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Compound Detail

CHEMBL5277275

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O=C(O)[C@@H]1CN(C(=O)c2ccc(C(=O)N3C[C@@H](C(=O)N[C@H]4C[C@@H]4c4ccccc4)[C@H](C(=O)N[C@@H]4C[C@H]4c4ccccc4)C3)cc2)C[C@H]1C(=O)N[C@H]1C[C@@H]1c1ccccc1

Basic Information

ChEMBL ID CHEMBL5277275
Phase Preclinical
Structure Type MOL
InChI Key KMINHKPRVBVGTB-QNQSMATOSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

793.9
MW (Da)
4.16
ALogP
6
HBA
4
HBD
165.2
PSA (Ų)
0.17
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C47H47N5O7
MW 793.92
Aromatic Rings 4
Heavy Atoms 59
NP-Likeness -0.32

Activity Summary

EC50 1 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Toll-like receptor 1/2
CHEMBL3885643
EC50 6.7 6.7 200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Toll-like receptor 1/2 EC50 = 200.0 nM 6.7 Agonist activity at TLR2/TLR1 in human THP-1 cells 33346636

Literature References

PubMed DOI Target Context # Activities
33346636 10.1021/acs.jmedchem.0c01627 Toll-like receptor 1/2 2

Data from ChEMBL 36 via Core Engine