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Assay Detail

CHEMBL4032436

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

ADMET
CYtotoxicity against human MRC5 cells after 69 hrs by resazurin assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type MRC5
Confidence 1 — Organism
Curated By Autocuration

Target

MRC5 (CHEMBL614181)
Type CELL-LINE
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
EC50 38 5.58 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3358120 1 6.70
CHEMBL1230468 1 6.40
CHEMBL3358114 1 6.00
CHEMBL4061001 1 5.85
CHEMBL4080376 1 5.82
CHEMBL4104613 1 5.82
CHEMBL4087726 1 5.70
CHEMBL4069679 1 5.68
CHEMBL4090626 1 5.66
CHEMBL4081852 1 5.64
CHEMBL4069661 1 5.60
CHEMBL4065925 1 5.55
CHEMBL4067547 1 5.51
CHEMBL4096874 1 5.48
CHEMBL4062669 1 5.46
CHEMBL4083888 1 5.43
CHEMBL4093525 1 5.34
CHEMBL4099270 1 5.30
CHEMBL4062043 1 5.20
CHEMBL4101887 1 5.17
CHEMBL4062072 1 5.06
CHEMBL4095958 1 5.05
CHEMBL4080389 1 4.85
CHEMBL4088228 1 -
CHEMBL4096886 1 -
CHEMBL4075895 1 -
CHEMBL4076386 1 -
CHEMBL4105605 1 -
CHEMBL4068594 1 -
CHEMBL4077369 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3358120 EC50 = 200.0 nM 6.70
CHEMBL1230468 EC50 = 400.0 nM 6.40
CHEMBL3358114 EC50 = 1000.0 nM 6.00
CHEMBL4061001 EC50 = 1400.0 nM 5.85
CHEMBL4080376 EC50 = 1500.0 nM 5.82
CHEMBL4104613 EC50 = 1500.0 nM 5.82
CHEMBL4087726 EC50 = 2000.0 nM 5.70
CHEMBL4069679 EC50 = 2100.0 nM 5.68
CHEMBL4090626 EC50 = 2200.0 nM 5.66
CHEMBL4081852 EC50 = 2300.0 nM 5.64
CHEMBL4069661 EC50 = 2500.0 nM 5.60
CHEMBL4065925 EC50 = 2800.0 nM 5.55
CHEMBL4067547 EC50 = 3100.0 nM 5.51
CHEMBL4096874 EC50 = 3300.0 nM 5.48
CHEMBL4062669 EC50 = 3500.0 nM 5.46
CHEMBL4083888 EC50 = 3700.0 nM 5.43
CHEMBL4093525 EC50 = 4600.0 nM 5.34
CHEMBL4099270 EC50 = 5000.0 nM 5.30
CHEMBL4062043 EC50 = 6300.0 nM 5.20
CHEMBL4101887 EC50 = 6700.0 nM 5.17
CHEMBL4062072 EC50 = 8700.0 nM 5.06
CHEMBL4095958 EC50 = 8900.0 nM 5.05
CHEMBL4080389 EC50 = 14000.0 nM 4.85
CHEMBL4089716 EC50 > 1000.0 nM -
CHEMBL4059932 EC50 > 1000.0 nM -
CHEMBL4071314 EC50 > 10000.0 nM -
CHEMBL4098349 EC50 > 100000.0 nM -
CHEMBL4094965 EC50 > 10000.0 nM -
CHEMBL4103178 EC50 > 1000.0 nM -
CHEMBL4078895 EC50 > 100000.0 nM -
CHEMBL4076087 EC50 > 1000.0 nM -
CHEMBL4077369 EC50 > 1000.0 nM -
CHEMBL4068594 EC50 > 1000.0 nM -
CHEMBL4105605 EC50 > 10000.0 nM -
CHEMBL4076386 EC50 > 1000.0 nM -
CHEMBL4075895 EC50 > 50000.0 nM -
CHEMBL4096886 EC50 > 1000.0 nM -
CHEMBL4088228 EC50 > 1000.0 nM -