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Compound Detail

CHEMBL1801395

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O=C(NO)C1(S(=O)(=O)c2ccc(Oc3ccc(OC(F)(F)F)cc3)cc2)CCN(CCO)CC1

Basic Information

ChEMBL ID CHEMBL1801395
Phase Preclinical
Structure Type MOL
InChI Key OMFMQXSBXJDRCB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

504.5
MW (Da)
2.48
ALogP
8
HBA
3
HBD
125.4
PSA (Ų)
0.37
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23F3N2O7S
MW 504.48
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.86

Activity Summary

IC50 1 meas. best 5.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Interstitial collagenase
CHEMBL332
IC50 5.35 5.35 4500.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 2735.49 nM Rattus norvegicus
F 21.9 % Rattus norvegicus
T1/2 1.39 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20726512 10.1021/jm100669j Rattus norvegicus 4
20726512 10.1021/jm100669j Collagenase 3 1
20726512 10.1021/jm100669j 72 kDa type IV collagenase 1
20726512 10.1021/jm100669j Interstitial collagenase 1

Data from ChEMBL 36 via Core Engine