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Assay Detail

CHEMBL5136953

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Toxicity
Inhibition of human ERG by fluorescence polarization assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Structure-Activity Relationship and <i>In Silico</i> Evaluation of <i>cis</i>- and <i>trans</i>-PCPA-Derived Inhibitors of LSD1 and LSD2.
Niwa H, Watanabe C, Sato S, Harada T, Watanabe H, Tabusa R, Fukasawa S, Shiobara A, Hashimoto T, Ohno O, Nakamura K, Tsuganezawa K, Tanaka A, Shirouzu M, Honma T, Matsuno K, Umehara T.
ACS Med Chem Lett (2022) 13 : 1485 -1492
PubMed 36105323 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.79 5.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5206551 1 5.14
CHEMBL5186086 1 5.11
CHEMBL4285048 1 4.89
CHEMBL5176392 1 4.82
CHEMBL5204816 1 4.80
CHEMBL5195724 1 4.75
CHEMBL5206853 1 4.46
CHEMBL5197683 1 4.36
CHEMBL5201156 1 -
CHEMBL5196815 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5206551 IC50 = 7300.0 nM 5.14
CHEMBL5186086 IC50 = 7700.0 nM 5.11
CHEMBL4285048 IC50 = 13000.0 nM 4.89
CHEMBL5176392 IC50 = 15000.0 nM 4.82
CHEMBL5204816 IC50 = 16000.0 nM 4.80
CHEMBL5195724 IC50 = 18000.0 nM 4.75
CHEMBL5206853 IC50 = 35000.0 nM 4.46
CHEMBL5197683 IC50 = 44000.0 nM 4.36
CHEMBL5201156 IC50 - -
CHEMBL5196815 IC50 - -