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Compound Detail

CHEMBL101261

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N=C(N)c1ccc(OCCOc2ccc(-c3nc4cc(C(=N)N)ccc4[nH]3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL101261
Phase Preclinical
Structure Type MOL
InChI Key BJXTWYLLSITRJP-UHFFFAOYSA-N
6
Targets
7
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

414.5
MW (Da)
3.26
ALogP
5
HBA
5
HBD
146.9
PSA (Ų)
0.17
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22N6O2
MW 414.47
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -0.73

Activity Summary

Ki 7 meas. best 5.56

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL4471
Ki 5.56 5.56 2730.0 2
Plasminogen
CHEMBL1801
Ki 5.41 5.41 3900.0 1
Serine protease 1
CHEMBL3769
Ki 5.22 5.22 5980.0 1
Unchecked
CHEMBL612545
Ki 5.22 5.22 5980.0 1
Glandular kallikrein
CHEMBL3243909
Ki 4.95 4.95 11300.0 1
Urokinase-type plasminogen activator
CHEMBL3286
Ki 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
671460 10.1021/jm00205a005 Plasma 3
6219223 10.1021/jm00356a036 Plasminogen 1
6219223 10.1021/jm00356a036 Urokinase-type plasminogen activator 1
6219223 10.1021/jm00356a036 Prothrombin 1
6219223 10.1021/jm00356a036 Serine protease 1 1
6219223 10.1021/jm00356a036 HEp-2 1
671460 10.1021/jm00205a005 Prothrombin 1
671460 10.1021/jm00205a005 Unchecked 1
671460 10.1021/jm00205a005 Glandular kallikrein 1

Data from ChEMBL 36 via Core Engine