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Assay Detail

CHEMBL4404753

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

Binding
Inhibition of recombinant KAT6A (unknown origin) expressed in C57BL/6 mouse embryonic fibroblasts assessed as reduction in cell proliferation supplemented with fresh medium containing compounds every 48 hrs after for 168 hrs under low oxygen condition
9
Total Activities
9
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

Histone acetyltransferase KAT6A (CHEMBL3774298)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents.
Priebbenow DL, Leaver DJ, Nguyen N, Cleary B, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Shackleford DM, Katneni K, Cuellar M, Strasser JM, Dahlin JL, Walters MA, Street IP, Monahan BJ, Jarman KE, Jousset Sabroux H, Falk H, Chung MC, Hermans SJ, Downer NL, Parker MW, Voss AK, Thomas T, Baell JB.
J Med Chem (2020) 63 : 4655 -4684
PubMed 32118427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.13 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4451170 1 6.32
CHEMBL4455897 1 6.26
CHEMBL4461380 1 6.21
CHEMBL4449359 1 6.20
CHEMBL4445093 1 6.19
CHEMBL4464911 1 6.00
CHEMBL4446917 1 5.93
CHEMBL4566403 1 5.90
CHEMBL4513522 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4451170 IC50 = 480.0 nM 6.32
CHEMBL4455897 IC50 = 551.0 nM 6.26
CHEMBL4461380 IC50 = 610.0 nM 6.21
CHEMBL4449359 IC50 = 630.0 nM 6.20
CHEMBL4445093 IC50 = 650.0 nM 6.19
CHEMBL4464911 IC50 = 990.0 nM 6.00
CHEMBL4446917 IC50 = 1170.0 nM 5.93
CHEMBL4566403 IC50 = 1260.0 nM 5.90
CHEMBL4513522 IC50 > 10000.0 nM -