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Assay Detail

CHEMBL4325174

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 blood stream forms after 72 hrs by resazurin dye based fluorescence assay
79
Total Activities
77
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei brucei
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma brucei brucei (CHEMBL612851)
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-<i>b</i>]pyridazines for the Treatment of Human African Trypanosomiasis.
Tear WF, Bag S, Diaz-Gonzalez R, Ceballos-Pérez G, Rojas-Barros DI, Cordon-Obras C, Pérez-Moreno G, García-Hernández R, Martinez-Martinez MS, Ruiz-Perez LM, Gamarro F, Gonzalez Pacanowska D, Caffrey CR, Ferrins L, Manzano P, Navarro M, Pollastri MP.
J Med Chem (2020) 63 : 756 -783
PubMed 31846577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 79 6.54 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4548942 1 8.30
CHEMBL495696 GW778894X 1 8.20
CHEMBL526110 1 8.20
CHEMBL4580246 1 7.90
CHEMBL468963 GW779439X 1 7.80
CHEMBL4553256 1 7.70
CHEMBL4468068 1 7.70
CHEMBL4436808 2 7.70
CHEMBL187081 PYRAZOLOPYRIDAZINE 1 1 7.60
CHEMBL4444383 1 7.60
CHEMBL4551743 1 7.50
CHEMBL359554 1 7.40
CHEMBL4594155 1 7.30
CHEMBL359999 GW801372X 1 7.20
CHEMBL4445914 1 7.20
CHEMBL4536553 1 7.20
CHEMBL4473418 1 7.20
CHEMBL361894 GW806290X 1 7.20
CHEMBL4456711 1 7.20
CHEMBL4439435 1 7.10
CHEMBL4592510 1 7.10
CHEMBL4543805 1 7.00
CHEMBL4527659 1 7.00
CHEMBL4440756 1 7.00
CHEMBL4514007 2 6.82
CHEMBL4573796 1 6.80
CHEMBL4538725 1 6.80
CHEMBL4465474 1 6.80
CHEMBL364370 1 6.80
CHEMBL4556458 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4548942 EC50 = 5.012 nM 8.30
CHEMBL495696 GW778894X EC50 = 6.31 nM 8.20
CHEMBL526110 EC50 = 6.31 nM 8.20
CHEMBL4580246 EC50 = 12.59 nM 7.90
CHEMBL468963 GW779439X EC50 = 15.85 nM 7.80
CHEMBL4436808 EC50 = 19.95 nM 7.70
CHEMBL4553256 EC50 = 19.95 nM 7.70
CHEMBL4468068 EC50 = 19.95 nM 7.70
CHEMBL4436808 EC50 = 20.0 nM 7.70
CHEMBL187081 PYRAZOLOPYRIDAZINE 1 EC50 = 25.12 nM 7.60
CHEMBL4444383 EC50 = 25.12 nM 7.60
CHEMBL4551743 EC50 = 31.62 nM 7.50
CHEMBL359554 EC50 = 39.81 nM 7.40
CHEMBL4594155 EC50 = 50.12 nM 7.30
CHEMBL4536553 EC50 = 63.1 nM 7.20
CHEMBL4456711 EC50 = 63.1 nM 7.20
CHEMBL359999 GW801372X EC50 = 63.1 nM 7.20
CHEMBL4473418 EC50 = 63.1 nM 7.20
CHEMBL4445914 EC50 = 63.1 nM 7.20
CHEMBL361894 GW806290X EC50 = 63.1 nM 7.20
CHEMBL4592510 EC50 = 79.43 nM 7.10
CHEMBL4439435 EC50 = 79.43 nM 7.10
CHEMBL4440756 EC50 = 100.0 nM 7.00
CHEMBL4527659 EC50 = 100.0 nM 7.00
CHEMBL4543805 EC50 = 100.0 nM 7.00
CHEMBL4514007 EC50 = 152.0 nM 6.82
CHEMBL364370 EC50 = 158.49 nM 6.80
CHEMBL4465474 EC50 = 158.49 nM 6.80
CHEMBL4451174 EC50 = 158.49 nM 6.80
CHEMBL4514007 EC50 = 158.49 nM 6.80
CHEMBL4538725 EC50 = 158.49 nM 6.80
CHEMBL4573796 EC50 = 158.49 nM 6.80
CHEMBL4556458 EC50 = 158.49 nM 6.80
CHEMBL4568663 EC50 = 199.53 nM 6.70
CHEMBL4459827 EC50 = 199.53 nM 6.70
CHEMBL4458410 EC50 = 251.19 nM 6.60
CHEMBL4439547 EC50 = 251.19 nM 6.60
CHEMBL4545591 EC50 = 251.19 nM 6.60
CHEMBL4437208 EC50 = 251.19 nM 6.60
CHEMBL4439027 EC50 = 316.23 nM 6.50
CHEMBL525194 EC50 = 398.11 nM 6.40
CHEMBL495771 GW708336X EC50 = 398.11 nM 6.40
CHEMBL4530784 EC50 = 501.19 nM 6.30
CHEMBL4470061 EC50 = 501.19 nM 6.30
CHEMBL4449705 EC50 = 501.19 nM 6.30
CHEMBL4549995 EC50 = 630.96 nM 6.20
CHEMBL4573667 EC50 = 630.96 nM 6.20
CHEMBL364587 EC50 = 630.96 nM 6.20
CHEMBL4461016 EC50 = 630.96 nM 6.20
CHEMBL4474825 EC50 = 630.96 nM 6.20