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Assay Detail

CHEMBL4047448

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

Binding
Binding affinity to LSD1 (unknown origin) by SPR analysis
19
Total Activities
19
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 1A (CHEMBL6136)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development and evaluation of 4-(pyrrolidin-3-yl)benzonitrile derivatives as inhibitors of lysine specific demethylase 1.
Mould DP, Bremberg U, Jordan AM, Geitmann M, McGonagle AE, Somervaille TCP, Spencer GJ, Ogilvie DJ.
Bioorg Med Chem Lett (2017) 27 : 4755 -4759
PubMed 28927796 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 19 6.38 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3134377 1 8.10
CHEMBL4071991 1 7.66
CHEMBL4066130 1 7.32
CHEMBL4100487 1 7.21
CHEMBL4092760 1 7.01
CHEMBL4087724 1 6.96
CHEMBL4082476 1 6.92
CHEMBL4105603 1 6.72
CHEMBL4079847 1 6.37
CHEMBL4079770 1 6.27
CHEMBL4097870 1 6.21
CHEMBL4074738 1 6.11
CHEMBL4063365 1 6.02
CHEMBL4101423 1 5.85
CHEMBL4085006 1 5.77
CHEMBL4093703 1 5.70
CHEMBL4104027 1 4.42
CHEMBL4066293 1 4.28
CHEMBL4087649 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3134377 Kd = 8.0 nM 8.10
CHEMBL4071991 Kd = 22.0 nM 7.66
CHEMBL4066130 Kd = 48.0 nM 7.32
CHEMBL4100487 Kd = 61.0 nM 7.21
CHEMBL4092760 Kd = 98.0 nM 7.01
CHEMBL4087724 Kd = 110.0 nM 6.96
CHEMBL4082476 Kd = 120.0 nM 6.92
CHEMBL4105603 Kd = 190.0 nM 6.72
CHEMBL4079847 Kd = 430.0 nM 6.37
CHEMBL4079770 Kd = 540.0 nM 6.27
CHEMBL4097870 Kd = 610.0 nM 6.21
CHEMBL4074738 Kd = 770.0 nM 6.11
CHEMBL4063365 Kd = 950.0 nM 6.02
CHEMBL4101423 Kd = 1400.0 nM 5.85
CHEMBL4085006 Kd = 1700.0 nM 5.77
CHEMBL4093703 Kd = 2000.0 nM 5.70
CHEMBL4104027 Kd = 38000.0 nM 4.42
CHEMBL4066293 Kd = 53000.0 nM 4.28
CHEMBL4087649 Kd > 100000.0 nM -