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Assay Detail

CHEMBL2378715

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

Binding
Inhibition of human methionine aminopeptidase 1 in presence of Mn2+
32
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
Zhang F, Bhat S, Gabelli SB, Chen X, Miller MS, Nacev BA, Cheng YL, Meyers DJ, Tenney K, Shim JS, Crews P, Amzel LM, Ma D, Liu JO.
J Med Chem (2013) 56 : 3996 -4016
PubMed 23634668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 5.07 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2375609 1 5.47
CHEMBL2375621 1 5.43
CHEMBL2375610 1 5.32
CHEMBL2375622 1 5.32
CHEMBL2375607 1 5.30
CHEMBL2375624 1 5.29
CHEMBL2375612 1 5.28
CHEMBL2375613 1 5.12
CHEMBL2375608 1 5.10
CHEMBL2375620 1 5.09
CHEMBL2375615 1 5.08
CHEMBL2375618 1 4.96
CHEMBL472879 1 4.82
CHEMBL2375616 1 4.82
CHEMBL2375623 1 4.77
CHEMBL1518085 1 4.62
CHEMBL1329554 1 4.39
CHEMBL39879 DIPYRIDYL 1 -
CHEMBL327579 2 -
CHEMBL2375627 1 -
CHEMBL2375626 1 -
CHEMBL2375625 1 -
CHEMBL2375628 1 -
CHEMBL2375629 1 -
CHEMBL2375611 1 -
CHEMBL2375619 1 -
CHEMBL2375617 1 -
CHEMBL625 THIABENDAZOLE 4.0 1 -
CHEMBL49678 1 -
CHEMBL45721 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2375609 EC50 = 3400.0 nM 5.47
CHEMBL2375621 EC50 = 3700.0 nM 5.43
CHEMBL2375610 EC50 = 4800.0 nM 5.32
CHEMBL2375622 EC50 = 4800.0 nM 5.32
CHEMBL2375607 EC50 = 5000.0 nM 5.30
CHEMBL2375624 EC50 = 5100.0 nM 5.29
CHEMBL2375612 EC50 = 5300.0 nM 5.28
CHEMBL2375613 EC50 = 7600.0 nM 5.12
CHEMBL2375608 EC50 = 8000.0 nM 5.10
CHEMBL2375620 EC50 = 8100.0 nM 5.09
CHEMBL2375615 EC50 = 8400.0 nM 5.08
CHEMBL2375618 EC50 = 11000.0 nM 4.96
CHEMBL2375616 EC50 = 15000.0 nM 4.82
CHEMBL472879 EC50 = 15000.0 nM 4.82
CHEMBL2375623 EC50 = 17000.0 nM 4.77
CHEMBL1518085 EC50 = 24000.0 nM 4.62
CHEMBL1329554 EC50 = 41000.0 nM 4.39
CHEMBL2375626 EC50 > 100000.0 nM -
CHEMBL2375625 EC50 > 100000.0 nM -
CHEMBL625 THIABENDAZOLE EC50 > 100000.0 nM -
CHEMBL327579 EC50 > 100000.0 nM -
CHEMBL2375619 EC50 > 400000.0 nM -
CHEMBL2375617 EC50 > 100000.0 nM -
CHEMBL49678 EC50 > 100000.0 nM -
CHEMBL45721 EC50 > 100000.0 nM -
CHEMBL2375614 EC50 > 100000.0 nM -
CHEMBL2375611 EC50 > 100000.0 nM -
CHEMBL2375629 EC50 > 100000.0 nM -
CHEMBL2375628 EC50 > 200000.0 nM -
CHEMBL2375627 EC50 > 100000.0 nM -
CHEMBL327579 EC50 > 100000.0 nM -
CHEMBL39879 DIPYRIDYL EC50 > 100000.0 nM -