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Assay Detail

CHEMBL4178185

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Functional
Antiparasitic activity against Cryptosporidium parvum Iowa oocysts infected in human HCT8 cells pretreated prior to infection measured after 48 hrs by fluorescein labeled Vicia villosa lectin/Hoechst 33258 staining based epifluorescence microscopic analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cryptosporidium parvum
Confidence 1 — Organism
Curated By Intermediate

Target

Cryptosporidium parvum (CHEMBL612855)
Type ORGANISM
Organism Cryptosporidium parvum

Publication

Discovery and structure activity relationship of the first potent cryptosporidium FIKK kinase inhibitor.
Osman KT, Ye J, Shi Z, Toker C, Lovato D, Jumani RS, Zuercher W, Huston CD, Edwards AM, Lautens M, Santhakumar V, Hui R.
Bioorg Med Chem (2017) 25 : 1672 -1680
PubMed 28162900 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.51 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205167 1 5.89
CHEMBL4209540 1 5.58
CHEMBL4208125 1 5.41
CHEMBL264406 1 5.39
CHEMBL365663 GW780159X 1 5.26
CHEMBL4214228 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205167 EC50 = 1300.0 nM 5.89
CHEMBL4209540 EC50 = 2600.0 nM 5.58
CHEMBL4208125 EC50 = 3900.0 nM 5.41
CHEMBL264406 EC50 = 4100.0 nM 5.39
CHEMBL365663 GW780159X EC50 = 5500.0 nM 5.26
CHEMBL4214228 EC50 - -