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Assay Detail

CHEMBL5583228

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

Binding
Inhibition of recombinant LSD1 (unknown origin) expressed in BL21(DE3) cells using H3K4me2 as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by microplate reader assay
ChEMBL ↗
54
Total Activities
54
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

Discovery of 2-Aryl-4-aminoquinazolin-Based LSD1 Inhibitors to Activate Immune Response in Gastric Cancer.
Wang B, Wang SW, Zhou Y, Wang SP, Gao Y, Liu HM, Ji SK, Wang SQ, Zheng YC, Zhang C, Mardinoglu A, Liu HM, Chen XB, Dai XJ.
J Med Chem (2024) 67 : 16165 -16184
PubMed 39264726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 6.22 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5593371 — — 1 7.89
CHEMBL3781751 IADADEMSTAT 2.0 1 7.68
CHEMBL5593512 — — 1 6.97
CHEMBL5593145 — — 1 6.95
CHEMBL5595400 — — 1 6.84
CHEMBL5593849 — — 1 6.81
CHEMBL5595354 — — 1 6.79
CHEMBL5594750 — — 1 6.76
CHEMBL5584197 — — 1 6.72
CHEMBL602537 — — 1 6.69
CHEMBL5592214 — — 1 6.63
CHEMBL5590047 — — 1 6.58
CHEMBL5590236 — — 1 6.58
CHEMBL5592342 — — 1 6.57
CHEMBL5593414 — — 1 6.55
CHEMBL5590716 — — 1 6.45
CHEMBL5595228 — — 1 6.45
CHEMBL5589850 — — 1 6.38
CHEMBL5594683 — — 1 6.37
CHEMBL5592912 — — 1 6.32
CHEMBL5592106 — — 1 6.29
CHEMBL5593673 — — 1 6.28
CHEMBL5595945 — — 1 6.25
CHEMBL5590453 — — 1 6.21
CHEMBL5592035 — — 1 6.21
CHEMBL5592972 — — 1 6.19
CHEMBL5593380 — — 1 6.18
CHEMBL5592286 — — 1 6.15
CHEMBL5593386 — — 1 6.14
CHEMBL5594210 — — 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5593371 — IC50 = 13.0 nM 7.89
CHEMBL3781751 IADADEMSTAT IC50 = 21.0 nM 7.68
CHEMBL5593512 — IC50 = 108.0 nM 6.97
CHEMBL5593145 — IC50 = 113.0 nM 6.95
CHEMBL5595400 — IC50 = 145.0 nM 6.84
CHEMBL5593849 — IC50 = 156.0 nM 6.81
CHEMBL5595354 — IC50 = 161.0 nM 6.79
CHEMBL5594750 — IC50 = 174.0 nM 6.76
CHEMBL5584197 — IC50 = 192.0 nM 6.72
CHEMBL602537 — IC50 = 203.0 nM 6.69
CHEMBL5592214 — IC50 = 236.0 nM 6.63
CHEMBL5590047 — IC50 = 261.0 nM 6.58
CHEMBL5590236 — IC50 = 265.0 nM 6.58
CHEMBL5592342 — IC50 = 272.0 nM 6.57
CHEMBL5593414 — IC50 = 284.0 nM 6.55
CHEMBL5590716 — IC50 = 359.0 nM 6.45
CHEMBL5595228 — IC50 = 352.0 nM 6.45
CHEMBL5589850 — IC50 = 418.0 nM 6.38
CHEMBL5594683 — IC50 = 431.0 nM 6.37
CHEMBL5592912 — IC50 = 476.0 nM 6.32
CHEMBL5592106 — IC50 = 513.0 nM 6.29
CHEMBL5593673 — IC50 = 521.0 nM 6.28
CHEMBL5595945 — IC50 = 569.0 nM 6.25
CHEMBL5590453 — IC50 = 620.0 nM 6.21
CHEMBL5592035 — IC50 = 616.0 nM 6.21
CHEMBL5592972 — IC50 = 650.0 nM 6.19
CHEMBL5593380 — IC50 = 666.0 nM 6.18
CHEMBL5592286 — IC50 = 715.0 nM 6.15
CHEMBL5593386 — IC50 = 728.0 nM 6.14
CHEMBL5594210 — IC50 = 728.0 nM 6.14
CHEMBL5583974 — IC50 = 776.0 nM 6.11
CHEMBL5590454 — IC50 = 855.0 nM 6.07
CHEMBL5595125 — IC50 = 864.0 nM 6.06
CHEMBL5592535 — IC50 = 1273.0 nM 5.89
CHEMBL5593356 — IC50 = 1301.0 nM 5.89
CHEMBL5593977 — IC50 = 1494.0 nM 5.83
CHEMBL5593985 — IC50 = 1604.0 nM 5.79
CHEMBL5592113 — IC50 = 1727.0 nM 5.76
CHEMBL5594365 — IC50 = 2563.0 nM 5.59
CHEMBL5592458 — IC50 = 2608.0 nM 5.58
CHEMBL5593562 — IC50 = 2949.0 nM 5.53
CHEMBL5595372 — IC50 = 3190.0 nM 5.50
CHEMBL5595614 — IC50 = 3174.0 nM 5.50
CHEMBL5594371 — IC50 = 4536.0 nM 5.34
CHEMBL5593682 — IC50 = 6192.0 nM 5.21
CHEMBL5595436 — IC50 = 7772.0 nM 5.11
CHEMBL553 ERLOTINIB IC50 = 35800.0 nM 4.45
CHEMBL5590932 — IC50 > 10000.0 nM -
CHEMBL5591619 — IC50 = 234000.0 nM -
CHEMBL5592039 — IC50 > 10000.0 nM -