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Compound Detail

CHEMBL3104245

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CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](CO)NC(=O)[C@H](CCSC)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)C)C(=O)N2

Basic Information

ChEMBL ID CHEMBL3104245
Phase Preclinical
Structure Type BOTH
InChI Key XYNXUMFICNCKEN-LBSPCVAOSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

1489.8
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C58H92N18O18S5
MW 1489.82

Activity Summary

IC50 5 meas. best 8.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907593
IC50 8.44 8.17 3.6 2
Nicotinic acetylcholine receptor alpha6/alpha3/beta4
CHEMBL3137276
IC50 7.47 7.25 34.0 2
Neuronal acetylcholine receptor; alpha2/beta4
CHEMBL1907590
IC50 5.34 5.34 4550.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24200193 10.1021/jm401254c Unchecked 10
24200193 10.1021/jm401254c Nicotinic acetylcholine receptor alpha9/alpha10 2
24200193 10.1021/jm401254c Neuronal acetylcholine receptor subunit alpha-7 2
24200193 10.1021/jm401254c Neuronal acetylcholine receptor; alpha4/beta4 2
24200193 10.1021/jm401254c Neuronal acetylcholine receptor; alpha3/beta2 2
24200193 10.1021/jm401254c Neuronal acetylcholine receptor; alpha3/beta4 2
24200193 10.1021/jm401254c Nicotinic acetylcholine receptor alpha1/beta1/epsilon/delta 1
24200193 10.1021/jm401254c Nicotinic acetylcholine receptor alpha6/alpha3/beta4 1
24200193 10.1021/jm401254c Neuronal acetylcholine receptor; alpha2/beta4 1
24200193 10.1021/jm401254c Neuronal acetylcholine receptor; alpha4/beta2 1
24200193 10.1021/jm401254c Nicotinic acetylcholine receptor alpha6/alpha3/beta2/beta3 1
24200193 10.1021/jm401254c Neuronal acetylcholine receptor; alpha2/beta2 1
30252466 10.1021/acs.jmedchem.8b00967 Neuronal acetylcholine receptor; alpha3/beta4 1
30252466 10.1021/acs.jmedchem.8b00967 Nicotinic acetylcholine receptor alpha6/alpha3/beta4 1
30252466 10.1021/acs.jmedchem.8b00967 Unchecked 1

Data from ChEMBL 36 via Core Engine