-methyltransferase KMT5B (CHEMBL2321645)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity.
Bromberg KD, Mitchell TR, Upadhyay AK, Jakob CG, Jhala MA, Comess KM, Lasko LM, Li C, Tuzon CT, Dai Y, Li F, Eram MS, Nuber A, Soni NB, Manaves V, Algire MA, Sweis RF, Torrent M, Schotta G, Sun C, Michaelides MR, Shoemaker AR, Arrowsmith CH, Brown PJ, Santhakumar V, Martin A, Rice JC, Chiang GG, Vedadi M, Barsyte-Lovejoy D, Pappano WN.
Nat Chem Biol (2017) 13 : 317 -324
PubMed 28114273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.67 7.60
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4521971 2 7.60
CHEMBL5653590 1 6.23
CHEMBL1288796 1 5.23
CHEMBL5653592 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4521971 IC50 = 25.0 nM 7.60
CHEMBL4521971 IC50 = 25.0 nM 7.60
CHEMBL5653590 IC50 = 590.0 nM 6.23
CHEMBL1288796 IC50 = 5900.0 nM 5.23
CHEMBL5653592 IC50 > 10000.0 nM -
CHEMBL5653592 Inhibition - % -