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Assay Detail

CHEMBL4417039

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

Binding
Inhibition of MetAP2 in HUVEC assessed as reduction in viability incubated for 3 days by CyQUANT Direct Cell proliferation assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HUVEC
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Methionine aminopeptidase 2 (CHEMBL3922)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor M8891: A Clinical Compound for the Treatment of Cancer.
Heinrich T, Seenisamy J, Becker F, Blume B, Bomke J, Dietz M, Eckert U, Friese-Hamim M, Gunera J, Hansen K, Leuthner B, Musil D, Pfalzgraf J, Rohdich F, Siegl C, Spuck D, Wegener A, Zenke FT.
J Med Chem (2019) 62 : 11119 -11134
PubMed 31725285 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.04 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4572028 1 8.05
CHEMBL4463138 1 7.92
CHEMBL4591797 1 7.89
CHEMBL4445117 1 7.85
CHEMBL4553094 1 7.85
CHEMBL4475680 1 7.82
CHEMBL4550096 1 7.80
CHEMBL4448724 1 7.75
CHEMBL4464946 1 7.70
CHEMBL4460444 1 7.52
CHEMBL4448427 1 7.34
CHEMBL4551283 1 7.31
CHEMBL4451402 1 7.26
CHEMBL4547442 1 7.17
CHEMBL4450159 1 7.14
CHEMBL4460950 1 6.96
CHEMBL4522216 1 6.85
CHEMBL4570368 1 6.77
CHEMBL4454587 1 6.70
CHEMBL4458906 1 6.31
CHEMBL4566917 1 6.09
CHEMBL4441643 1 6.05
CHEMBL4575412 1 6.03
CHEMBL4444681 1 5.96
CHEMBL4473359 1 5.56
CHEMBL4470242 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4572028 IC50 = 9.0 nM 8.05
CHEMBL4463138 IC50 = 12.0 nM 7.92
CHEMBL4591797 IC50 = 13.0 nM 7.89
CHEMBL4445117 IC50 = 14.0 nM 7.85
CHEMBL4553094 IC50 = 14.0 nM 7.85
CHEMBL4475680 IC50 = 15.0 nM 7.82
CHEMBL4550096 IC50 = 16.0 nM 7.80
CHEMBL4448724 IC50 = 18.0 nM 7.75
CHEMBL4464946 IC50 = 20.0 nM 7.70
CHEMBL4460444 IC50 = 30.0 nM 7.52
CHEMBL4448427 IC50 = 46.0 nM 7.34
CHEMBL4551283 IC50 = 49.0 nM 7.31
CHEMBL4451402 IC50 = 55.0 nM 7.26
CHEMBL4547442 IC50 = 68.0 nM 7.17
CHEMBL4450159 IC50 = 72.0 nM 7.14
CHEMBL4460950 IC50 = 110.0 nM 6.96
CHEMBL4522216 IC50 = 140.0 nM 6.85
CHEMBL4570368 IC50 = 170.0 nM 6.77
CHEMBL4454587 IC50 = 200.0 nM 6.70
CHEMBL4458906 IC50 = 490.0 nM 6.31
CHEMBL4566917 IC50 = 809.0 nM 6.09
CHEMBL4441643 IC50 = 900.0 nM 6.05
CHEMBL4575412 IC50 = 930.0 nM 6.03
CHEMBL4444681 IC50 = 1100.0 nM 5.96
CHEMBL4473359 IC50 = 2757.0 nM 5.56
CHEMBL4470242 IC50 = 4300.0 nM 5.37