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Compound Detail

CHEMBL309465

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O=C(NO)c1c(F)cccc1S(=O)(=O)N1CCC(Oc2ccc(C(F)(F)F)cc2)CC1

Basic Information

ChEMBL ID CHEMBL309465
Phase Preclinical
Structure Type MOL
InChI Key SMUHFCXUZGSRMF-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

462.4
MW (Da)
3.20
ALogP
5
HBA
2
HBD
95.9
PSA (Ų)
0.40
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H18F4N2O5S
MW 462.42
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.40

Activity Summary

IC50 2 meas. best 8.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 8.48 8.48 3.3 1
Collagenase 3
CHEMBL280
IC50 7.91 7.91 12.2 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax - ug.mL-1 Rattus norvegicus
T1/2 - hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11549451 10.1016/s0960-894x(01)00487-5 Rattus norvegicus 3
11133099 10.1016/s0960-894x(00)00584-9 72 kDa type IV collagenase 1
11133099 10.1016/s0960-894x(00)00584-9 Collagenase 3 1
11133099 10.1016/s0960-894x(00)00584-9 Interstitial collagenase 1
11549451 10.1016/s0960-894x(01)00487-5 Interstitial collagenase 1
11549451 10.1016/s0960-894x(01)00487-5 72 kDa type IV collagenase 1
11549451 10.1016/s0960-894x(01)00487-5 Collagenase 3 1

Data from ChEMBL 36 via Core Engine