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Assay Detail

CHEMBL1111994

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

Functional
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 7 days by alamar blue assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Cell Type NIH3T3
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

Second generation analogues of the cancer drug clinical candidate tipifarnib for anti-Chagas disease drug discovery.
Kraus JM, Tatipaka HB, McGuffin SA, Chennamaneni NK, Karimi M, Arif J, Verlinde CL, Buckner FS, Gelb MH.
J Med Chem (2010) 53 : 3887 -3898
PubMed 20429511 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 34 8.29 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1397 POSACONAZOLE 4.0 1 9.52
CHEMBL1097187 1 9.51
CHEMBL1097079 1 9.30
CHEMBL1097102 1 9.22
CHEMBL1097771 1 9.15
CHEMBL1097448 1 9.10
CHEMBL1094185 1 9.10
CHEMBL1097772 1 9.10
CHEMBL1097078 1 9.09
CHEMBL1097775 1 8.96
CHEMBL1097769 1 8.92
CHEMBL1097188 1 8.85
CHEMBL1094184 1 8.74
CHEMBL1094183 1 8.70
CHEMBL1097836 1 8.66
CHEMBL1096793 1 8.52
CHEMBL1094235 1 8.52
CHEMBL1097444 1 8.51
CHEMBL1097186 1 8.49
CHEMBL289228 TIPIFARNIB 3.0 1 8.40
CHEMBL1095514 1 8.30
CHEMBL1094540 1 8.30
CHEMBL1095823 1 8.00
CHEMBL1097770 1 7.92
CHEMBL343172 1 7.77
CHEMBL1097174 1 7.57
CHEMBL1094215 1 7.48
CHEMBL1097175 1 7.16
CHEMBL1094362 1 7.08
CHEMBL1096484 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1397 POSACONAZOLE EC50 = 0.3 nM 9.52
CHEMBL1097187 EC50 = 0.31 nM 9.51
CHEMBL1097079 EC50 = 0.5 nM 9.30
CHEMBL1097102 EC50 = 0.6 nM 9.22
CHEMBL1097771 EC50 = 0.7 nM 9.15
CHEMBL1097448 EC50 = 0.8 nM 9.10
CHEMBL1094185 EC50 = 0.8 nM 9.10
CHEMBL1097772 EC50 = 0.8 nM 9.10
CHEMBL1097078 EC50 = 0.82 nM 9.09
CHEMBL1097775 EC50 = 1.1 nM 8.96
CHEMBL1097769 EC50 = 1.2 nM 8.92
CHEMBL1097188 EC50 = 1.4 nM 8.85
CHEMBL1094184 EC50 = 1.8 nM 8.74
CHEMBL1094183 EC50 = 2.0 nM 8.70
CHEMBL1097836 EC50 = 2.2 nM 8.66
CHEMBL1096793 EC50 = 3.0 nM 8.52
CHEMBL1094235 EC50 = 3.0 nM 8.52
CHEMBL1097444 EC50 = 3.1 nM 8.51
CHEMBL1097186 EC50 = 3.21 nM 8.49
CHEMBL289228 TIPIFARNIB EC50 = 4.0 nM 8.40
CHEMBL1095514 EC50 = 5.0 nM 8.30
CHEMBL1094540 EC50 = 5.0 nM 8.30
CHEMBL1095823 EC50 = 10.0 nM 8.00
CHEMBL1097770 EC50 = 12.0 nM 7.92
CHEMBL343172 EC50 = 17.0 nM 7.77
CHEMBL1097174 EC50 = 27.0 nM 7.57
CHEMBL1094215 EC50 = 33.0 nM 7.48
CHEMBL1097175 EC50 = 69.0 nM 7.16
CHEMBL1094362 EC50 = 83.0 nM 7.08
CHEMBL1096484 EC50 = 100.0 nM 7.00
CHEMBL1097806 EC50 = 112.0 nM 6.95
CHEMBL1096483 EC50 = 118.0 nM 6.93
CHEMBL1094234 EC50 = 228.0 nM 6.64
CHEMBL1094361 EC50 = 320.0 nM 6.50