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Compound Detail

CHEMBL4872191

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CC(C)C[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)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 CHEMBL4872191
Phase Preclinical
Structure Type MOL
InChI Key XFBDKMSGGGCNAI-WVHVKVEVSA-N
11
Targets
11
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

1764.1
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C69H114N30O17S4
MW 1764.13

Activity Summary

IC50 11 meas. best 8.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nicotinic acetylcholine receptor alpha6/alpha3/beta2/beta3
CHEMBL3137275
IC50 8.5 8.5 3.1 1
Neuronal acetylcholine receptor; alpha3/alpha6/beta2/beta3
CHEMBL2109233
IC50 8.26 8.26 5.5 1
Nicotinic acetylcholine receptor alpha-1/beta-1/delta/epsilon
CHEMBL4106145
IC50 6.88 6.88 131.0 1
Neuronal acetylcholine receptor; alpha9/alpha10
CHEMBL2109238
IC50 6.24 6.24 576.0 1
Nicotinic acetylcholine receptor alpha9/alpha10
CHEMBL3038462
IC50 6.18 6.18 667.0 1
Nicotinic acetylcholine receptor alpha6/alpha3/beta4
CHEMBL3137285
IC50 6.07 6.07 853.0 1
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL4980
IC50 5.4 5.4 3942.0 1
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL2492
IC50 5.25 5.25 5556.0 1
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907594
IC50 5.04 5.04 9064.0 1
Neuronal acetylcholine receptor; alpha3/beta2
CHEMBL1907587
IC50 5.02 5.02 9505.0 1
Neuronal acetylcholine receptor; alpha3/beta2
CHEMBL2109234
IC50 4.91 4.91 12200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nicotinic acetylcholine receptor alpha6/alpha3/beta2/beta3 IC50 = 3.14 nM 8.5 Inhibition of rat alpha6/alpha3beta2beta3 nAChR expressed in Xenopus laevis oocy... 33523678
Neuronal acetylcholine receptor; alpha3/alpha6/beta2/beta3 IC50 = 5.55 nM 8.26 Inhibition of human alpha6/alpha3beta2beta3 nAChR expressed in Xenopus laevis oo... 33523678
Nicotinic acetylcholine receptor alpha-1/beta-1/delta/epsilon IC50 = 131.0 nM 6.88 Inhibition of human alpha1beta1deltaepsilon nAChR expressed in Xenopus laevis oo... 33523678
Neuronal acetylcholine receptor; alpha9/alpha10 IC50 = 576.0 nM 6.24 Inhibition of human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes asse... 33523678
Nicotinic acetylcholine receptor alpha9/alpha10 IC50 = 667.0 nM 6.18 Inhibition of rat alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assess... 33523678
Nicotinic acetylcholine receptor alpha6/alpha3/beta4 IC50 = 853.0 nM 6.07 Inhibition of human alpha6/alpha3beta4 nAChR expressed in Xenopus laevis oocytes... 33523678
Neuronal acetylcholine receptor subunit alpha-7 IC50 = 3942.0 nM 5.4 Inhibition of rat alpha7 nAChR expressed in Xenopus laevis oocytes assessed as i... 33523678
Neuronal acetylcholine receptor subunit alpha-7 IC50 = 5556.0 nM 5.25 Inhibition of human alpha7 nAChR expressed in Xenopus laevis oocytes assessed as... 33523678
Neuronal acetylcholine receptor; alpha3/beta4 IC50 = 9064.0 nM 5.04 Inhibition of human alpha3beta4 nAChR expressed in Xenopus laevis oocytes assess... 33523678
Neuronal acetylcholine receptor; alpha3/beta2 IC50 = 9505.0 nM 5.02 Inhibition of rat alpha3beta2 nAChR expressed in Xenopus laevis oocytes assessed... 33523678
Neuronal acetylcholine receptor; alpha3/beta2 IC50 = 12200.0 nM 4.91 Inhibition of human alpha3beta2 nAChR expressed in Xenopus laevis oocytes assess... 33523678

Literature References

PubMed DOI Target Context # Activities
33523678 10.1021/acs.jmedchem.0c01973 Unchecked 21
33523678 10.1021/acs.jmedchem.0c01973 Nicotinic acetylcholine receptor alpha6/alpha3/beta4 9
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; alpha4/beta2 4
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha3/beta4 3
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha3/beta2 2
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha4/beta4 2
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor subunit alpha-7 2
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor subunit alpha-6/alpha-3 1
33523678 10.1021/acs.jmedchem.0c01973 Nicotinic acetylcholine receptor alpha-1/beta-1/delta/epsilon 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
33523678 10.1021/acs.jmedchem.0c01973 Neuronal acetylcholine receptor; alpha9/alpha10 1
33523678 10.1021/acs.jmedchem.0c01973 Nicotinic acetylcholine receptor alpha9/alpha10 1

Data from ChEMBL 36 via Core Engine