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Assay Detail

CHEMBL4032433

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Binding
Inhibition of Trypanosoma brucei NMT using [3H]-myristoyl-coA/biotinylated CAP5.5 as substrate after 50 mins by scintillation/luminescence counting method
ChEMBL ↗
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma brucei
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

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 55 6.27 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3358114 — — 1 8.70
CHEMBL3358120 — — 1 8.70
CHEMBL1230468 — — 1 8.70
CHEMBL4096886 — — 1 7.70
CHEMBL4104613 — — 1 7.70
CHEMBL4090626 — — 1 7.30
CHEMBL4061001 — — 1 7.22
CHEMBL4071314 — — 1 7.22
CHEMBL4082383 — — 1 7.16
CHEMBL4062043 — — 1 7.10
CHEMBL4069679 — — 1 7.10
CHEMBL4093525 — — 1 7.00
CHEMBL4080389 — — 1 7.00
CHEMBL4083888 — — 1 7.00
CHEMBL4078895 — — 1 6.70
CHEMBL4081852 — — 1 6.52
CHEMBL4076087 — — 1 6.52
CHEMBL4094965 — — 1 6.52
CHEMBL4062669 — — 1 6.52
CHEMBL4094560 — — 1 6.40
CHEMBL4101887 — — 1 6.30
CHEMBL4103178 — — 1 6.30
CHEMBL4099270 — — 1 6.22
CHEMBL4090756 — — 1 6.22
CHEMBL4067091 — — 1 6.22
CHEMBL4065925 — — 1 6.10
CHEMBL4059932 — — 1 6.10
CHEMBL4080376 — — 1 6.10
CHEMBL4080457 — — 1 5.92
CHEMBL4096874 — — 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3358114 — IC50 = 2.0 nM 8.70
CHEMBL3358120 — IC50 = 2.0 nM 8.70
CHEMBL1230468 — IC50 = 2.0 nM 8.70
CHEMBL4096886 — IC50 = 20.0 nM 7.70
CHEMBL4104613 — IC50 = 20.0 nM 7.70
CHEMBL4090626 — IC50 = 50.0 nM 7.30
CHEMBL4061001 — IC50 = 60.0 nM 7.22
CHEMBL4071314 — IC50 = 60.0 nM 7.22
CHEMBL4082383 — IC50 = 70.0 nM 7.16
CHEMBL4062043 — IC50 = 80.0 nM 7.10
CHEMBL4069679 — IC50 = 80.0 nM 7.10
CHEMBL4083888 — IC50 = 100.0 nM 7.00
CHEMBL4080389 — IC50 = 100.0 nM 7.00
CHEMBL4093525 — IC50 = 100.0 nM 7.00
CHEMBL4078895 — IC50 = 200.0 nM 6.70
CHEMBL4081852 — IC50 = 300.0 nM 6.52
CHEMBL4062669 — IC50 = 300.0 nM 6.52
CHEMBL4094965 — IC50 = 300.0 nM 6.52
CHEMBL4076087 — IC50 = 300.0 nM 6.52
CHEMBL4094560 — IC50 = 400.0 nM 6.40
CHEMBL4101887 — IC50 = 500.0 nM 6.30
CHEMBL4103178 — IC50 = 500.0 nM 6.30
CHEMBL4099270 — IC50 = 600.0 nM 6.22
CHEMBL4090756 — IC50 = 600.0 nM 6.22
CHEMBL4067091 — IC50 = 600.0 nM 6.22
CHEMBL4065925 — IC50 = 800.0 nM 6.10
CHEMBL4080376 — IC50 = 800.0 nM 6.10
CHEMBL4059932 — IC50 = 800.0 nM 6.10
CHEMBL4080457 — IC50 = 1200.0 nM 5.92
CHEMBL4096874 — IC50 = 1200.0 nM 5.92
CHEMBL4067547 — IC50 = 1300.0 nM 5.89
CHEMBL4089716 — IC50 = 1300.0 nM 5.89
CHEMBL4088311 — IC50 = 1400.0 nM 5.85
CHEMBL4061084 — IC50 = 1600.0 nM 5.80
CHEMBL4088228 — IC50 = 1600.0 nM 5.80
CHEMBL4078984 — IC50 = 1700.0 nM 5.77
CHEMBL4062072 — IC50 = 2000.0 nM 5.70
CHEMBL4077369 — IC50 = 2000.0 nM 5.70
CHEMBL4069661 — IC50 = 2000.0 nM 5.70
CHEMBL4098349 — IC50 = 2900.0 nM 5.54
CHEMBL4104723 — IC50 = 2900.0 nM 5.54
CHEMBL4087726 — IC50 = 3500.0 nM 5.46
CHEMBL4105605 — IC50 = 4200.0 nM 5.38
CHEMBL4068594 — IC50 = 4600.0 nM 5.34
CHEMBL4076386 — IC50 = 5400.0 nM 5.27
CHEMBL4082965 — IC50 = 9500.0 nM 5.02
CHEMBL4060075 — IC50 = 13000.0 nM 4.89
CHEMBL4100392 — IC50 = 13000.0 nM 4.89
CHEMBL4096995 — IC50 = 15000.0 nM 4.82
CHEMBL4095958 — IC50 = 16000.0 nM 4.80