Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL4072836

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
CC[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)NC[C@@]1(C2CC2)NC(=O)NC1=O

Basic Information

ChEMBL ID CHEMBL4072836
Phase Preclinical
Structure Type MOL
InChI Key XTJBTJMEXZEGIF-XIKOKIGWSA-N
11
Targets
20
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

397.4
MW (Da)
2.38
ALogP
3
HBA
3
HBD
87.3
PSA (Ų)
0.62
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H22F3N3O3
MW 397.40
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -0.63

Activity Summary

IC50 20 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ADAM metallopeptidase with thrombospondin type 1 motif 4
CHEMBL3988592
IC50 9.0 7.745 1.0 2
A disintegrin and metalloproteinase with thrombospondin motifs 5
CHEMBL2285
IC50 8.7 8.3667 2.0 3
A disintegrin and metalloproteinase with thrombospondin motifs 4
CHEMBL2318
IC50 8.7 8.7 2.0 2
A disintegrin-like and metallopeptidase (Reprolysin type) with thrombospondin type 1 motif, 5 (Aggrecanase-2)
CHEMBL3988600
IC50 7.7 7.7 20.0 1
Macrophage metalloelastase
CHEMBL4393
IC50 7.58 7.58 26.0 2
Matrix metalloproteinase-9
CHEMBL321
IC50 6.36 6.36 439.0 1
72 kDa type IV collagenase
CHEMBL333
IC50 6.15 5.835 704.0 2
Interstitial collagenase
CHEMBL332
IC50 6.05 6.05 897.0 1
Collagenase 3
CHEMBL280
IC50 5.38 5.38 4189.0 2
Matrix metalloproteinase-14
CHEMBL3869
IC50 5.1 5.1 7990.0 2
Stromelysin-1
CHEMBL283
IC50 4.82 4.815 15000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
ADAM metallopeptidase with thrombospondin type 1 motif 4 IC50 = 1.0 nM 9.0 AlphaScreen Assay: The compounds of the present invention can be evaluated by us... -
A disintegrin and metalloproteinase with thrombospondin motifs 4 IC50 = 2.0 nM 8.7 AlphaScreen Assay: The compounds of the present invention can be evaluated by us... -
A disintegrin and metalloproteinase with thrombospondin motifs 5 IC50 = 2.0 nM 8.7 AlphaScreen Assay: The compounds of the present invention can be evaluated by us... -
A disintegrin and metalloproteinase with thrombospondin motifs 4 IC50 = 2.0 nM 8.7 Inhibition of human ADAMTS4 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG pe... 28613895
A disintegrin and metalloproteinase with thrombospondin motifs 5 IC50 = 2.0 nM 8.7 Inhibition of human ADAMTS5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG pe... 28613895
A disintegrin-like and metallopeptidase (Reprolysin type) with thrombospondin type 1 motif, 5 (Aggrecanase-2) IC50 = 20.0 nM 7.7 Shift AlphaScreen Assay : The AlphaScreen Assay is modified to include the testi... -
A disintegrin and metalloproteinase with thrombospondin motifs 5 IC50 = 20.0 nM 7.7 Inhibition of human ADAMTS5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG pe... 28613895
Macrophage metalloelastase IC50 = 26.0 nM 7.58 In Vitro Fluorescence Assay: A continuous assay is used in which the substrate i... -
Macrophage metalloelastase IC50 = 26.0 nM 7.58 Inhibition of human MMP12 using Mca-PQGL-(3-[2, 4-dinitrophenyl]-L-2, 3-diaminop... 28613895
ADAM metallopeptidase with thrombospondin type 1 motif 4 IC50 = 326.0 nM 6.49 Shift AlphaScreen Assay : The AlphaScreen Assay is modified to include the testi... -
Matrix metalloproteinase-9 IC50 = 439.0 nM 6.36 In Vitro Fluorescence Assay: A continuous assay is used in which the substrate i... -
72 kDa type IV collagenase IC50 = 704.0 nM 6.15 In Vitro Fluorescence Assay: A continuous assay is used in which the substrate i... -
Interstitial collagenase IC50 = 897.0 nM 6.05 In Vitro Fluorescence Assay: A continuous assay is used in which the substrate i... -
72 kDa type IV collagenase IC50 = 3000.0 nM 5.52 Inhibition of human MMP2 using Mca-PQGL-(3-[2, 4-dinitrophenyl]-L-2, 3-diaminopr... 28613895
Collagenase 3 IC50 = 4189.0 nM 5.38 In Vitro Fluorescence Assay: A continuous assay is used in which the substrate i... -
Collagenase 3 IC50 = 4200.0 nM 5.38 Inhibition of human MMP13 using Mca-PQGL-(3-[2, 4-dinitrophenyl]-L-2, 3-diaminop... 28613895
Matrix metalloproteinase-14 IC50 = 7990.0 nM 5.1 In Vitro Fluorescence Assay: A continuous assay is used in which the substrate i... -
Matrix metalloproteinase-14 IC50 = 8000.0 nM 5.1 Inhibition of human MMP14 using Mca-PQGL-(3-[2, 4-dinitrophenyl]-L-2, 3-diaminop... 28613895
Stromelysin-1 IC50 = 15000.0 nM 4.82 Inhibition of human MMP3 using Mca-PQGL-(3-[2, 4-dinitrophenyl]-L-2, 3-diaminopr... 28613895
Stromelysin-1 IC50 = 15342.0 nM 4.81 In Vitro Fluorescence Assay: A continuous assay is used in which the substrate i... -

Literature References

PubMed DOI Target Context # Activities
28613895 10.1021/acs.jmedchem.7b00650 A disintegrin and metalloproteinase with thrombospondin motifs 5 2
28613895 10.1021/acs.jmedchem.7b00650 A disintegrin and metalloproteinase with thrombospondin motifs 4 1
28613895 10.1021/acs.jmedchem.7b00650 72 kDa type IV collagenase 1
28613895 10.1021/acs.jmedchem.7b00650 Stromelysin-1 1
28613895 10.1021/acs.jmedchem.7b00650 Macrophage metalloelastase 1
28613895 10.1021/acs.jmedchem.7b00650 Collagenase 3 1
28613895 10.1021/acs.jmedchem.7b00650 Matrix metalloproteinase-14 1
28613895 10.1021/acs.jmedchem.7b00650 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine