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Compound Detail

CHEMBL57531

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Nc1ncc2cc(-c3c(Br)cccc3Br)c(N)nc2n1

Basic Information

ChEMBL ID CHEMBL57531
Phase Preclinical
Structure Type MOL
InChI Key HGIPWJYTPOHUGK-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
20
Publications
0
Known Names

Molecular Properties

395.1
MW (Da)
3.38
ALogP
5
HBA
2
HBD
90.7
PSA (Ų)
0.66
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C13H9Br2N5
MW 395.06
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.33

Activity Summary

IC50 3 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Biotin carboxylase
CHEMBL4523221
IC50 6.75 6.75 180.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL3655
IC50 5.8 5.8 1600.0 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 4.89 4.89 13000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 21.88 mL.min-1.g-1 Homo sapiens
CL 120.23 uL.min-1.(10^6cells)-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31306011 10.1021/acs.jmedchem.9b00625 Pseudomonas aeruginosa 17
36459397 10.1021/acs.jmedchem.2c01380 Escherichia coli 8
31306011 10.1021/acs.jmedchem.9b00625 Escherichia coli 8
36459397 10.1021/acs.jmedchem.2c01380 Unchecked 4
- 10.6019/CHEMBL3301361 ADMET 3
31306011 10.1021/acs.jmedchem.9b00625 Klebsiella pneumoniae 1
31306011 10.1021/acs.jmedchem.9b00625 Mitogen-activated protein kinase kinase kinase kinase 4 1
31306011 10.1021/acs.jmedchem.9b00625 Epidermal growth factor receptor 1
38134355 10.1021/acs.jmedchem.3c01831 Pseudomonas aeruginosa 1
31306011 10.1021/acs.jmedchem.9b00625 Tyrosine-protein kinase BTK 1
31306011 10.1021/acs.jmedchem.9b00625 Proto-oncogene tyrosine-protein kinase Src 1
31306011 10.1021/acs.jmedchem.9b00625 Tyrosine-protein kinase Fyn 1
31306011 10.1021/acs.jmedchem.9b00625 Tyrosine-protein kinase ABL1 1
11384237 10.1021/jm0004291 Platelet-derived growth factor receptor beta 1
31306011 10.1021/acs.jmedchem.9b00625 Acinetobacter baumannii 1
31306011 10.1021/acs.jmedchem.9b00625 Biotin carboxylase 1
- 10.6019/CHEMBL3301361 No relevant target 1
21235241 10.1021/jm101121s Unchecked 1
21235241 10.1021/jm101121s Haemophilus influenzae 1
11384237 10.1021/jm0004291 Proto-oncogene tyrosine-protein kinase Src 1

Data from ChEMBL 36 via Core Engine