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Compound Detail

CHEMBL1688558

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Oc1c(C(Nc2ccccn2)c2ccccc2)ccc2cccnc12

Basic Information

ChEMBL ID CHEMBL1688558
Phase Preclinical
Structure Type MOL
InChI Key WHPVVFZPXKODBB-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
4
PK Parameters
20
Publications
0
Known Names

Molecular Properties

327.4
MW (Da)
4.54
ALogP
4
HBA
2
HBD
58.0
PSA (Ų)
0.58
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H17N3O
MW 327.39
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -1.00

Activity Summary

IC50 5 meas. best 5.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Botulinum neurotoxin type A
CHEMBL5192
IC50 5.82 5.775 1500.0 4
Bifunctional peptidase and (3S)-lysyl hydroxylase JMJD7
CHEMBL4879430
IC50 4.5 4.5 31640.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 13.5 hr Rattus norvegicus
T1/2 0.1433 hr Rattus norvegicus
T1/2 11.4 hr Homo sapiens
T1/2 0.4933 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19528275 10.1128/aac.00141-09 Botulinum neurotoxin type A 6
24387280 10.1021/jm4012164 Plasma 4
24387280 10.1021/jm4012164 Liver microsome 4
24387280 10.1021/jm4012164 No relevant target 2
28043798 10.1016/j.bmcl.2016.11.019 Botulinum neurotoxin type A 2
27966961 10.1021/acs.jmedchem.6b01393 Botulinum neurotoxin type A 2
- 10.6019/CHEMBL4513161 Pseudomonas aeruginosa 2
- 10.6019/CHEMBL4513161 Candida albicans 1
34048880 10.1016/j.bmcl.2021.128139 Bifunctional peptidase and (3S)-lysyl hydroxylase JMJD7 1
- 10.6019/CHEMBL4513161 HEK293 1
- 10.6019/CHEMBL4513161 Erythrocyte 1
- 10.6019/CHEMBL4513161 Staphylococcus aureus 1
- 10.6019/CHEMBL4513161 Acinetobacter baumannii 1
- 10.6019/CHEMBL4513161 Klebsiella pneumoniae 1
- 10.6019/CHEMBL4513161 Escherichia coli 1
- 10.6019/CHEMBL4513161 Cryptococcus neoformans 1
24387280 10.1021/jm4012164 Botulinum neurotoxin type A 1
19528275 10.1128/aac.00141-09 Unchecked 1
19528275 10.1128/aac.00141-09 Botulinum neurotoxin type E 1
19528275 10.1128/aac.00141-09 Botulinum neurotoxin type B 1

Data from ChEMBL 36 via Core Engine