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Assay Detail

CHEMBL3776539

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

Binding
Inhibition of full length N-terminal His-tagged human LSD2 (1 to 822 residues) expressed in Escherichia coli BL21(DE3) cells using H3K4me2 peptide substrate by MALDI-TOF mass spectrometric analysis
8
Total Activities
8
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 histone demethylase 2 (CHEMBL1938208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of SNAIL1 Peptide-Based Irreversible Lysine-Specific Demethylase 1-Selective Inactivators.
Itoh Y, Aihara K, Mellini P, Tojo T, Ota Y, Tsumoto H, Solomon VR, Zhan P, Suzuki M, Ogasawara D, Shigenaga A, Inokuma T, Nakagawa H, Miyata N, Mizukami T, Otaka A, Suzuki T.
J Med Chem (2016) 59 : 1531 -1544
PubMed 26700437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.88 5.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4299307 1 5.12
CHEMBL4299324 1 4.88
CHEMBL4299278 1 4.63
CHEMBL4299336 1 -
CHEMBL4299338 1 -
CHEMBL4299285 1 -
CHEMBL4299296 1 -
CHEMBL4299323 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4299307 IC50 = 7510.0 nM 5.12
CHEMBL4299324 IC50 = 13200.0 nM 4.88
CHEMBL4299278 IC50 = 23200.0 nM 4.63
CHEMBL4299336 IC50 - -
CHEMBL4299338 IC50 > 50000.0 nM -
CHEMBL4299285 IC50 > 50000.0 nM -
CHEMBL4299296 IC50 - -
CHEMBL4299323 IC50 - -