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Compound Detail

CHEMBL4522506

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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](C)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]1CSSC[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](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)O)C(C)C)[C@@H](C)O

Basic Information

ChEMBL ID CHEMBL4522506
Phase Preclinical
Structure Type MOL
InChI Key KGZULMBLZSVZNR-JHKJEGEHSA-N
6
Targets
7
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

3390.8
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C139H229N55O41S2
MW 3390.84

Activity Summary

IC50 7 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nicotinic acetylcholine receptor alpha9/alpha10
CHEMBL3038462
IC50 7.85 7.85 14.0 1
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL4980
IC50 5.85 5.85 1400.0 1
Unchecked
CHEMBL612545
IC50 5.6 5.33 2490.0 2
Neuronal acetylcholine receptor; alpha2/beta2
CHEMBL1907592
IC50 5.51 5.51 3120.0 1
Neuronal acetylcholine receptor; alpha3/beta2
CHEMBL1907587
IC50 5.49 5.49 3250.0 1
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907593
IC50 5.21 5.21 6130.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31986036 10.1021/acs.jmedchem.9b01409 Unchecked 8
31986036 10.1021/acs.jmedchem.9b01409 Neuronal acetylcholine receptor subunit alpha-7 1
31986036 10.1021/acs.jmedchem.9b01409 Nicotinic acetylcholine receptor alpha9/alpha10 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; alpha2/beta4 1
31986036 10.1021/acs.jmedchem.9b01409 Neuronal acetylcholine receptor; alpha4/beta2 1
31986036 10.1021/acs.jmedchem.9b01409 Neuronal acetylcholine receptor; alpha4/beta4 1

Data from ChEMBL 36 via Core Engine