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Compound Detail

CHEMBL1287969

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CCN1CCN(/C(=N\O)c2ccc(C#C[C@]3(CN4Cc5ccc(OC)cc5C4=O)NC(=O)NC3=O)cn2)CC1

Basic Information

ChEMBL ID CHEMBL1287969
Phase Preclinical
Structure Type MOL
InChI Key WFCALHCUTXXTKL-XGEGXCHWSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

531.6
MW (Da)
0.45
ALogP
8
HBA
3
HBD
139.7
PSA (Ų)
0.13
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H29N7O5
MW 531.57
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness -0.68

Activity Summary

Ki 1 meas. best 9.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Disintegrin and metalloproteinase domain-containing protein 17
CHEMBL3706
Ki 9.74 9.74 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Disintegrin and metalloproteinase domain-containing protein 17 Ki = 0.18 nM 9.74 Inhibition of TACE 21106451

Literature References

PubMed DOI Target Context # Activities
21106451 10.1016/j.bmcl.2010.10.081 Disintegrin and metalloproteinase domain-containing protein 17 1
21106451 10.1016/j.bmcl.2010.10.081 Blood 1

Data from ChEMBL 36 via Core Engine