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Compound Detail

CHEMBL4847170

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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(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2CC#CC[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](CC(=O)O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2

Basic Information

ChEMBL ID CHEMBL4847170
Phase Preclinical
Structure Type MOL
InChI Key VSRMCPVTOJHMJM-LARGJRDBSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

1766.9
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C73H103N23O25S2
MW 1766.90

Activity Summary

IC50 1 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-B receptor
CHEMBL2111463
IC50 7.89 7.89 13.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA-B receptor IC50 = 13.0 nM 7.89 Agonist activity at human GABAB expressed in HEK293T cells co-transfected with h... 33724033

Literature References

PubMed DOI Target Context # Activities
33724033 10.1021/acs.jmedchem.0c02151 Rattus norvegicus 6
33724033 10.1021/acs.jmedchem.0c02151 GABA-B receptor 4
33724033 10.1021/acs.jmedchem.0c02151 Neuronal acetylcholine receptor subunit alpha-7 1
33724033 10.1021/acs.jmedchem.0c02151 Neuronal acetylcholine receptor; alpha9/alpha10 1
33724033 10.1021/acs.jmedchem.0c02151 Neuronal acetylcholine receptor; alpha3/beta2 1

Data from ChEMBL 36 via Core Engine