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Assay Detail

CHEMBL4397058

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Functional
Antiproliferative activity against HUVEC measured after 3 days by CyQUANT reagent-based fluorescence assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

HUVEC (CHEMBL613979)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery and Structure-Based Optimization of Next-Generation Reversible Methionine Aminopeptidase-2 (MetAP-2) Inhibitors.
Heinrich T, Seenisamy J, Blume B, Bomke J, Calderini M, Eckert U, Friese-Hamim M, Kohl R, Lehmann M, Leuthner B, Musil D, Rohdich F, Zenke FT.
J Med Chem (2019) 62 : 5025 -5039
PubMed 30939017 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.79 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4475680 1 7.82
CHEMBL4466601 1 7.50
CHEMBL4552396 1 7.00
CHEMBL4524329 1 6.77
CHEMBL4465025 1 6.62
CHEMBL4558399 1 6.60
CHEMBL4464652 1 6.55
CHEMBL4546986 1 6.52
CHEMBL4460784 1 6.51
CHEMBL4462995 1 6.46
CHEMBL4549484 1 5.82
CHEMBL4536649 1 5.80
CHEMBL4584721 1 5.80
CHEMBL4469817 1 5.77
CHEMBL4566670 1 5.72
CHEMBL4441859 1 5.60
CHEMBL4463329 1 5.54
CHEMBL4587873 1 5.40
CHEMBL4556036 1 5.28
CHEMBL4563305 1 5.28
CHEMBL4559822 1 5.21
CHEMBL4464827 1 5.05
CHEMBL4441472 1 5.01
CHEMBL4469283 1 4.82
CHEMBL4576078 1 4.77
CHEMBL4543409 1 4.75
CHEMBL4447796 1 4.75
CHEMBL4589384 1 4.75
CHEMBL4529723 1 4.54
CHEMBL4545625 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4475680 IC50 = 15.0 nM 7.82
CHEMBL4466601 IC50 = 32.0 nM 7.50
CHEMBL4552396 IC50 = 100.0 nM 7.00
CHEMBL4524329 IC50 = 170.0 nM 6.77
CHEMBL4465025 IC50 = 240.0 nM 6.62
CHEMBL4558399 IC50 = 250.0 nM 6.60
CHEMBL4464652 IC50 = 280.0 nM 6.55
CHEMBL4546986 IC50 = 300.0 nM 6.52
CHEMBL4460784 IC50 = 310.0 nM 6.51
CHEMBL4462995 IC50 = 350.0 nM 6.46
CHEMBL4549484 IC50 = 1500.0 nM 5.82
CHEMBL4536649 IC50 = 1600.0 nM 5.80
CHEMBL4584721 IC50 = 1600.0 nM 5.80
CHEMBL4469817 IC50 = 1700.0 nM 5.77
CHEMBL4566670 IC50 = 1900.0 nM 5.72
CHEMBL4441859 IC50 = 2500.0 nM 5.60
CHEMBL4463329 IC50 = 2900.0 nM 5.54
CHEMBL4587873 IC50 = 4000.0 nM 5.40
CHEMBL4556036 IC50 = 5200.0 nM 5.28
CHEMBL4563305 IC50 = 5200.0 nM 5.28
CHEMBL4559822 IC50 = 6100.0 nM 5.21
CHEMBL4464827 IC50 = 8900.0 nM 5.05
CHEMBL4441472 IC50 = 9700.0 nM 5.01
CHEMBL4469283 IC50 = 15000.0 nM 4.82
CHEMBL4576078 IC50 = 17000.0 nM 4.77
CHEMBL4543409 IC50 = 18000.0 nM 4.75
CHEMBL4447796 IC50 = 18000.0 nM 4.75
CHEMBL4589384 IC50 = 18000.0 nM 4.75
CHEMBL4529723 IC50 = 29000.0 nM 4.54
CHEMBL4545625 IC50 - -
CHEMBL4444678 IC50 - -
CHEMBL4438796 IC50 - -
CHEMBL4556838 IC50 - -
CHEMBL4572185 IC50 - -