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Assay Detail

CHEMBL4353693

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

Binding
Inhibition of KDM3A (unknown origin) by Alphascreen assay
6
Total Activities
6
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

Lysine-specific demethylase 3A (CHEMBL1938209)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.
Le Bihan YV, Lanigan RM, Atrash B, McLaughlin MG, Velupillai S, Malcolm AG, England KS, Ruda GF, Mok NY, Tumber A, Tomlin K, Saville H, Shehu E, McAndrew C, Carmichael L, Bennett JM, Jeganathan F, Eve P, Donovan A, Hayes A, Wood F, Raynaud FI, Fedorov O, Brennan PE, Burke R, van Montfort RLM, Rossanese OW, Blagg J, Bavetsias V.
Eur J Med Chem (2019) 177 : 316 -337
PubMed 31158747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.39 5.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4592908 1 5.73
CHEMBL4585876 1 5.70
CHEMBL4516101 1 5.25
CHEMBL4449500 1 5.24
CHEMBL4525269 1 5.21
CHEMBL4447515 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4592908 IC50 = 1850.0 nM 5.73
CHEMBL4585876 IC50 = 2020.0 nM 5.70
CHEMBL4516101 IC50 = 5680.0 nM 5.25
CHEMBL4449500 IC50 = 5780.0 nM 5.24
CHEMBL4525269 IC50 = 6130.0 nM 5.21
CHEMBL4447515 IC50 = 6420.0 nM 5.19