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Assay Detail

CHEMBL3267982

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Functional
Antimalarial activity against CQ, MFQ-resistant Plasmodium falciparum TM91C235 clone Southeast asian isolate assessed as inhibition of parasite proliferation by MSF assay
ChEMBL ↗
65
Total Activities
38
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

Second generation steroidal 4-aminoquinolines are potent, dual-target inhibitors of the botulinum neurotoxin serotype A metalloprotease and P. falciparum malaria.
Videnović M, Opsenica DM, Burnett JC, Gomba L, Nuss JE, Selaković Z, Konstantinović J, Krstić M, Segan S, Zlatović M, Sciotti RJ, Bavari S, Solaja BA.
J Med Chem (2014) 57 : 4134 -4153
PubMed 24742203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 7.42 8.54
IC90 27 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3264503 — — 2 8.54
CHEMBL3264501 — — 2 8.21
CHEMBL3264190 — — 2 8.18
CHEMBL3264174 — — 2 8.17
CHEMBL3264179 — — 2 8.04
CHEMBL3264175 — — 2 7.92
CHEMBL269671 ARTEMISININ 3.0 2 7.87
CHEMBL3264171 — — 2 7.84
CHEMBL3264184 — — 2 7.82
CHEMBL3264192 — — 2 7.79
CHEMBL3264178 — — 2 7.75
CHEMBL3264191 — — 2 7.69
CHEMBL3264183 — — 2 7.65
CHEMBL3264182 — — 2 7.64
CHEMBL3264186 — — 2 7.58
CHEMBL3264188 — — 2 7.56
CHEMBL450398 — — 2 7.56
CHEMBL3264185 — — 2 7.55
CHEMBL3264187 — — 2 7.52
CHEMBL3264497 — — 1 7.49
CHEMBL172 (S,R)-MEFLOQUINE — 2 7.44
CHEMBL3264177 — — 1 7.39
CHEMBL3264181 — — 1 7.29
CHEMBL3264172 — — 1 7.26
CHEMBL3264176 — — 1 7.25
CHEMBL3264504 — — 1 7.13
CHEMBL3264505 — — 2 7.07
CHEMBL3264498 — — 2 7.05
CHEMBL3264502 — — 2 7.00
CHEMBL3264173 — — 1 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3264503 — IC50 = 2.9 nM 8.54
CHEMBL3264501 — IC50 = 6.18 nM 8.21
CHEMBL3264190 — IC50 = 6.59 nM 8.18
CHEMBL3264174 — IC50 = 6.71 nM 8.17
CHEMBL3264179 — IC50 = 9.19 nM 8.04
CHEMBL3264175 — IC50 = 11.92 nM 7.92
CHEMBL269671 ARTEMISININ IC50 = 13.4 nM 7.87
CHEMBL3264171 — IC50 = 14.54 nM 7.84
CHEMBL3264184 — IC50 = 15.21 nM 7.82
CHEMBL3264192 — IC50 = 16.34 nM 7.79
CHEMBL3264178 — IC50 = 17.64 nM 7.75
CHEMBL3264191 — IC50 = 20.33 nM 7.69
CHEMBL3264183 — IC50 = 22.26 nM 7.65
CHEMBL3264182 — IC50 = 22.97 nM 7.64
CHEMBL3264186 — IC50 = 26.4 nM 7.58
CHEMBL3264188 — IC50 = 27.6 nM 7.56
CHEMBL450398 — IC50 = 27.74 nM 7.56
CHEMBL3264185 — IC50 = 28.12 nM 7.55
CHEMBL3264187 — IC50 = 30.29 nM 7.52
CHEMBL3264497 — IC50 = 32.42 nM 7.49
CHEMBL172 (S,R)-MEFLOQUINE IC50 = 36.5 nM 7.44
CHEMBL3264177 — IC50 = 40.63 nM 7.39
CHEMBL3264181 — IC50 = 51.6 nM 7.29
CHEMBL3264172 — IC50 = 54.49 nM 7.26
CHEMBL3264176 — IC50 = 56.31 nM 7.25
CHEMBL3264504 — IC50 = 74.58 nM 7.13
CHEMBL3264505 — IC50 = 85.89 nM 7.07
CHEMBL3264498 — IC50 = 88.71 nM 7.05
CHEMBL3264502 — IC50 = 100.15 nM 7.00
CHEMBL3264173 — IC50 = 103.78 nM 6.98
CHEMBL3264508 — IC50 = 124.15 nM 6.91
CHEMBL76 CHLOROQUINE IC50 = 138.82 nM 6.86
CHEMBL3264499 — IC50 = 146.77 nM 6.83
CHEMBL3264509 — IC50 = 194.74 nM 6.71
CHEMBL3264180 — IC50 = 213.74 nM 6.67
CHEMBL3264500 — IC50 = 242.74 nM 6.62
CHEMBL3264507 — IC50 = 297.19 nM 6.53
CHEMBL3264506 — IC50 = 368.93 nM 6.43
CHEMBL3264498 — IC90 = 165.04 nM -
CHEMBL3264499 — IC90 = 220.15 nM -
CHEMBL3264500 — IC90 = 347.28 nM -
CHEMBL3264501 — IC90 = 9.2 nM -
CHEMBL3264502 — IC90 = 128.18 nM -
CHEMBL3264503 — IC90 = 3.32 nM -
CHEMBL3264505 — IC90 = 175.28 nM -
CHEMBL3264507 — IC90 = 312.51 nM -
CHEMBL76 CHLOROQUINE IC90 = 373.25 nM -
CHEMBL172 (S,R)-MEFLOQUINE IC90 = 134.07 nM -
CHEMBL269671 ARTEMISININ IC90 = 17.4 nM -
CHEMBL3264190 — IC90 = 12.59 nM -