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Assay Detail

CHEMBL1173893

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

Binding
Inhibition of human MetAP2 expressed in baculovirus infected Sf9 cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Subtype-selectivity of metal-dependent methionine aminopeptidase inhibitors.
Altmeyer MA, Marschner A, Schiffmann R, Klein CD.
Bioorg Med Chem Lett (2010) 20 : 4038 -4044
PubMed 20621724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.64 5.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310555 OXYQUINOLINE -1.0 1 5.25
CHEMBL352049 1 5.11
CHEMBL202826 1 5.10
CHEMBL199925 1 5.03
CHEMBL370420 1 5.00
CHEMBL72683 1 4.88
CHEMBL199982 1 4.83
CHEMBL166127 1 4.74
CHEMBL372564 1 4.61
CHEMBL89671 1 4.59
CHEMBL371481 1 4.57
CHEMBL370581 1 4.55
CHEMBL371956 1 4.55
CHEMBL200059 1 4.48
CHEMBL199806 1 4.48
CHEMBL1170610 BENZOXIQUINE 2.0 1 4.46
CHEMBL371544 1 4.44
CHEMBL370580 1 4.42
CHEMBL257286 1 4.40
CHEMBL199448 1 4.39
CHEMBL1169657 1 4.38
CHEMBL198342 1 4.36
CHEMBL625 THIABENDAZOLE 4.0 1 4.35
CHEMBL201143 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310555 OXYQUINOLINE IC50 = 5600.0 nM 5.25
CHEMBL352049 IC50 = 7700.0 nM 5.11
CHEMBL202826 IC50 = 8000.0 nM 5.10
CHEMBL199925 IC50 = 9300.0 nM 5.03
CHEMBL370420 IC50 = 10100.0 nM 5.00
CHEMBL72683 IC50 = 13300.0 nM 4.88
CHEMBL199982 IC50 = 14900.0 nM 4.83
CHEMBL166127 IC50 = 18100.0 nM 4.74
CHEMBL372564 IC50 = 24300.0 nM 4.61
CHEMBL89671 IC50 = 25800.0 nM 4.59
CHEMBL371481 IC50 = 26700.0 nM 4.57
CHEMBL370581 IC50 = 28000.0 nM 4.55
CHEMBL371956 IC50 = 28400.0 nM 4.55
CHEMBL200059 IC50 = 32900.0 nM 4.48
CHEMBL199806 IC50 = 32900.0 nM 4.48
CHEMBL1170610 BENZOXIQUINE IC50 = 34800.0 nM 4.46
CHEMBL371544 IC50 = 36400.0 nM 4.44
CHEMBL370580 IC50 = 38400.0 nM 4.42
CHEMBL257286 IC50 = 39800.0 nM 4.40
CHEMBL199448 IC50 = 40600.0 nM 4.39
CHEMBL1169657 IC50 = 41700.0 nM 4.38
CHEMBL198342 IC50 = 44100.0 nM 4.36
CHEMBL625 THIABENDAZOLE IC50 = 44700.0 nM 4.35
CHEMBL201143 IC50 = 48400.0 nM 4.32