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Compound Detail

CHEMBL2371820

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CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CS)C(=O)N[C@@H](CS)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](C(=O)N[C@@H](CS)C(N)=O)C(C)C)C(C)C

Basic Information

ChEMBL ID CHEMBL2371820
Phase Preclinical
Structure Type BOTH
InChI Key MOMRLMDRIJFWPM-QWZZPYHMSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

2145.5
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C83H137N31O28S4
MW 2145.47

Activity Summary

IC50 5 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907589
IC50 8.3 8.3 5.0 1
Neuronal acetylcholine receptor; alpha4/beta4
CHEMBL1907591
IC50 8.3 8.3 5.0 1
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907594
IC50 8.3 8.3 5.0 1
Neuronal acetylcholine receptor; alpha3/beta2
CHEMBL2109234
IC50 8.3 8.3 5.0 1
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL2492
IC50 8.3 8.3 5.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16033252 10.1021/jm040219e Neuronal acetylcholine receptor; alpha3/beta2 1
16033252 10.1021/jm040219e Neuronal acetylcholine receptor subunit alpha-7 1
16033252 10.1021/jm040219e Neuronal acetylcholine receptor; alpha4/beta2 1
16033252 10.1021/jm040219e Neuronal acetylcholine receptor; alpha3/beta4 1
16033252 10.1021/jm040219e Neuronal acetylcholine receptor; alpha4/beta4 1

Data from ChEMBL 36 via Core Engine