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Compound Detail

CHEMBL2347704

ACOZIBOROLE
🧪 Phase II
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🧪 Phase II
CC1(C)OB(O)c2cc(NC(=O)c3ccc(F)cc3C(F)(F)F)ccc21
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL2347704
Name ACOZIBOROLE
Phase Phase II
Structure Type MOL
InChI Key PTYGDEXEGLDNAZ-UHFFFAOYSA-N

Known Names

Acoziborol Acoziborole Sctx-7158 Scyx-7158
2
Targets
9
Activities
2
Assay Types
2
PK Parameters
11
Publications
4
Known Names
2
Indications
1
Mechanisms

Molecular Properties

367.1
MW (Da)

Drug Information

Molecule Type Small molecule
Chirality Achiral
USAN Stem -borole

Extended Properties

Molecular Formula C17H14BF4NO3
MW 367.11

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Cleavage and polyadenylation specificity factor subunit inhibitor INHIBITOR Cleavage and polyadenylation specificity factor subunit ✓ ✓

Indications

Trypanosomiasis, African Trypanosomiasis

Activity Summary

EC50 8 meas. best 6.54
IC50 1 meas. best 6.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei brucei
CHEMBL612851
 EC50 6.54 6.2467 290.0 3
Trypanosoma brucei brucei
CHEMBL612851
 IC50 6.25 6.25 556.0 1
Leishmania donovani
CHEMBL367
 EC50 5.6 5.0775 2500.0 4

Pharmacokinetic Data

Parameter Value Units Species
AUC 100000.0 ng.hr.mL-1 Rattus norvegicus
Cmax 27239.79 nM Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma brucei brucei EC50 = 290.0 nM 6.54 Antitrypanosomal activity against Trypanosoma brucei brucei 427 after 48 hrs by ... 30565932
Trypanosoma brucei brucei IC50 = 556.0 nM 6.25 Antitrypanosomal activity against Trypanosoma brucei brucei after 72 hrs by resa... 28850227
Trypanosoma brucei brucei EC50 = 794.0 nM 6.1 Antitrypanosomal activity against bloodstream form Trypanosoma brucei brucei Lis... 23597080
Trypanosoma brucei brucei EC50 = 795.0 nM 6.1 Antitrypanosomal activity against bloodstream form of trypanosoma brucei brucei ... 34711050
Leishmania donovani EC50 = 2500.0 nM 5.6 Antileishmanial activity against promastigote form of wild-type Leishmania donov... 34711050
Leishmania donovani EC50 = 2800.0 nM 5.55 Antileishmanial activity against promastigote form of Leishmania donovani overex... 34711050
Leishmania donovani EC50 = 11700.0 nM 4.93 Antileishmanial activity against promastigote form of Leishmania donovani overex... 34711050
Leishmania donovani EC50 = 59000.0 nM 4.23 Antileishmanial activity against amastigote stage of Leishmania donovani MHOM/ET... 34711050

Literature References

PubMed DOI Target Context # Activities
28187957 10.1016/j.bmc.2016.11.019 Trypanosoma brucei brucei 12
34711050 10.1021/acs.jmedchem.1c01437 Leishmania donovani 4
29191556 10.1016/j.bmcl.2017.10.067 Trypanosoma brucei brucei 2
30565932 10.1021/acs.jmedchem.8b01365 Trypanosoma brucei brucei 2
35453036 10.1016/j.bmc.2022.116748 ADMET 2
23597080 10.1021/jm400349k Trypanosoma brucei brucei 1
28850227 10.1021/acs.jmedchem.7b00315 Trypanosoma brucei brucei 1
29191556 10.1016/j.bmcl.2017.10.067 Mus musculus 1
34711050 10.1021/acs.jmedchem.1c01437 Peritoneal macrophage 1
34711050 10.1021/acs.jmedchem.1c01437 Leishmania infantum 1
34711050 10.1021/acs.jmedchem.1c01437 Trypanosoma brucei brucei 1

Data from ChEMBL 36 via Core Engine