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Compound Detail

CHEMBL3398617

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Nc1nccc2cc(C(=O)N[C@@H](Cc3ccccc3)c3nc(-c4ccc5c(N)n[nH]c5c4)c(Cl)[nH]3)ccc12

Basic Information

ChEMBL ID CHEMBL3398617
Phase Preclinical
Structure Type MOL
InChI Key KWHJKKRXFUNBAJ-QFIPXVFZSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

523.0
MW (Da)
5.03
ALogP
6
HBA
5
HBD
151.4
PSA (Ų)
0.21
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H23ClN8O
MW 523.00
Aromatic Rings 6
Heavy Atoms 38
NP-Likeness -0.78

Activity Summary

Ki 2 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
Ki 7.72 7.72 19.0 1
Trypsin
CHEMBL2095204
Ki 6.42 6.42 380.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 49.5 mL.min-1.kg-1 Canis lupus familiaris
F 2.0 % Canis lupus familiaris
T1/2 0.14 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI Ki = 19.0 nM 7.72 Inhibition of human coagulation factor 11a at 25 degC 25728130
Trypsin Ki = 380.0 nM 6.42 Inhibition of human trypsin at 25 degC 25728130

Literature References

PubMed DOI Target Context # Activities
25728130 10.1016/j.bmcl.2015.01.028 Canis familiaris 4
25728130 10.1016/j.bmcl.2015.01.028 Coagulation factor XI 1
25728130 10.1016/j.bmcl.2015.01.028 Trypsin 1
25728130 10.1016/j.bmcl.2015.01.028 ADMET 1

Data from ChEMBL 36 via Core Engine