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Compound Detail

CHEMBL5590645

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c1ccc2c(NCCCCCCNCCc3c[nH]cn3)c3c(nc2c1)CCCC3

Basic Information

ChEMBL ID CHEMBL5590645
Phase Preclinical
Structure Type MOL
InChI Key OCIWKQUQLWGQQC-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
5
PK Parameters
8
Publications
0
Known Names

Molecular Properties

391.6
MW (Da)
4.64
ALogP
4
HBA
3
HBD
65.6
PSA (Ų)
0.42
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H33N5
MW 391.56
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.63

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 8.7 8.7 2.0 1
Acetylcholinesterase
CHEMBL4078
IC50 8.66 8.66 2.2 1

Pharmacokinetic Data

Parameter Value Units Species
KA 236.0 nM Homo sapiens
KA 102.0 nM Homo sapiens
KA 2280.0 nM Homo sapiens
KA 500.0 nM Homo sapiens
KA 386.0 nM Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
39283654 10.1021/acs.jmedchem.4c01866 Carbonic anhydrase 1 1
39283654 10.1021/acs.jmedchem.4c01866 Carbonic anhydrase 2 1
39283654 10.1021/acs.jmedchem.4c01866 Carbonic anhydrase 4 1
39283654 10.1021/acs.jmedchem.4c01866 Carbonic anhydrase 5B, mitochondrial 1
39283654 10.1021/acs.jmedchem.4c01866 Carbonic anhydrase 7 1
39283654 10.1021/acs.jmedchem.4c01866 Acetylcholinesterase 1
39283654 10.1021/acs.jmedchem.4c01866 Cholinesterase 1
39283654 10.1021/acs.jmedchem.4c01866 Unchecked 1

Data from ChEMBL 36 via Core Engine