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Compound Detail

CHEMBL4438403

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CC(C)C[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@H](NC(=O)CN)C(=O)N[C@@H](CSSC[C@@H](C(N)=O)NC1=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2

Basic Information

ChEMBL ID CHEMBL4438403
Phase Preclinical
Structure Type MOL
InChI Key WXJMNOKWJJRHJY-KZAUDZKBSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

1623.8
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C63H94N22O21S4
MW 1623.85

Activity Summary

IC50 4 meas. best 8.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nicotinic acetylcholine receptor alpha6/alpha3/beta2/beta3
CHEMBL3137275
IC50 8.62 8.62 2.4 1
Neuronal acetylcholine receptor; alpha3/beta2
CHEMBL1907587
IC50 8.47 8.47 3.4 1
Nicotinic acetylcholine receptor alpha6/alpha3/beta4
CHEMBL3137285
IC50 7.66 7.66 22.1 1
Nicotinic acetylcholine receptor alpha6/alpha3/beta4
CHEMBL3137276
IC50 6.86 6.86 137.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33523678 10.1021/acs.jmedchem.0c01973 Nicotinic acetylcholine receptor alpha6/alpha3/beta4 4
31194549 10.1021/acs.jmedchem.9b00566 Neuronal acetylcholine receptor; alpha3/beta2 2
31194549 10.1021/acs.jmedchem.9b00566 Nicotinic acetylcholine receptor alpha6/alpha3/beta2/beta3 2
31194549 10.1021/acs.jmedchem.9b00566 Unchecked 1

Data from ChEMBL 36 via Core Engine