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Compound Detail

CHEMBL408300

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N=C(N)Nc1ccc(CNC(=O)CCNC(=O)OCc2ccc(COC(=O)NCCC(=O)NCc3ccc(NC(=N)N)cc3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL408300
Phase Preclinical
Structure Type MOL
InChI Key QKOSVMOEBWMQSO-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

660.7
MW (Da)
2.16
ALogP
8
HBA
10
HBD
258.7
PSA (Ų)
0.08
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H40N10O6
MW 660.74
Aromatic Rings 3
Heavy Atoms 48
NP-Likeness -0.52

Activity Summary

Ki 2 meas. best 7.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 7.05 7.05 90.0 1
Serine protease 1
CHEMBL209
Ki 4.14 4.14 72000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 90.0 nM 7.05 Inhibitory potency against tryptase 11055355
Serine protease 1 Ki = 72000.0 nM 4.14 Inhibitory potency against trypsin 11055355

Literature References

PubMed DOI Target Context # Activities
11055355 10.1016/s0960-894x(00)00484-4 Tryptase beta-1 1
11055355 10.1016/s0960-894x(00)00484-4 Serine protease 1 1
11055355 10.1016/s0960-894x(00)00484-4 Prothrombin 1
11055355 10.1016/s0960-894x(00)00484-4 Plasminogen 1

Data from ChEMBL 36 via Core Engine