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Compound Detail

CHEMBL4869892

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CC[C@H](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(C)C)NC(=O)[C@H](CC(N)=O)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 CHEMBL4869892
Phase Preclinical
Structure Type MOL
InChI Key ATDHPNPDBDEQAK-BCTYQQKGSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

1707.0
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C68H103N23O21S4
MW 1706.98

Activity Summary

IC50 7 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nicotinic acetylcholine receptor alpha6/alpha3/beta4
CHEMBL3137285
IC50 9.7 9.7 0.2 1
Nicotinic acetylcholine receptor alpha6/alpha3/beta4
CHEMBL3137276
IC50 9.32 9.32 0.5 1
Nicotinic acetylcholine receptor alpha6/alpha3/beta2/beta3
CHEMBL3137275
IC50 6.96 6.96 111.0 1
Neuronal acetylcholine receptor; alpha3/alpha6/beta2/beta3
CHEMBL2109233
IC50 6.87 6.87 135.0 1
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907594
IC50 6.75 6.75 179.0 1
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907593
IC50 6.64 6.64 230.0 1
Unchecked
CHEMBL612545
IC50 5.4 5.4 4015.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33523678 10.1021/acs.jmedchem.0c01973 Unchecked 20
33523678 10.1021/acs.jmedchem.0c01973 Nicotinic acetylcholine receptor alpha6/alpha3/beta4 7
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha2/beta2 4
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha2/beta4 4
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha3/beta2 4
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha4/beta2 4
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor subunit alpha-7 4
33523678 10.1021/acs.jmedchem.0c01973 Nicotinic acetylcholine receptor alpha-1/beta-1/delta/epsilon 2
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha3/beta4 2
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha4/beta4 2
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha9/alpha10 2
33523678 10.1021/acs.jmedchem.0c01973 Nicotinic acetylcholine receptor alpha9/alpha10 2
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor subunit alpha-6/alpha-3 1
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha3/alpha6/beta2/beta3 1
33523678 10.1021/acs.jmedchem.0c01973 Nicotinic acetylcholine receptor alpha6/alpha3/beta2/beta3 1

Data from ChEMBL 36 via Core Engine