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Compound Detail

CHEMBL4460879

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CC[C@H](C)[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N2)CSSC[C@@H](C(=O)N[C@H](C(=O)O)C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]([C@@H](C)O)NC1=O

Basic Information

ChEMBL ID CHEMBL4460879
Phase Preclinical
Structure Type MOL
InChI Key DRTISZFZZALDJX-VLSRZGDXSA-N
9
Targets
14
Activities
1
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

3453.0
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C139H227N55O41S4
MW 3452.96

Activity Summary

IC50 14 meas. best 8.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nicotinic acetylcholine receptor alpha9/alpha10
CHEMBL3038462
IC50 8.34 8.1867 4.6 3
Neuronal acetylcholine receptor; alpha9/alpha10
CHEMBL2109238
IC50 7.69 7.485 20.3 2
Nicotinic acetylcholine receptor alpha1/beta1/epsilon/delta
CHEMBL3137264
IC50 6.28 6.28 520.0 1
Unchecked
CHEMBL612545
IC50 6.28 6.07 520.0 2
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL4980
IC50 6.19 6.185 650.0 2
Neuronal acetylcholine receptor; alpha3/beta2
CHEMBL1907587
IC50 6.03 6.03 940.0 1
Neuronal acetylcholine receptor; alpha2/beta2
CHEMBL1907592
IC50 5.79 5.79 1610.0 1
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907596
IC50 5.37 5.37 4290.0 1
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907593
IC50 5.16 5.16 6930.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nicotinic acetylcholine receptor alpha9/alpha10 IC50 = 4.6 nM 8.34 Antagonist activity at rat alpha9alpha10 nACh receptor expressed in Xenopus oocy... 37464764
Nicotinic acetylcholine receptor alpha9/alpha10 IC50 = 5.0 nM 8.3 Antagonist activity at rat alpha9alpha10 nAChR expressed in Xenopus laevis oocyt... 31986036
Nicotinic acetylcholine receptor alpha9/alpha10 IC50 = 12.0 nM 7.92 Antagonist activity at rat alpha9alpha10 nAChR expressed in Xenopus laevis oocyt... 31986036
Neuronal acetylcholine receptor; alpha9/alpha10 IC50 = 20.3 nM 7.69 Antagonist activity at human alpha9alpha10 nACh receptor expressed in Xenopus oo... 37464764
Neuronal acetylcholine receptor; alpha9/alpha10 IC50 = 52.0 nM 7.28 Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis ooc... 31986036
Unchecked IC50 = 520.0 nM 6.28 Antagonist activity at mouse alpha1beta1epsilondelta nAChR expressed in Xenopus ... 31986036
Nicotinic acetylcholine receptor alpha1/beta1/epsilon/delta IC50 = 520.0 nM 6.28 Antagonist activity at mouse alpha1beta1deltaepsilon nACh receptor expressed in ... 37464764
Neuronal acetylcholine receptor subunit alpha-7 IC50 = 650.0 nM 6.19 Antagonist activity at rat alpha7 nACh receptor expressed in Xenopus oocyte asse... 37464764
Neuronal acetylcholine receptor subunit alpha-7 IC50 = 660.0 nM 6.18 Antagonist activity at rat alpha7 nAChR expressed in Xenopus laevis oocytes asse... 31986036
Neuronal acetylcholine receptor; alpha3/beta2 IC50 = 940.0 nM 6.03 Antagonist activity at rat alpha3beta2 nAChR expressed in Xenopus laevis oocytes... 31986036
Unchecked IC50 = 1380.0 nM 5.86 Antagonist activity at rat alpha6alpha3beta4 nAChR expressed in Xenopus laevis o... 31986036
Neuronal acetylcholine receptor; alpha2/beta2 IC50 = 1610.0 nM 5.79 Antagonist activity at rat alpha2beta2 nAChR expressed in Xenopus laevis oocytes... 31986036
Neuronal acetylcholine receptor; alpha4/beta2 IC50 = 4290.0 nM 5.37 Antagonist activity at rat alpha4beta2 nAChR expressed in Xenopus laevis oocytes... 31986036
Neuronal acetylcholine receptor; alpha3/beta4 IC50 = 6930.0 nM 5.16 Antagonist activity at rat alpha3beta4 nAChR expressed in Xenopus laevis oocytes... 31986036

Literature References

PubMed DOI Target Context # Activities
31986036 10.1021/acs.jmedchem.9b01409 Unchecked 9
31986036 10.1021/acs.jmedchem.9b01409 Nicotinic acetylcholine receptor alpha9/alpha10 3
31986036 10.1021/acs.jmedchem.9b01409 Neuronal acetylcholine receptor; alpha9/alpha10 3
37464764 10.1021/acs.jmedchem.3c01023 Nicotinic acetylcholine receptor alpha9/alpha10 2
37464764 10.1021/acs.jmedchem.3c01023 Neuronal acetylcholine receptor subunit alpha-7 2
37464764 10.1021/acs.jmedchem.3c01023 Nicotinic acetylcholine receptor alpha1/beta1/epsilon/delta 2
37464764 10.1021/acs.jmedchem.3c01023 Unchecked 2
31986036 10.1021/acs.jmedchem.9b01409 Neuronal acetylcholine receptor subunit alpha-7 1
31986036 10.1021/acs.jmedchem.9b01409 Neuronal acetylcholine receptor; alpha3/beta2 1
31986036 10.1021/acs.jmedchem.9b01409 Neuronal acetylcholine receptor; alpha3/beta4 1
31986036 10.1021/acs.jmedchem.9b01409 Neuronal acetylcholine receptor; alpha2/beta2 1
31986036 10.1021/acs.jmedchem.9b01409 Neuronal acetylcholine receptor; alpha4/beta2 1
37464764 10.1021/acs.jmedchem.3c01023 Neuronal acetylcholine receptor; alpha9/alpha10 1
37464764 10.1021/acs.jmedchem.3c01023 ADMET 1

Data from ChEMBL 36 via Core Engine