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Compound Detail

CHEMBL275206

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Oc1ccc2c(Cc3ccc(CN4CCCC4)c(Br)c3)c(-c3ccc(OCCN4CCCC4)cc3)sc2c1

Basic Information

ChEMBL ID CHEMBL275206
Phase Preclinical
Structure Type MOL
InChI Key QVDZMCVSIVITGR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

591.6
MW (Da)
7.70
ALogP
5
HBA
1
HBD
35.9
PSA (Ų)
0.22
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H35BrN2O2S
MW 591.62
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.75

Activity Summary

Ki 1 meas. best 8.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.68 8.68 2.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 2.1 nM 8.68 Binding inhibition against thrombin was measured by nonlinear regression analysi... 10201846

Literature References

PubMed DOI Target Context # Activities
10201846 10.1016/s0960-894x(99)00074-8 Prothrombin 2
10201846 10.1016/s0960-894x(99)00074-8 ADMET 2
10691691 10.1021/jm9903388 ADMET 2
10866380 10.1016/s0960-894x(00)00211-0 Prothrombin 1
10201846 10.1016/s0960-894x(99)00074-8 NON-PROTEIN TARGET 1
12036355 10.1021/jm0200299 Prothrombin 1
10691691 10.1021/jm9903388 Prothrombin 1
10691691 10.1021/jm9903388 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine