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Compound Detail

CHEMBL4172976

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CNC(=O)[C@@H](NC(=O)c1ccc(-c2ccc(CSc3ncc(F)c(=O)[nH]3)c(F)c2)o1)C(C)C

Basic Information

ChEMBL ID CHEMBL4172976
Phase Preclinical
Structure Type MOL
InChI Key WLDHKEKIONLLAU-SFHVURJKSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
7
Publications
0
Known Names

Molecular Properties

476.5
MW (Da)
3.10
ALogP
6
HBA
3
HBD
117.1
PSA (Ų)
0.34
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22F2N4O4S
MW 476.51
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.53

Activity Summary

IC50 1 meas. best 5.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 5.58 5.58 2600.0 1

Pharmacokinetic Data

Parameter Value Units Species
t1/2 - - Homo sapiens
t1/2 - - Rattus norvegicus
t1/2 - - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 2600.0 nM 5.58 Inhibition of recombinant human full length MMP13 expressed in mouse NS0 cells u... 30249495

Literature References

PubMed DOI Target Context # Activities
30249495 10.1016/j.bmc.2018.08.020 ADMET 3
30249495 10.1016/j.bmc.2018.08.020 Collagenase 3 1
30249495 10.1016/j.bmc.2018.08.020 Interstitial collagenase 1
30249495 10.1016/j.bmc.2018.08.020 72 kDa type IV collagenase 1
30249495 10.1016/j.bmc.2018.08.020 Neutrophil collagenase 1
30249495 10.1016/j.bmc.2018.08.020 Matrix metalloproteinase-9 1
30249495 10.1016/j.bmc.2018.08.020 Matrix metalloproteinase-14 1

Data from ChEMBL 36 via Core Engine