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Assay Detail

CHEMBL828603

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Binding
Inhibitory concentration against ScMetAP1 enzyme activity
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Saccharomyces cerevisiae
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Methionine aminopeptidase 1 (CHEMBL2526)
Type SINGLE PROTEIN
Organism Saccharomyces cerevisiae S288c

Publication

Identification of potent type I MetAPs inhibitors by simple bioisosteric replacement. Part 2: SAR studies of 5-heteroalkyl substituted TCAT derivatives.
Cui YM, Huang QQ, Xu J, Chen LL, Li JY, Ye QZ, Li J, Nan FJ.
Bioorg Med Chem Lett (2005) 15 : 4130 -4135
PubMed 16005224 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.01 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188263 1 7.12
CHEMBL363943 1 6.82
CHEMBL426802 1 6.64
CHEMBL189688 1 6.57
CHEMBL188976 1 6.51
CHEMBL363299 1 6.47
CHEMBL188845 1 6.46
CHEMBL441389 1 6.41
CHEMBL190357 1 6.40
CHEMBL188429 1 6.39
CHEMBL365192 1 6.36
CHEMBL361480 1 6.35
CHEMBL189619 1 6.35
CHEMBL186028 1 6.35
CHEMBL364821 1 6.30
CHEMBL179919 1 6.30
CHEMBL361307 1 6.28
CHEMBL189127 1 6.26
CHEMBL371393 1 6.24
CHEMBL362123 1 6.24
CHEMBL190342 1 6.12
CHEMBL363875 1 6.10
CHEMBL178091 1 6.06
CHEMBL362937 1 5.81
CHEMBL188053 1 5.75
CHEMBL175540 1 5.65
CHEMBL188575 1 5.51
CHEMBL188195 1 5.49
CHEMBL188796 1 5.43
CHEMBL190195 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188263 IC50 = 75.0 nM 7.12
CHEMBL363943 IC50 = 150.0 nM 6.82
CHEMBL426802 IC50 = 230.0 nM 6.64
CHEMBL189688 IC50 = 270.0 nM 6.57
CHEMBL188976 IC50 = 310.0 nM 6.51
CHEMBL363299 IC50 = 340.0 nM 6.47
CHEMBL188845 IC50 = 350.0 nM 6.46
CHEMBL441389 IC50 = 390.0 nM 6.41
CHEMBL190357 IC50 = 400.0 nM 6.40
CHEMBL188429 IC50 = 410.0 nM 6.39
CHEMBL365192 IC50 = 440.0 nM 6.36
CHEMBL361480 IC50 = 450.0 nM 6.35
CHEMBL189619 IC50 = 450.0 nM 6.35
CHEMBL186028 IC50 = 450.0 nM 6.35
CHEMBL179919 IC50 = 500.0 nM 6.30
CHEMBL364821 IC50 = 500.0 nM 6.30
CHEMBL361307 IC50 = 520.0 nM 6.28
CHEMBL189127 IC50 = 550.0 nM 6.26
CHEMBL371393 IC50 = 570.0 nM 6.24
CHEMBL362123 IC50 = 570.0 nM 6.24
CHEMBL190342 IC50 = 750.0 nM 6.12
CHEMBL363875 IC50 = 800.0 nM 6.10
CHEMBL178091 IC50 = 880.0 nM 6.06
CHEMBL362937 IC50 = 1560.0 nM 5.81
CHEMBL188053 IC50 = 1760.0 nM 5.75
CHEMBL175540 IC50 = 2260.0 nM 5.65
CHEMBL188575 IC50 = 3080.0 nM 5.51
CHEMBL188195 IC50 = 3210.0 nM 5.49
CHEMBL188796 IC50 = 3720.0 nM 5.43
CHEMBL190195 IC50 = 4250.0 nM 5.37
CHEMBL366071 IC50 = 6040.0 nM 5.22
CHEMBL365566 IC50 = 6430.0 nM 5.19
CHEMBL89671 IC50 = 7000.0 nM 5.16
CHEMBL365124 IC50 = 7530.0 nM 5.12
CHEMBL365225 IC50 = 10390.0 nM 4.98
CHEMBL188759 IC50 = 17920.0 nM 4.75