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Compound Detail

CHEMBL461220

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NC(=O)[C@@]1(Cc2ccc(OCc3cc(-c4ccccc4)nc4ccccc34)c(F)c2)C[C@@H]1C(=O)NO

Basic Information

ChEMBL ID CHEMBL461220
Phase Preclinical
Structure Type MOL
InChI Key ZVRPHGZPZLMEPV-PIKZIKFNSA-N
1
Targets
5
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

485.5
MW (Da)
4.16
ALogP
5
HBA
3
HBD
114.5
PSA (Ų)
0.26
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 C28H24FN3O4
MW 485.52
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.70

Activity Summary

Ki 5 meas. best 9.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Disintegrin and metalloproteinase domain-containing protein 17
CHEMBL3706
Ki 9.85 9.85 0.1 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19054672 10.1016/j.bmcl.2008.11.034 Disintegrin and metalloproteinase domain-containing protein 17 1
18835710 10.1016/j.bmcl.2008.09.045 Blood 1
18835710 10.1016/j.bmcl.2008.09.045 Unchecked 1
18835710 10.1016/j.bmcl.2008.09.045 Disintegrin and metalloproteinase domain-containing protein 10 1
18835710 10.1016/j.bmcl.2008.09.045 Matrix metalloproteinase-14 1
18835710 10.1016/j.bmcl.2008.09.045 Matrilysin 1
18835710 10.1016/j.bmcl.2008.09.045 Stromelysin-1 1
18835710 10.1016/j.bmcl.2008.09.045 72 kDa type IV collagenase 1
18835710 10.1016/j.bmcl.2008.09.045 Interstitial collagenase 1
18835710 10.1016/j.bmcl.2008.09.045 Disintegrin and metalloproteinase domain-containing protein 17 1
18835710 10.1016/j.bmcl.2008.09.045 Caco-2 1

Data from ChEMBL 36 via Core Engine