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Compound Detail

CHEMBL5570016

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CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)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](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CN)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(N)=O)[C@@H](C)O

Basic Information

ChEMBL ID CHEMBL5570016
Phase Preclinical
Structure Type MOL
InChI Key ZGMXUPVWRQVUKG-ONTXGEKHSA-N
5
Targets
9
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

2441.8
MW (Da)

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C103H169N43O27
MW 2441.76

Activity Summary

IC50 9 meas. best 8.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.44 7.945 3.6 4
Voltage-dependent N-type calcium channel subunit alpha-1B
CHEMBL4478
IC50 8.34 8.34 4.6 1
Neuronal acetylcholine receptor; alpha9/alpha10
CHEMBL2109238
IC50 8.3 7.945 5.0 2
Nicotinic acetylcholine receptor alpha9/alpha10
CHEMBL3038462
IC50 7.74 7.74 18.3 1
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL2492
IC50 7.36 7.36 43.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38217860 10.1021/acs.jmedchem.3c00979 Unchecked 10
38217860 10.1021/acs.jmedchem.3c00979 Neuronal acetylcholine receptor; alpha9/alpha10 6
38217860 10.1021/acs.jmedchem.3c00979 Rattus norvegicus 6
38217860 10.1021/acs.jmedchem.3c00979 Neuronal acetylcholine receptor subunit alpha-7 5
38217860 10.1021/acs.jmedchem.3c00979 Voltage-dependent N-type calcium channel subunit alpha-1B 5
38217860 10.1021/acs.jmedchem.3c00979 ADMET 4
38217860 10.1021/acs.jmedchem.3c00979 Neuronal acetylcholine receptor; alpha3/beta4 3
38217860 10.1021/acs.jmedchem.3c00979 Neuronal acetylcholine receptor; alpha4/beta2 3
38217860 10.1021/acs.jmedchem.3c00979 Neuronal acetylcholine receptor; alpha3/beta2 3
38217860 10.1021/acs.jmedchem.3c00979 Nicotinic acetylcholine receptor alpha9/alpha10 1
38217860 10.1021/acs.jmedchem.3c00979 Sodium channel protein type 9 subunit alpha 1
38217860 10.1021/acs.jmedchem.3c00979 Sodium channel protein type 10 subunit alpha 1
38217860 10.1021/acs.jmedchem.3c00979 Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 1
38217860 10.1021/acs.jmedchem.3c00979 Potassium voltage-gated channel subfamily KQT member 3 1
38217860 10.1021/acs.jmedchem.3c00979 Acid-sensing ion channel 3 1

Data from ChEMBL 36 via Core Engine