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Assay Detail

CHEMBL4031138

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Functional
Antiparasitic activity against Toxoplasma gondii RH genotype 1 2F clone expressing bacterial beta-galactosidase infected in human HFF cells preincubated for 4 hrs followed by compound washout measured after 72 hrs by chlorophenol red-beta-D-galactopyranoside based spectrophotometry
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Toxoplasma gondii
Confidence 1 — Organism
Curated By Autocuration

Target

Toxoplasma gondii (CHEMBL612888)
Type ORGANISM
Organism Toxoplasma gondii

Publication

Inhibition of Calcium Dependent Protein Kinase 1 (CDPK1) by Pyrazolopyrimidine Analogs Decreases Establishment and Reoccurrence of Central Nervous System Disease by Toxoplasma gondii.
Rutaganira FU, Barks J, Dhason MS, Wang Q, Lopez MS, Long S, Radke JB, Jones NG, Maddirala AR, Janetka JW, El Bakkouri M, Hui R, Shokat KM, Sibley LD.
J Med Chem (2017) 60 : 9976 -9989
PubMed 28933846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 6.11 6.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4094646 1 6.79
CHEMBL2324597 1 6.78
CHEMBL4086945 1 6.72
CHEMBL4090858 1 6.62
CHEMBL4102392 1 6.61
CHEMBL4069991 1 6.58
CHEMBL4078124 1 6.52
CHEMBL4074754 1 6.43
CHEMBL4093769 1 6.36
CHEMBL4087915 1 6.30
CHEMBL4097112 1 6.27
CHEMBL2324593 1 6.21
CHEMBL4069866 1 6.14
CHEMBL4096137 1 6.10
CHEMBL4088534 1 6.00
CHEMBL4098707 1 6.00
CHEMBL4065764 1 5.95
CHEMBL4060191 1 5.74
CHEMBL4090973 1 5.74
CHEMBL4065140 1 5.72
CHEMBL4068845 1 5.58
CHEMBL4095218 1 5.53
CHEMBL4098582 1 5.46
CHEMBL4073069 1 5.39
CHEMBL4080552 1 5.22
CHEMBL4067196 1 -
CHEMBL4088414 1 -
CHEMBL4080665 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4094646 EC50 = 163.0 nM 6.79
CHEMBL2324597 EC50 = 167.0 nM 6.78
CHEMBL4086945 EC50 = 190.0 nM 6.72
CHEMBL4090858 EC50 = 242.0 nM 6.62
CHEMBL4102392 EC50 = 246.0 nM 6.61
CHEMBL4069991 EC50 = 264.0 nM 6.58
CHEMBL4078124 EC50 = 305.0 nM 6.52
CHEMBL4074754 EC50 = 367.0 nM 6.43
CHEMBL4093769 EC50 = 437.0 nM 6.36
CHEMBL4087915 EC50 = 497.0 nM 6.30
CHEMBL4097112 EC50 = 537.0 nM 6.27
CHEMBL2324593 EC50 = 613.0 nM 6.21
CHEMBL4069866 EC50 = 729.0 nM 6.14
CHEMBL4096137 EC50 = 799.0 nM 6.10
CHEMBL4088534 EC50 = 1000.0 nM 6.00
CHEMBL4098707 EC50 = 1004.0 nM 6.00
CHEMBL4065764 EC50 = 1131.0 nM 5.95
CHEMBL4060191 EC50 = 1821.0 nM 5.74
CHEMBL4090973 EC50 = 1803.0 nM 5.74
CHEMBL4065140 EC50 = 1897.0 nM 5.72
CHEMBL4068845 EC50 = 2653.0 nM 5.58
CHEMBL4095218 EC50 = 2979.0 nM 5.53
CHEMBL4098582 EC50 = 3476.0 nM 5.46
CHEMBL4073069 EC50 = 4091.0 nM 5.39
CHEMBL4080552 EC50 = 5976.0 nM 5.22
CHEMBL4067196 EC50 > 10000.0 nM -
CHEMBL4088414 EC50 > 10000.0 nM -
CHEMBL4080665 EC50 > 10000.0 nM -