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Compound Detail

CHEMBL75531

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N=C(N)c1ccc(C(=O)NCCC2CCN(C(=O)NCCC(c3ccccc3)c3ccccc3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL75531
Phase Preclinical
Structure Type MOL
InChI Key RWDVSBLGMMLBCU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

511.7
MW (Da)
4.73
ALogP
3
HBA
4
HBD
111.3
PSA (Ų)
0.23
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H37N5O2
MW 511.67
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.80

Activity Summary

Ki 1 meas. best 4.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 4.96 4.96 11000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 11000.0 nM 4.96 Inhibitory activity against human tryptase enzyme 11527724

Literature References

PubMed DOI Target Context # Activities
11527724 10.1016/s0960-894x(01)00444-9 Tryptase beta-1 1
11527724 10.1016/s0960-894x(01)00444-9 Unchecked 1

Data from ChEMBL 36 via Core Engine