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Compound Detail

CHEMBL416421

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COCCOc1ccc(-c2ccc(OCC(CN3C(=O)NC(C)(C)C3=O)N(O)C=O)cc2)cc1

Basic Information

ChEMBL ID CHEMBL416421
Phase Preclinical
Structure Type MOL
InChI Key ZLPOIHFXRODFHL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

471.5
MW (Da)
2.30
ALogP
7
HBA
2
HBD
117.6
PSA (Ų)
0.16
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N3O7
MW 471.51
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.70

Activity Summary

IC50 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 8.4 8.4 4.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.0 hr Cercopithecidae

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase IC50 = 4.0 nM 8.4 In vitro inhibition of human Matrix metalloprotease-2. 11412980

Literature References

PubMed DOI Target Context # Activities
11412980 10.1016/s0960-894x(01)00032-4 Interstitial collagenase 1
11412980 10.1016/s0960-894x(01)00032-4 72 kDa type IV collagenase 1
11412980 10.1016/s0960-894x(01)00032-4 ADMET 1

Data from ChEMBL 36 via Core Engine