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Assay Detail

CHEMBL4722525

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

ADMET
Inhibition of human MetAP1 expressed in Escherichia coli BL21 (DE3) using L-methionine-4-methyl-coumary1-7-amide as substrate preincubated for 30 mins followed by substrate addition and measured at 1 min interval for 30 mins by spectrofluorometric method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Methionine aminopeptidase 1 (CHEMBL2474)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and characterization of quinoline-carbaldehyde derivatives as novel inhibitors for leishmanial methionine aminopeptidase 1.
Bhat SY,Jagruthi P,Srinivas A,Arifuddin M,Qureshi IA
Eur J Med Chem (2020) 186 : 111860 -111860
PubMed 31759728 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.63 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4740594 1 5.05
CHEMBL4783117 1 4.96
CHEMBL4758588 1 4.90
CHEMBL4741746 1 4.21
CHEMBL4743353 1 4.01
CHEMBL4759464 1 -
CHEMBL4764436 1 -
CHEMBL4745980 1 -
CHEMBL4749821 1 -
CHEMBL4784882 1 -
CHEMBL4743733 1 -
CHEMBL4755128 1 -
CHEMBL4795438 1 -
CHEMBL4777085 1 -
CHEMBL4785449 1 -
CHEMBL4752621 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4740594 IC50 = 8900.0 nM 5.05
CHEMBL4783117 IC50 = 10940.0 nM 4.96
CHEMBL4758588 IC50 = 12580.0 nM 4.90
CHEMBL4741746 IC50 = 61400.0 nM 4.21
CHEMBL4743353 IC50 = 98700.0 nM 4.01
CHEMBL4759464 IC50 = 126800.0 nM -
CHEMBL4764436 IC50 = 174600.0 nM -
CHEMBL4745980 IC50 = 112700.0 nM -
CHEMBL4749821 IC50 = 104200.0 nM -
CHEMBL4784882 IC50 = 127500.0 nM -
CHEMBL4743733 IC50 = 284000.0 nM -
CHEMBL4755128 IC50 = 217200.0 nM -
CHEMBL4795438 IC50 = 107000.0 nM -
CHEMBL4777085 IC50 = 116100.0 nM -
CHEMBL4785449 IC50 = 143000.0 nM -
CHEMBL4752621 IC50 = 104700.0 nM -