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Assay Detail

CHEMBL4370539

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Binding
Inhibition of full length human menin/FAM-tagged MLL1 (unknown origin) protein-protein interaction after 15 mins by fluorescence polarization assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Menin/Histone-lysine N-methyltransferase MLL (CHEMBL2093861)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.
Wang X, Su M, Li Y, Liu T, Wang Y, Chen Y, Tang L, He YP, Ding X, Yu F, Shen J, Li J, Zhou Y, Chen YL, Xiong B.
Bioorg Med Chem Lett (2019) 29 : 844 -847
PubMed 30713023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.96 6.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3586090 1 6.93
CHEMBL4533143 1 5.67
CHEMBL4442317 1 4.99
CHEMBL4580675 1 4.76
CHEMBL4530202 1 4.61
CHEMBL4593261 1 4.51
CHEMBL4526830 1 4.46
CHEMBL4474185 1 4.43
CHEMBL4437554 1 4.29
CHEMBL3786182 GSK2879552 1.0 1 -
CHEMBL3989843 TRANYLCYPROMINE 4.0 1 -
CHEMBL4440500 1 -
CHEMBL4569986 1 -
CHEMBL4447074 1 -
CHEMBL4589914 1 -
CHEMBL4520948 1 -
CHEMBL4550942 1 -
CHEMBL4558443 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3586090 IC50 = 118.3 nM 6.93
CHEMBL4533143 IC50 = 2130.0 nM 5.67
CHEMBL4442317 IC50 = 10240.0 nM 4.99
CHEMBL4580675 IC50 = 17330.0 nM 4.76
CHEMBL4530202 IC50 = 24730.0 nM 4.61
CHEMBL4593261 IC50 = 30940.0 nM 4.51
CHEMBL4526830 IC50 = 34540.0 nM 4.46
CHEMBL4474185 IC50 = 36930.0 nM 4.43
CHEMBL4437554 IC50 = 50750.0 nM 4.29
CHEMBL3786182 GSK2879552 IC50 - -
CHEMBL3989843 TRANYLCYPROMINE IC50 - -
CHEMBL4440500 IC50 > 100000.0 nM -
CHEMBL4569986 IC50 > 100000.0 nM -
CHEMBL4447074 IC50 > 100000.0 nM -
CHEMBL4589914 IC50 > 100000.0 nM -
CHEMBL4520948 IC50 > 100000.0 nM -
CHEMBL4550942 IC50 > 100000.0 nM -
CHEMBL4558443 IC50 > 100000.0 nM -