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Compound Detail

CHEMBL3637888

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Cc1ccc(-c2cc(C(=O)Nc3cccnc3)c3cc(Br)ccc3n2)cc1

Basic Information

ChEMBL ID CHEMBL3637888
Phase Preclinical
Structure Type MOL
InChI Key MWJSPLARDCGVLH-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
2
PK Parameters
20
Publications
0
Known Names

Molecular Properties

418.3
MW (Da)
5.62
ALogP
3
HBA
1
HBD
54.9
PSA (Ų)
0.47
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H16BrN3O
MW 418.29
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -1.72

Activity Summary

EC50 3 meas. best 6.92
IC50 1 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 7.0 7.0 100.0 1
Plasmodium falciparum
CHEMBL364
EC50 6.92 6.92 120.0 2
MRC5
CHEMBL614181
EC50 4.68 4.68 21000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 5.3 mL.min-1.g-1 Mus musculus
CL 5.0 mL.min-1.g-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3832761 Plasmodium falciparum 2
27775354 10.1021/acs.jmedchem.6b01486 Plasmodium falciparum 1
- 10.6019/CHEMBL3832761 MRC5 1
27775354 10.1021/acs.jmedchem.6b01486 Unchecked 1
27775354 10.1021/acs.jmedchem.6b01486 No relevant target 1
27775354 10.1021/acs.jmedchem.6b01486 ADMET 1
27631715 10.1021/acs.jmedchem.6b00723 No relevant target 1
27631715 10.1021/acs.jmedchem.6b00723 ADMET 1
27631715 10.1021/acs.jmedchem.6b00723 MRC5 1
27631715 10.1021/acs.jmedchem.6b00723 Plasmodium falciparum 1
- 10.6019/CHEMBL4513149 Staphylococcus aureus 1
- 10.6019/CHEMBL4513149 Acinetobacter baumannii 1
- 10.6019/CHEMBL4513149 Pseudomonas aeruginosa 1
- 10.6019/CHEMBL4513149 Klebsiella pneumoniae 1
- 10.6019/CHEMBL4513149 Escherichia coli 1
- 10.6019/CHEMBL4513149 Cryptococcus neoformans 1
- 10.6019/CHEMBL4513149 Candida albicans 1
- 10.6019/CHEMBL4513101 Naegleria gruberi 1
- 10.6019/CHEMBL3987221 Porphobilinogen deaminase 1
- 10.6019/CHEMBL3987221 Ferrochelatase, mitochondrial 1

Data from ChEMBL 36 via Core Engine