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Assay Detail

CHEMBL5737876

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

Binding
Biochemical Inhibition Activity Assay: The biochemical inhibition activity of the synthesized compounds on LSD1 was measured. The activity measurement was performed using LSD1 fluorescence analysis kit (available from BPS Bioscience Co., Ltd., Catalog No: 50106). This analysis kit is designed to measure activity of LSD1 enzyme. H2O2 generated upon demethylation of Lys4 moiety of histone H3 by LSD1 is reacted with HRP/Amplex Red reagent to form fluorescent Resorufin, which is measured by this kit, thereby confirming demethylation.
ChEMBL ↗
216
Total Activities
72
Compounds Tested
3
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

Pyrazole derivative compound and use thereof
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 72 7.14 7.70
kon 72 - -
k_off 72 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6048582 — — 3 7.70
CHEMBL6026376 — — 3 7.68
CHEMBL5930152 — — 3 7.68
CHEMBL5990101 — — 3 7.68
CHEMBL5866802 — — 3 7.68
CHEMBL5794835 — — 3 7.66
CHEMBL5962997 — — 3 7.64
CHEMBL5756245 — — 3 7.58
CHEMBL5947633 — — 3 7.58
CHEMBL5742198 — — 3 7.55
CHEMBL5808028 — — 3 7.55
CHEMBL6063153 — — 3 7.55
CHEMBL5909198 — — 3 7.55
CHEMBL5900560 — — 3 7.54
CHEMBL5805027 — — 3 7.52
CHEMBL5815453 — — 3 7.48
CHEMBL5975792 — — 3 7.48
CHEMBL6058079 — — 3 7.47
CHEMBL6020247 — — 3 7.47
CHEMBL6004627 — — 3 7.47
CHEMBL5797077 — — 3 7.46
CHEMBL6044720 — — 3 7.46
CHEMBL5752799 — — 3 7.44
CHEMBL5761631 — — 3 7.44
CHEMBL6063932 — — 3 7.44
CHEMBL5798005 — — 3 7.42
CHEMBL5855229 — — 3 7.42
CHEMBL6001987 — — 3 7.40
CHEMBL5913375 — — 3 7.39
CHEMBL5773119 — — 3 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6048582 — IC50 = 20.0 nM 7.70
CHEMBL6026376 — IC50 = 21.0 nM 7.68
CHEMBL5866802 — IC50 = 21.0 nM 7.68
CHEMBL5930152 — IC50 = 21.0 nM 7.68
CHEMBL5990101 — IC50 = 21.0 nM 7.68
CHEMBL5794835 — IC50 = 22.0 nM 7.66
CHEMBL5962997 — IC50 = 23.0 nM 7.64
CHEMBL5947633 — IC50 = 26.0 nM 7.58
CHEMBL5756245 — IC50 = 26.0 nM 7.58
CHEMBL5742198 — IC50 = 28.0 nM 7.55
CHEMBL5808028 — IC50 = 28.0 nM 7.55
CHEMBL6063153 — IC50 = 28.0 nM 7.55
CHEMBL5909198 — IC50 = 28.0 nM 7.55
CHEMBL5900560 — IC50 = 29.0 nM 7.54
CHEMBL5805027 — IC50 = 30.0 nM 7.52
CHEMBL5975792 — IC50 = 33.0 nM 7.48
CHEMBL5815453 — IC50 = 33.0 nM 7.48
CHEMBL6058079 — IC50 = 34.0 nM 7.47
CHEMBL6020247 — IC50 = 34.0 nM 7.47
CHEMBL6004627 — IC50 = 34.0 nM 7.47
CHEMBL5797077 — IC50 = 35.0 nM 7.46
CHEMBL6044720 — IC50 = 35.0 nM 7.46
CHEMBL6063932 — IC50 = 36.0 nM 7.44
CHEMBL5761631 — IC50 = 36.0 nM 7.44
CHEMBL5752799 — IC50 = 36.0 nM 7.44
CHEMBL5798005 — IC50 = 38.0 nM 7.42
CHEMBL5855229 — IC50 = 38.0 nM 7.42
CHEMBL6001987 — IC50 = 40.0 nM 7.40
CHEMBL5913375 — IC50 = 41.0 nM 7.39
CHEMBL5773119 — IC50 = 41.0 nM 7.39
CHEMBL6020669 — IC50 = 42.0 nM 7.38
CHEMBL5888204 — IC50 = 44.0 nM 7.36
CHEMBL5829443 — IC50 = 46.0 nM 7.34
CHEMBL6047765 — IC50 = 46.0 nM 7.34
CHEMBL5887308 — IC50 = 46.0 nM 7.34
CHEMBL5892798 — IC50 = 46.0 nM 7.34
CHEMBL6064953 — IC50 = 47.0 nM 7.33
CHEMBL5925626 — IC50 = 48.0 nM 7.32
CHEMBL6008249 — IC50 = 49.0 nM 7.31
CHEMBL5889960 — IC50 = 53.0 nM 7.28
CHEMBL5797867 — IC50 = 55.0 nM 7.26
CHEMBL6006242 — IC50 = 56.0 nM 7.25
CHEMBL5847150 — IC50 = 56.0 nM 7.25
CHEMBL5801034 — IC50 = 57.0 nM 7.24
CHEMBL6050461 — IC50 = 61.0 nM 7.21
CHEMBL5935847 — IC50 = 67.0 nM 7.17
CHEMBL5945639 — IC50 = 70.0 nM 7.16
CHEMBL5939564 — IC50 = 87.0 nM 7.06
CHEMBL5752802 — IC50 = 100.0 nM 7.00
CHEMBL5779492 — IC50 = 125.0 nM 6.90