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Assay Detail

CHEMBL1954201

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

Binding
Inhibition of human N-myristoyltransferase 1 using [3H]myristoyl-CoA and GCGGSKVKPQPPQAK(biotin)-amide as substrate preincubated for 5 mins prior substrate addition measured after 50 mins by streptavidin-coated scintillation proximity assay
27
Total Activities
27
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

Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors.
Brand S, Cleghorn LA, McElroy SP, Robinson DA, Smith VC, Hallyburton I, Harrison JR, Norcross NR, Spinks D, Bayliss T, Norval S, Stojanovski L, Torrie LS, Frearson JA, Brenk R, Fairlamb AH, Ferguson MA, Read KD, Wyatt PG, Gilbert IH.
J Med Chem (2012) 55 : 140 -152
PubMed 22148754 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.74 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230468 1 8.52
CHEMBL1951295 1 8.15
CHEMBL1951287 1 6.96
CHEMBL1951296 1 6.92
CHEMBL1951293 1 6.12
CHEMBL1951282 1 6.00
CHEMBL1951286 1 5.80
CHEMBL1951284 1 5.62
CHEMBL1951274 1 5.57
CHEMBL1951291 1 5.38
CHEMBL1951294 1 5.37
CHEMBL1951277 1 5.09
CHEMBL1951285 1 5.06
CHEMBL1951278 1 4.80
CHEMBL1951273 1 4.77
CHEMBL1951105 1 4.66
CHEMBL1951292 1 4.35
CHEMBL1951279 1 4.13
CHEMBL1951283 1 -
CHEMBL1951288 1 -
CHEMBL1951289 1 -
CHEMBL1951290 1 -
CHEMBL1951281 1 -
CHEMBL1951280 1 -
CHEMBL1951276 1 -
CHEMBL1951275 1 -
CHEMBL1951272 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230468 IC50 = 3.0 nM 8.52
CHEMBL1951295 IC50 = 7.0 nM 8.15
CHEMBL1951287 IC50 = 110.0 nM 6.96
CHEMBL1951296 IC50 = 120.0 nM 6.92
CHEMBL1951293 IC50 = 750.0 nM 6.12
CHEMBL1951282 IC50 = 1000.0 nM 6.00
CHEMBL1951286 IC50 = 1600.0 nM 5.80
CHEMBL1951284 IC50 = 2400.0 nM 5.62
CHEMBL1951274 IC50 = 2700.0 nM 5.57
CHEMBL1951291 IC50 = 4200.0 nM 5.38
CHEMBL1951294 IC50 = 4300.0 nM 5.37
CHEMBL1951277 IC50 = 8200.0 nM 5.09
CHEMBL1951285 IC50 = 8700.0 nM 5.06
CHEMBL1951278 IC50 = 16000.0 nM 4.80
CHEMBL1951273 IC50 = 17000.0 nM 4.77
CHEMBL1951105 IC50 = 22000.0 nM 4.66
CHEMBL1951292 IC50 = 45000.0 nM 4.35
CHEMBL1951279 IC50 = 74000.0 nM 4.13
CHEMBL1951283 IC50 > 1000.0 nM -
CHEMBL1951288 IC50 > 10000.0 nM -
CHEMBL1951289 IC50 > 10000.0 nM -
CHEMBL1951290 IC50 > 100000.0 nM -
CHEMBL1951281 IC50 - -
CHEMBL1951280 IC50 > 1000.0 nM -
CHEMBL1951276 IC50 - -
CHEMBL1951275 IC50 - -
CHEMBL1951272 IC50 > 100000.0 nM -