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Assay Detail

CHEMBL5609713

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

Functional
Antiplasmodial activity against asexual blood stage of Plasmodium falciparum 3D7 assessed as inhibition of parasite growth incubated for 72 hrs by LDH assay
44
Total Activities
44
Compounds Tested
1
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

Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3.
Calic PPS, Ashton TD, Mansouri M, Loi K, Jarman KE, Qiu D, Lehane AM, Roy S, Rao GP, Maity B, Wittlin S, Crespo B, Gamo FJ, Deni I, Fidock DA, Chowdury M, de Koning-Ward TF, Cowman AF, Jackson PF, Baud D, Brand S, Laleu B, Sleebs BE.
Eur J Med Chem (2024) 276 : 116677 -116677
PubMed 39024967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 44 6.36 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5613291 1 8.30
CHEMBL5612285 1 7.82
CHEMBL5613620 1 7.80
CHEMBL5612641 1 7.72
CHEMBL5612724 1 7.10
CHEMBL5612163 1 6.91
CHEMBL5612025 1 6.89
CHEMBL5613408 1 6.89
CHEMBL5611999 1 6.81
CHEMBL5612240 1 6.79
CHEMBL5612287 1 6.77
CHEMBL5612686 1 6.74
CHEMBL5612132 1 6.59
CHEMBL5613193 1 6.58
CHEMBL5612722 1 6.54
CHEMBL5613537 1 6.51
CHEMBL5612135 1 6.34
CHEMBL5614323 1 6.33
CHEMBL5613878 1 6.31
CHEMBL5614134 1 6.26
CHEMBL5612162 1 6.24
CHEMBL5614092 1 6.20
CHEMBL581128 1 6.17
CHEMBL5613594 1 6.13
CHEMBL5613052 1 6.07
CHEMBL5613130 1 6.07
CHEMBL5614146 1 6.07
CHEMBL5612661 1 6.00
CHEMBL5611976 1 5.98
CHEMBL5612938 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5613291 EC50 = 5.0 nM 8.30
CHEMBL5612285 EC50 = 15.0 nM 7.82
CHEMBL5613620 EC50 = 16.0 nM 7.80
CHEMBL5612641 EC50 = 19.0 nM 7.72
CHEMBL5612724 EC50 = 79.0 nM 7.10
CHEMBL5612163 EC50 = 123.0 nM 6.91
CHEMBL5612025 EC50 = 130.0 nM 6.89
CHEMBL5613408 EC50 = 130.0 nM 6.89
CHEMBL5611999 EC50 = 155.0 nM 6.81
CHEMBL5612240 EC50 = 164.0 nM 6.79
CHEMBL5612287 EC50 = 170.0 nM 6.77
CHEMBL5612686 EC50 = 181.0 nM 6.74
CHEMBL5612132 EC50 = 257.0 nM 6.59
CHEMBL5613193 EC50 = 260.0 nM 6.58
CHEMBL5612722 EC50 = 288.0 nM 6.54
CHEMBL5613537 EC50 = 310.0 nM 6.51
CHEMBL5612135 EC50 = 453.0 nM 6.34
CHEMBL5614323 EC50 = 463.0 nM 6.33
CHEMBL5613878 EC50 = 490.0 nM 6.31
CHEMBL5614134 EC50 = 545.0 nM 6.26
CHEMBL5612162 EC50 = 580.0 nM 6.24
CHEMBL5614092 EC50 = 635.0 nM 6.20
CHEMBL581128 EC50 = 680.0 nM 6.17
CHEMBL5613594 EC50 = 740.0 nM 6.13
CHEMBL5613052 EC50 = 860.0 nM 6.07
CHEMBL5613130 EC50 = 843.0 nM 6.07
CHEMBL5614146 EC50 = 856.0 nM 6.07
CHEMBL5612661 EC50 = 1000.0 nM 6.00
CHEMBL5611976 EC50 = 1050.0 nM 5.98
CHEMBL5612938 EC50 = 1040.0 nM 5.98
CHEMBL5613049 EC50 = 1130.0 nM 5.95
CHEMBL5612916 EC50 = 1120.0 nM 5.95
CHEMBL5613454 EC50 = 2070.0 nM 5.68
CHEMBL5613593 EC50 = 2180.0 nM 5.66
CHEMBL5613389 EC50 = 2300.0 nM 5.64
CHEMBL5613855 EC50 = 2360.0 nM 5.63
CHEMBL5611990 EC50 = 2330.0 nM 5.63
CHEMBL5614337 EC50 = 2480.0 nM 5.61
CHEMBL5613641 EC50 = 2500.0 nM 5.60
CHEMBL5612653 EC50 = 3850.0 nM 5.42
CHEMBL5613314 EC50 = 5630.0 nM 5.25
CHEMBL5612761 EC50 > 10000.0 nM -
CHEMBL5612479 EC50 > 10000.0 nM -
CHEMBL5612608 EC50 > 10000.0 nM -