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Assay Detail

CHEMBL4032434

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

Binding
Inhibition of human NMT1 using [3H]-myristoyl-coA/biotinylated CAP5.5 as substrate after 15 mins by scintillation/luminescence counting method
38
Total Activities
38
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

Glycylpeptide N-tetradecanoyltransferase 1 (CHEMBL2593)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.
Bayliss T, Robinson DA, Smith VC, Brand S, McElroy SP, Torrie LS, Mpamhanga C, Norval S, Stojanovski L, Brenk R, Frearson JA, Read KD, Gilbert IH, Wyatt PG.
J Med Chem (2017) 60 : 9790 -9806
PubMed 29125744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.55 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230468 1 8.40
CHEMBL3358120 1 8.30
CHEMBL4080376 1 8.00
CHEMBL3358114 1 7.92
CHEMBL4069661 1 7.52
CHEMBL4071314 1 7.52
CHEMBL4096886 1 7.40
CHEMBL4104613 1 7.40
CHEMBL4080389 1 7.40
CHEMBL4096874 1 7.22
CHEMBL4062072 1 7.10
CHEMBL4090626 1 7.10
CHEMBL4099270 1 7.05
CHEMBL4088228 1 7.00
CHEMBL4061001 1 6.75
CHEMBL4069679 1 6.70
CHEMBL4081852 1 6.70
CHEMBL4101887 1 6.52
CHEMBL4083888 1 6.52
CHEMBL4076087 1 6.52
CHEMBL4089716 1 6.30
CHEMBL4068594 1 6.16
CHEMBL4077369 1 6.05
CHEMBL4078895 1 6.05
CHEMBL4062043 1 6.00
CHEMBL4065925 1 5.89
CHEMBL4095958 1 5.75
CHEMBL4087726 1 5.42
CHEMBL4062669 1 5.36
CHEMBL4093525 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230468 IC50 = 4.0 nM 8.40
CHEMBL3358120 IC50 = 5.0 nM 8.30
CHEMBL4080376 IC50 = 10.0 nM 8.00
CHEMBL3358114 IC50 = 12.0 nM 7.92
CHEMBL4069661 IC50 = 30.0 nM 7.52
CHEMBL4071314 IC50 = 30.0 nM 7.52
CHEMBL4096886 IC50 = 40.0 nM 7.40
CHEMBL4104613 IC50 = 40.0 nM 7.40
CHEMBL4080389 IC50 = 40.0 nM 7.40
CHEMBL4096874 IC50 = 60.0 nM 7.22
CHEMBL4062072 IC50 = 80.0 nM 7.10
CHEMBL4090626 IC50 = 80.0 nM 7.10
CHEMBL4099270 IC50 = 90.0 nM 7.05
CHEMBL4088228 IC50 = 100.0 nM 7.00
CHEMBL4061001 IC50 = 180.0 nM 6.75
CHEMBL4069679 IC50 = 200.0 nM 6.70
CHEMBL4081852 IC50 = 200.0 nM 6.70
CHEMBL4076087 IC50 = 300.0 nM 6.52
CHEMBL4101887 IC50 = 300.0 nM 6.52
CHEMBL4083888 IC50 = 300.0 nM 6.52
CHEMBL4089716 IC50 = 500.0 nM 6.30
CHEMBL4068594 IC50 = 700.0 nM 6.16
CHEMBL4077369 IC50 = 900.0 nM 6.05
CHEMBL4078895 IC50 = 900.0 nM 6.05
CHEMBL4062043 IC50 = 1000.0 nM 6.00
CHEMBL4065925 IC50 = 1300.0 nM 5.89
CHEMBL4095958 IC50 = 1800.0 nM 5.75
CHEMBL4087726 IC50 = 3800.0 nM 5.42
CHEMBL4062669 IC50 = 4400.0 nM 5.36
CHEMBL4093525 IC50 = 6500.0 nM 5.19
CHEMBL4103178 IC50 = 9900.0 nM 5.00
CHEMBL4105605 IC50 = 12000.0 nM 4.92
CHEMBL4094965 IC50 = 14000.0 nM 4.85
CHEMBL4067547 IC50 = 15000.0 nM 4.82
CHEMBL4098349 IC50 > 100000.0 nM -
CHEMBL4076386 IC50 > 1000.0 nM -
CHEMBL4059932 IC50 > 1000.0 nM -
CHEMBL4075895 IC50 > 50000.0 nM -