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Assay Detail

CHEMBL4042258

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Functional
Cytotoxicity against human A549 cells assessed as growth inhibition by MTT assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A549
Confidence 1 — Organism
Curated By Autocuration

Target

A549 (CHEMBL392)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors.
Wang S, Zhao LJ, Zheng YC, Shen DD, Miao EF, Qiao XP, Zhao LJ, Liu Y, Huang R, Yu B, Liu HM.
Eur J Med Chem (2017) 125 : 940 -951
PubMed 27769034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.87 5.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4091439 1 5.06
CHEMBL4087815 1 5.05
CHEMBL4069335 1 5.05
CHEMBL2177862 1 5.01
CHEMBL4070519 1 5.00
CHEMBL4089024 1 4.99
CHEMBL185 FLUOROURACIL 4.0 1 4.86
CHEMBL4099168 1 4.86
CHEMBL4067124 1 4.79
CHEMBL4080060 1 4.79
CHEMBL4060712 1 4.77
CHEMBL4083660 1 4.76
CHEMBL4060820 1 4.75
CHEMBL4061895 1 4.70
CHEMBL4101839 1 4.64
CHEMBL4099019 1 -
CHEMBL3786182 GSK2879552 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4091439 IC50 = 8790.0 nM 5.06
CHEMBL4087815 IC50 = 8870.0 nM 5.05
CHEMBL4069335 IC50 = 8850.0 nM 5.05
CHEMBL2177862 IC50 = 9740.0 nM 5.01
CHEMBL4070519 IC50 = 9900.0 nM 5.00
CHEMBL4089024 IC50 = 10340.0 nM 4.99
CHEMBL185 FLUOROURACIL IC50 = 13950.0 nM 4.86
CHEMBL4099168 IC50 = 13880.0 nM 4.86
CHEMBL4067124 IC50 = 16410.0 nM 4.79
CHEMBL4080060 IC50 = 16100.0 nM 4.79
CHEMBL4060712 IC50 = 17030.0 nM 4.77
CHEMBL4083660 IC50 = 17500.0 nM 4.76
CHEMBL4060820 IC50 = 17960.0 nM 4.75
CHEMBL4061895 IC50 = 19770.0 nM 4.70
CHEMBL4101839 IC50 = 22760.0 nM 4.64
CHEMBL4099019 IC50 - -
CHEMBL3786182 GSK2879552 IC50 - -