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Compound Detail

CHEMBL5590046

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COC(=O)[C@H](Cc1c[nH]c2ccccc12)NCCCCCCNc1c2c(nc3ccccc13)CCCC2

Basic Information

ChEMBL ID CHEMBL5590046
Phase Preclinical
Structure Type MOL
InChI Key RZEDLBYZLHTYNU-LJAQVGFWSA-N
2
Targets
2
Activities
1
Assay Types
5
PK Parameters
8
Publications
0
Known Names

Molecular Properties

498.7
MW (Da)
5.94
ALogP
5
HBA
3
HBD
79.0
PSA (Ų)
0.17
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H38N4O2
MW 498.67
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.40

Activity Summary

IC50 2 meas. best 8.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 8.55 8.55 2.8 1
Acetylcholinesterase
CHEMBL4078
IC50 7.63 7.63 23.3 1

Pharmacokinetic Data

Parameter Value Units Species
KA 436.0 nM Homo sapiens
KA 631.0 nM Homo sapiens
KA 2230.0 nM Homo sapiens
KA 5100.0 nM Homo sapiens
KA 637.0 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