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Assay Detail

CHEMBL1786291

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Binding
Inhibition of Cryptosporidium parvum recombinant N-terminal hexahistidine tagged CDPK1 expressed in Escherichia coli using syntide-2 as substrate after 90 mins by luminescence based scintillation counter
ChEMBL ↗
49
Total Activities
49
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 of Potent and Selective Inhibitors of Calcium-Dependent Protein Kinase 1 (CDPK1) from C. parvum and T. gondii.
Murphy RC, Ojo KK, Larson ET, Castellanos-Gonzalez A, Perera BG, Keyloun KR, Kim JE, Bhandari JG, Muller NR, Verlinde CL, White AC, Merritt EA, Van Voorhis WC, Maly DJ.
ACS Med Chem Lett (2010) 1 : 331 -335
PubMed 21116453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 6.84 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1785020 — — 1 8.30
CHEMBL1231372 — — 1 8.05
CHEMBL1241489 — — 1 8.00
CHEMBL1785021 — — 1 7.92
CHEMBL1785012 — — 1 7.89
CHEMBL1785018 — — 1 7.77
CHEMBL1242754 — — 1 7.70
CHEMBL1785017 — — 1 7.66
CHEMBL1784965 — — 1 7.47
CHEMBL1784969 — — 1 7.30
CHEMBL1782086 — — 1 7.28
CHEMBL1784964 — — 1 7.25
CHEMBL1785014 — — 1 7.23
CHEMBL1231371 — — 1 7.23
CHEMBL1784972 — — 1 7.12
CHEMBL1785015 — — 1 7.06
CHEMBL1242660 — — 1 7.03
CHEMBL1784966 — — 1 7.00
CHEMBL1784971 — — 1 7.00
CHEMBL1785024 — — 1 6.96
CHEMBL1785016 — — 1 6.94
CHEMBL1785054 — — 1 6.92
CHEMBL1785011 — — 1 6.92
CHEMBL1784960 — — 1 6.89
CHEMBL573578 — — 1 6.85
CHEMBL1231370 — — 1 6.82
CHEMBL1784970 — — 1 6.80
CHEMBL1242290 — — 1 6.77
CHEMBL1784968 — — 1 6.75
CHEMBL1784974 — — 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1785020 — IC50 = 5.0 nM 8.30
CHEMBL1231372 — IC50 = 9.0 nM 8.05
CHEMBL1241489 — IC50 = 10.0 nM 8.00
CHEMBL1785021 — IC50 = 12.0 nM 7.92
CHEMBL1785012 — IC50 = 13.0 nM 7.89
CHEMBL1785018 — IC50 = 17.0 nM 7.77
CHEMBL1242754 — IC50 = 20.0 nM 7.70
CHEMBL1785017 — IC50 = 22.0 nM 7.66
CHEMBL1784965 — IC50 = 34.0 nM 7.47
CHEMBL1784969 — IC50 = 50.0 nM 7.30
CHEMBL1782086 — IC50 = 53.0 nM 7.28
CHEMBL1784964 — IC50 = 56.0 nM 7.25
CHEMBL1231371 — IC50 = 59.0 nM 7.23
CHEMBL1785014 — IC50 = 59.0 nM 7.23
CHEMBL1784972 — IC50 = 75.0 nM 7.12
CHEMBL1785015 — IC50 = 87.0 nM 7.06
CHEMBL1242660 — IC50 = 93.0 nM 7.03
CHEMBL1784966 — IC50 = 100.0 nM 7.00
CHEMBL1784971 — IC50 = 100.0 nM 7.00
CHEMBL1785024 — IC50 = 110.0 nM 6.96
CHEMBL1785016 — IC50 = 114.0 nM 6.94
CHEMBL1785054 — IC50 = 120.0 nM 6.92
CHEMBL1785011 — IC50 = 120.0 nM 6.92
CHEMBL1784960 — IC50 = 130.0 nM 6.89
CHEMBL573578 — IC50 = 140.0 nM 6.85
CHEMBL1231370 — IC50 = 150.0 nM 6.82
CHEMBL1784970 — IC50 = 160.0 nM 6.80
CHEMBL1242290 — IC50 = 170.0 nM 6.77
CHEMBL1784968 — IC50 = 180.0 nM 6.75
CHEMBL1784974 — IC50 = 200.0 nM 6.70
CHEMBL1785013 — IC50 = 210.0 nM 6.68
CHEMBL1784975 — IC50 = 220.0 nM 6.66
CHEMBL1785023 — IC50 = 310.0 nM 6.51
CHEMBL1784967 — IC50 = 360.0 nM 6.44
CHEMBL1242847 — IC50 = 410.0 nM 6.39
CHEMBL1784959 — IC50 = 410.0 nM 6.39
CHEMBL1785022 — IC50 = 600.0 nM 6.22
CHEMBL1785019 — IC50 = 620.0 nM 6.21
CHEMBL1784973 — IC50 = 700.0 nM 6.16
CHEMBL1241588 — IC50 = 990.0 nM 6.00
CHEMBL1784961 — IC50 = 2000.0 nM 5.70
CHEMBL1241946 — IC50 = 2100.0 nM 5.68
CHEMBL264406 — IC50 = 2900.0 nM 5.54
CHEMBL1784962 — IC50 = 3000.0 nM 5.52
CHEMBL1785025 — IC50 = 3000.0 nM 5.52
CHEMBL1785052 — IC50 = 3000.0 nM 5.52
CHEMBL1784963 — IC50 > 2400.0 nM -
CHEMBL1785026 — IC50 > 1400.0 nM -
CHEMBL1785053 — IC50 > 1900.0 nM -