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Compound Detail

CHEMBL5572317

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CC(C)(C)[C@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)CNC(=O)CC[C@H](NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1)C(=O)O)C(=O)Nc1ccc(C(=O)N2CCN(C(=O)[C@@H](N)CN)CC2)cc1

Basic Information

ChEMBL ID CHEMBL5572317
Phase Preclinical
Structure Type MOL
InChI Key GJRRGDLZVFXOFI-XMZZPRPSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

981.5
MW (Da)
0.85
ALogP
12
HBA
8
HBD
305.4
PSA (Ų)
0.08
QED
3
Ro5 Violations
19
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H52ClF3N10O10S
MW 981.45
Aromatic Rings 3
Heavy Atoms 67
NP-Likeness -0.88

Activity Summary

IC50 1 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Matrilysin
CHEMBL4073
IC50 9.7 9.7 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Matrilysin IC50 = 0.2 nM 9.7 Inhibition of recombinant human MMP7 assessed as enzyme activity by measuring fl... 38214909

Literature References

PubMed DOI Target Context # Activities
38214909 10.1021/acs.jmedchem.3c01967 Solute carrier organic anion transporter family member 1B1 1
38214909 10.1021/acs.jmedchem.3c01967 Solute carrier organic anion transporter family member 1B3 1
38214909 10.1021/acs.jmedchem.3c01967 Matrilysin 1

Data from ChEMBL 36 via Core Engine