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Assay Detail

CHEMBL3387687

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ADMET
Antiproliferative activity against human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
ChEMBL ↗
48
Total Activities
48
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

Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis.
Brand S, Norcross NR, Thompson S, Harrison JR, Smith VC, Robinson DA, Torrie LS, McElroy SP, Hallyburton I, Norval S, Scullion P, Stojanovski L, Simeons FR, van Aalten D, Frearson JA, Brenk R, Fairlamb AH, Ferguson MA, Wyatt PG, Gilbert IH, Read KD.
J Med Chem (2014) 57 : 9855 -9869
PubMed 25412409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 48 5.72 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3357685 ZELENIRSTAT 2.0 1 7.05
CHEMBL3358119 — — 1 6.96
CHEMBL3357702 — — 1 6.85
CHEMBL3357688 — — 1 6.85
CHEMBL3358121 — — 1 6.80
CHEMBL3357697 — — 1 6.75
CHEMBL3358120 — — 1 6.70
CHEMBL3357682 — — 1 6.60
CHEMBL1230468 — — 1 6.52
CHEMBL3357699 — — 1 6.43
CHEMBL3358117 — — 1 6.29
CHEMBL3357684 — — 1 6.19
CHEMBL3358122 — — 1 6.19
CHEMBL3357686 — — 1 6.14
CHEMBL3357704 — — 1 6.10
CHEMBL3357705 — — 1 6.05
CHEMBL3358114 — — 1 6.00
CHEMBL3358112 — — 1 5.96
CHEMBL3357703 — — 1 5.92
CHEMBL3357681 — — 1 5.91
CHEMBL3357687 — — 1 5.82
CHEMBL3357693 — — 1 5.66
CHEMBL3358111 — — 1 5.66
CHEMBL3357695 — — 1 5.60
CHEMBL3358123 — — 1 5.55
CHEMBL3358127 — — 1 5.51
CHEMBL3358125 — — 1 5.50
CHEMBL3358126 — — 1 5.46
CHEMBL3357698 — — 1 5.44
CHEMBL3358115 — — 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3357685 ZELENIRSTAT EC50 = 90.0 nM 7.05
CHEMBL3358119 — EC50 = 110.0 nM 6.96
CHEMBL3357688 — EC50 = 140.0 nM 6.85
CHEMBL3357702 — EC50 = 140.0 nM 6.85
CHEMBL3358121 — EC50 = 160.0 nM 6.80
CHEMBL3357697 — EC50 = 180.0 nM 6.75
CHEMBL3358120 — EC50 = 200.0 nM 6.70
CHEMBL3357682 — EC50 = 250.0 nM 6.60
CHEMBL1230468 — EC50 = 300.0 nM 6.52
CHEMBL3357699 — EC50 = 370.0 nM 6.43
CHEMBL3358117 — EC50 = 510.0 nM 6.29
CHEMBL3357684 — EC50 = 640.0 nM 6.19
CHEMBL3358122 — EC50 = 650.0 nM 6.19
CHEMBL3357686 — EC50 = 730.0 nM 6.14
CHEMBL3357704 — EC50 = 790.0 nM 6.10
CHEMBL3357705 — EC50 = 900.0 nM 6.05
CHEMBL3358114 — EC50 = 1000.0 nM 6.00
CHEMBL3358112 — EC50 = 1100.0 nM 5.96
CHEMBL3357703 — EC50 = 1200.0 nM 5.92
CHEMBL3357681 — EC50 = 1230.0 nM 5.91
CHEMBL3357687 — EC50 = 1500.0 nM 5.82
CHEMBL3357693 — EC50 = 2200.0 nM 5.66
CHEMBL3358111 — EC50 = 2200.0 nM 5.66
CHEMBL3357695 — EC50 = 2500.0 nM 5.60
CHEMBL3358123 — EC50 = 2800.0 nM 5.55
CHEMBL3358127 — EC50 = 3100.0 nM 5.51
CHEMBL3358125 — EC50 = 3200.0 nM 5.50
CHEMBL3358126 — EC50 = 3500.0 nM 5.46
CHEMBL3357698 — EC50 = 3600.0 nM 5.44
CHEMBL3358115 — EC50 = 3800.0 nM 5.42
CHEMBL3358124 — EC50 = 3900.0 nM 5.41
CHEMBL3357700 — EC50 = 5300.0 nM 5.28
CHEMBL3358118 — EC50 = 7200.0 nM 5.14
CHEMBL3358110 — EC50 = 7800.0 nM 5.11
CHEMBL3357683 — EC50 = 10300.0 nM 4.99
CHEMBL3357689 — EC50 = 16600.0 nM 4.78
CHEMBL3358108 — EC50 = 17000.0 nM 4.77
CHEMBL3357706 — EC50 = 17000.0 nM 4.77
CHEMBL3357694 — EC50 = 18700.0 nM 4.73
CHEMBL3358116 — EC50 = 19000.0 nM 4.72
CHEMBL3358109 — EC50 = 21000.0 nM 4.68
CHEMBL3357701 — EC50 = 27200.0 nM 4.57
CHEMBL3357691 — EC50 = 31400.0 nM 4.50
CHEMBL3358113 — EC50 = 42000.0 nM 4.38
CHEMBL3357692 — EC50 > 50000.0 nM -
CHEMBL3357690 — EC50 > 50000.0 nM -
CHEMBL1951264 — EC50 > 50000.0 nM -
CHEMBL3357696 — EC50 > 50000.0 nM -