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Assay Detail

CHEMBL4729141

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Functional
Antimalarial activity against chloroquine-sensitive synchronized ring stage of Plasmodium falciparum 3D7 incubated for 48 to 52 hrs by SYBR green 1 dye based assay
31
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Development of Potent PfCLK3 Inhibitors Based on TCMDC-135051 as a New Class of Antimalarials.
Mahindra A,Janha O,Mapesa K,Sanchez-Azqueta A,Alam MM,Amambua-Ngwa A,Nwakanma DC,Tobin AB,Jamieson AG
J Med Chem (2020) 63 : 9300 -9315
PubMed 32787140 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 6.08 7.75
pEC50 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL36 PYRIMETHAMINE 4.0 1 7.75
CHEMBL4798421 2 6.75
CHEMBL4749934 2 6.60
CHEMBL4779045 2 6.51
CHEMBL4763273 2 6.42
CHEMBL4741460 2 6.34
CHEMBL4783687 2 5.93
CHEMBL4743985 2 5.90
CHEMBL4792168 2 5.84
CHEMBL531865 2 5.60
CHEMBL4776343 2 5.60
CHEMBL4750978 2 5.50
CHEMBL4787871 2 5.50
CHEMBL4783094 2 -
CHEMBL4752340 2 -
CHEMBL4799910 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL36 PYRIMETHAMINE EC50 = 18.0 nM 7.75
CHEMBL4798421 EC50 = 180.0 nM 6.75
CHEMBL4798421 EC50 = 199.53 nM 6.70
CHEMBL4749934 EC50 = 251.19 nM 6.60
CHEMBL4749934 EC50 = 270.0 nM 6.57
CHEMBL4779045 EC50 = 309.0 nM 6.51
CHEMBL4779045 EC50 = 316.23 nM 6.50
CHEMBL4763273 EC50 = 382.0 nM 6.42
CHEMBL4763273 EC50 = 398.11 nM 6.40
CHEMBL4741460 EC50 = 457.0 nM 6.34
CHEMBL4741460 EC50 = 501.19 nM 6.30
CHEMBL4783687 EC50 = 1185.0 nM 5.93
CHEMBL4743985 EC50 = 1258.93 nM 5.90
CHEMBL4743985 EC50 = 1339.0 nM 5.87
CHEMBL4792168 EC50 = 1456.0 nM 5.84
CHEMBL4792168 EC50 = 1584.89 nM 5.80
CHEMBL4776343 EC50 = 2511.89 nM 5.60
CHEMBL4783687 EC50 = 2511.89 nM 5.60
CHEMBL531865 EC50 = 2511.89 nM 5.60
CHEMBL4776343 EC50 = 2801.0 nM 5.55
CHEMBL4750978 EC50 = 3162.28 nM 5.50
CHEMBL4787871 EC50 = 3162.28 nM 5.50
CHEMBL531865 EC50 = 3167.0 nM 5.50
CHEMBL4750978 EC50 = 3272.0 nM 5.49
CHEMBL4787871 EC50 = 3529.0 nM 5.45
CHEMBL4783094 EC50 - -
CHEMBL4799910 EC50 - -
CHEMBL4783094 pEC50 - -
CHEMBL4752340 pEC50 - -
CHEMBL4799910 pEC50 - -
CHEMBL4752340 EC50 - -