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Assay Detail

CHEMBL5252147

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

Functional
Antiparasitic activity against Cryptosporidium parvum infected in human HCT-8 cells assessed as parasitic growth inhibition measured for 48 hrs by fluorescence based microscopic analysis
56
Total Activities
28
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cryptosporidium parvum
Cell Type HCT-8
Confidence 1 — Organism
Curated By Autocuration

Target

Cryptosporidium parvum (CHEMBL612855)
Type ORGANISM
Organism Cryptosporidium parvum

Publication

Structure-activity relationship of BMS906024 derivatives for Cryptosporidium parvum growth inhibition.
Lee S, Love MS, Modukuri R, Chatterjee AK, Huerta L, Lawson AP, McNamara CW, Mead JR, Hedstrom L, Cuny GD.
Bioorg Med Chem Lett (2023) 90 : 129328 -129328
PubMed 37196868 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC90 28 - -
EC50 28 6.70 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297269 OSUGACESTAT 2.0 2 8.74
CHEMBL5277661 2 8.19
CHEMBL5290152 2 7.75
CHEMBL5269363 2 7.60
CHEMBL5268899 2 7.51
CHEMBL5280057 2 7.28
CHEMBL5289461 2 7.11
CHEMBL5283121 2 7.09
CHEMBL5288459 2 6.96
CHEMBL5277099 2 6.96
CHEMBL5275988 2 6.96
CHEMBL5283775 2 6.55
CHEMBL5268967 2 6.50
CHEMBL5269620 2 6.46
CHEMBL5290986 2 6.26
CHEMBL5289149 2 5.84
CHEMBL5288433 2 5.77
CHEMBL5268841 2 5.64
CHEMBL5283923 2 5.60
CHEMBL5266604 2 5.26
CHEMBL5286214 2 4.60
CHEMBL5271513 2 -
CHEMBL5274430 2 -
CHEMBL5282809 2 -
CHEMBL5280809 2 -
CHEMBL5287140 2 -
CHEMBL5272298 2 -
CHEMBL5281234 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297269 OSUGACESTAT EC50 = 1.8 nM 8.74
CHEMBL5277661 EC50 = 6.4 nM 8.19
CHEMBL5290152 EC50 = 18.0 nM 7.75
CHEMBL5269363 EC50 = 25.0 nM 7.60
CHEMBL5268899 EC50 = 31.0 nM 7.51
CHEMBL5280057 EC50 = 52.0 nM 7.28
CHEMBL5289461 EC50 = 77.0 nM 7.11
CHEMBL5283121 EC50 = 81.0 nM 7.09
CHEMBL5288459 EC50 = 110.0 nM 6.96
CHEMBL5277099 EC50 = 110.0 nM 6.96
CHEMBL5275988 EC50 = 110.0 nM 6.96
CHEMBL5283775 EC50 = 280.0 nM 6.55
CHEMBL5268967 EC50 = 320.0 nM 6.50
CHEMBL5269620 EC50 = 350.0 nM 6.46
CHEMBL5290986 EC50 = 550.0 nM 6.26
CHEMBL5289149 EC50 = 1450.0 nM 5.84
CHEMBL5288433 EC50 = 1690.0 nM 5.77
CHEMBL5268841 EC50 = 2290.0 nM 5.64
CHEMBL5283923 EC50 = 2520.0 nM 5.60
CHEMBL5266604 EC50 = 5470.0 nM 5.26
CHEMBL5286214 EC50 = 25000.0 nM 4.60
CHEMBL5275988 EC90 = 0.21 uM -
CHEMBL5283923 EC90 = 11.1 uM -
CHEMBL5289461 EC90 = 0.16 uM -
CHEMBL5268899 EC90 = 0.066 uM -
CHEMBL5283121 EC90 = 0.15 uM -
CHEMBL5281234 EC50 > 25000.0 nM -
CHEMBL5280057 EC90 = 0.1 uM -
CHEMBL5277661 EC90 = 0.016 uM -
CHEMBL5288459 EC90 = 0.23 uM -
CHEMBL5286214 EC90 > 25.0 uM -
CHEMBL5287140 EC90 > 25.0 uM -
CHEMBL5280809 EC90 > 25.0 uM -
CHEMBL5282809 EC90 > 25.0 uM -
CHEMBL5271513 EC90 > 25.0 uM -
CHEMBL5268841 EC90 = 4.9 uM -
CHEMBL5272298 EC90 > 25.0 uM -
CHEMBL5266604 EC90 = 12.8 uM -
CHEMBL5268967 EC90 = 0.96 uM -
CHEMBL5288433 EC90 = 3.61 uM -
CHEMBL5269363 EC90 = 0.055 uM -
CHEMBL5281234 EC90 > 25.0 uM -
CHEMBL5274430 EC50 > 25000.0 nM -
CHEMBL5271513 EC50 > 25000.0 nM -
CHEMBL5282809 EC50 > 25000.0 nM -
CHEMBL5277099 EC90 = 0.31 uM -
CHEMBL5272298 EC50 > 25000.0 nM -
CHEMBL5287140 EC50 > 25000.0 nM -
CHEMBL4297269 OSUGACESTAT EC90 = 0.0023 uM -
CHEMBL5280809 EC50 > 25000.0 nM -