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Assay Detail

CHEMBL4178007

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Binding
Inhibition of Cryptosporidium parvum CDPK1 using PLARTLSVAGLPGKK peptide as substrate by NADH coupled LDH-PK ATPase assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cryptosporidium parvum
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
IC50 20 6.51 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4208125 1 7.72
CHEMBL4218785 1 7.14
CHEMBL4214870 1 7.13
CHEMBL365663 GW780159X 1 7.08
CHEMBL4209540 1 6.72
CHEMBL4206097 1 6.72
CHEMBL4205167 1 6.68
CHEMBL361237 GW785804X 1 6.66
CHEMBL4212444 1 6.58
CHEMBL4211693 1 6.48
CHEMBL4209953 1 6.46
CHEMBL4217687 1 6.43
CHEMBL4209312 1 6.40
CHEMBL4204551 1 6.35
CHEMBL4216667 1 5.82
CHEMBL4217402 1 5.82
CHEMBL4212736 1 5.58
CHEMBL4214228 1 5.46
CHEMBL4213278 1 -
CHEMBL4204005 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4208125 IC50 = 19.0 nM 7.72
CHEMBL4218785 IC50 = 73.0 nM 7.14
CHEMBL4214870 IC50 = 74.0 nM 7.13
CHEMBL365663 GW780159X IC50 = 84.0 nM 7.08
CHEMBL4209540 IC50 = 190.0 nM 6.72
CHEMBL4206097 IC50 = 190.0 nM 6.72
CHEMBL4205167 IC50 = 210.0 nM 6.68
CHEMBL361237 GW785804X IC50 = 220.0 nM 6.66
CHEMBL4212444 IC50 = 260.0 nM 6.58
CHEMBL4211693 IC50 = 330.0 nM 6.48
CHEMBL4209953 IC50 = 350.0 nM 6.46
CHEMBL4217687 IC50 = 375.0 nM 6.43
CHEMBL4209312 IC50 = 400.0 nM 6.40
CHEMBL4204551 IC50 = 450.0 nM 6.35
CHEMBL4216667 IC50 = 1510.0 nM 5.82
CHEMBL4217402 IC50 = 1500.0 nM 5.82
CHEMBL4212736 IC50 = 2600.0 nM 5.58
CHEMBL4214228 IC50 = 3500.0 nM 5.46
CHEMBL4213278 IC50 > 10000.0 nM -
CHEMBL4204005 IC50 > 10000.0 nM -