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Assay Detail

CHEMBL828659

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Binding
Inhibitory concentration against Escherichia coli methionine aminopeptidase 1
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Methionine aminopeptidase (CHEMBL3423)
Type SINGLE PROTEIN
Organism Escherichia coli K-12

Publication

Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1: SAR studies on the determination of the key scaffold.
Luo QL, Li JY, Liu ZY, Chen LL, Li J, Ye QZ, Nan FJ.
Bioorg Med Chem Lett (2005) 15 : 635 -638
PubMed 15664828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.58 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92374 1 6.58
CHEMBL313650 1 6.42
CHEMBL359929 1 6.00
CHEMBL315270 1 5.91
CHEMBL360513 1 5.85
CHEMBL183436 1 5.70
CHEMBL359541 1 5.68
CHEMBL183652 1 5.63
CHEMBL181349 1 5.35
CHEMBL183136 1 5.35
CHEMBL89671 1 5.30
CHEMBL360927 1 5.24
CHEMBL362218 1 5.24
CHEMBL183861 1 5.17
CHEMBL182901 1 5.04
CHEMBL179906 1 4.89
CHEMBL182954 1 -
CHEMBL183821 1 -
CHEMBL361849 1 -
CHEMBL361359 1 -
CHEMBL181520 1 -
CHEMBL183346 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92374 IC50 = 260.0 nM 6.58
CHEMBL313650 IC50 = 380.0 nM 6.42
CHEMBL359929 IC50 = 1010.0 nM 6.00
CHEMBL315270 IC50 = 1220.0 nM 5.91
CHEMBL360513 IC50 = 1410.0 nM 5.85
CHEMBL183436 IC50 = 1980.0 nM 5.70
CHEMBL359541 IC50 = 2090.0 nM 5.68
CHEMBL183652 IC50 = 2320.0 nM 5.63
CHEMBL181349 IC50 = 4510.0 nM 5.35
CHEMBL183136 IC50 = 4490.0 nM 5.35
CHEMBL89671 IC50 = 5000.0 nM 5.30
CHEMBL360927 IC50 = 5820.0 nM 5.24
CHEMBL362218 IC50 = 5820.0 nM 5.24
CHEMBL183861 IC50 = 6710.0 nM 5.17
CHEMBL182901 IC50 = 9220.0 nM 5.04
CHEMBL179906 IC50 = 12780.0 nM 4.89
CHEMBL182954 IC50 > 100000.0 nM -
CHEMBL183821 IC50 > 100000.0 nM -
CHEMBL361849 IC50 > 100000.0 nM -
CHEMBL361359 IC50 > 100000.0 nM -
CHEMBL181520 IC50 > 100000.0 nM -
CHEMBL183346 IC50 > 100000.0 nM -