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Compound Detail

CHEMBL206335

RAZAXABAN
🧪 Phase II
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🧪 Phase II
CN(C)Cc1nccn1-c1ccc(NC(=O)c2cc(C(F)(F)F)nn2-c2ccc3onc(N)c3c2)c(F)c1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL206335
Name RAZAXABAN
Phase Phase II
Structure Type MOL
InChI Key OFJRNBWSFXEHSA-UHFFFAOYSA-N

Known Names

BMS-5613 Razaxaban
10
Targets
33
Activities
3
Assay Types
28
PK Parameters
20
Publications
2
Known Names

Molecular Properties

528.5
MW (Da)
4.25
ALogP
9
HBA
2
HBD
120.0
PSA (Ų)
0.32
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral
USAN Stem -xaban
USAN Year 2003

Extended Properties

Molecular Formula C24H20F4N8O2
MW 528.47
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -2.02

Activity Summary

Ki 25 meas. best 9.72
IC50 5 meas. best 6.47
EC50 3 meas. best 6.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
 Ki 9.72 9.6364 0.2 11
Coagulation factor X
CHEMBL5062
 Ki 9.72 9.72 0.2 2
Oryctolagus cuniculus
CHEMBL374
 EC50 6.47 6.47 340.0 1
Oryctolagus cuniculus
CHEMBL374
 IC50 6.47 6.47 340.0 5
Prothrombin
CHEMBL204
 Ki 6.27 6.27 540.0 6
Unchecked
CHEMBL612545
 Ki 6.22 5.865 600.0 2
Plasma
CHEMBL613424
 Ki 5.52 5.52 3000.0 1
Plasma
CHEMBL613652
 EC50 5.21 5.04 6100.0 2
Chymotrypsinogen B
CHEMBL4796
 Ki 5.07 5.07 8500.0 1
Coagulation factor IX
CHEMBL2016
 Ki 5.05 5.05 9000.0 1
Coagulation factor V
CHEMBL3618
 Ki 4.71 4.71 19700.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 18.33 mL.min-1.kg-1 Canis lupus familiaris
CL 18.33 mL.min-1.kg-1 Canis lupus familiaris
CL 18.33 mL.min-1.kg-1 Canis lupus familiaris
CL 18.33 mL.min-1.kg-1 Canis lupus familiaris
CL 18.33 mL.min-1.kg-1 Canis lupus familiaris
CL 18.33 mL.min-1.kg-1 Canis lupus familiaris
CL 18.33 mL.min-1.kg-1 Canis lupus familiaris
CL 18.33 mL.min-1.kg-1 Canis lupus familiaris
CL 18.33 mL.min-1.kg-1 Canis lupus familiaris
F 84.0 % Canis lupus familiaris
F 84.0 % Canis lupus familiaris
F 84.0 % Canis lupus familiaris
F 84.0 % Canis lupus familiaris
F 84.0 % Canis lupus familiaris
F 84.0 % Canis lupus familiaris
F 84.0 % Canis lupus familiaris
F 84.0 % Canis lupus familiaris
F 84.0 % Canis lupus familiaris
T1/2 3.4 hr Canis lupus familiaris
T1/2 5.3 hr Canis lupus familiaris
T1/2 5.3 hr Canis lupus familiaris
T1/2 0.6333 hr Homo sapiens
T1/2 5.3 hr Canis lupus familiaris
T1/2 5.3 hr Canis lupus familiaris
T1/2 5.3 hr Canis lupus familiaris
T1/2 0.6 hr Homo sapiens
T1/2 3.4 hr Canis lupus familiaris
T1/2 3.4 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.19 nM 9.72 Inhibition of factor 10a 20503967
Coagulation factor X Ki = 0.19 nM 9.72 Inhibition of human factor 10a 20100660
Coagulation factor X Ki = 0.19 nM 9.72 Binding affinity to human coagulation factor 10a 19046881
Coagulation factor X Ki = 0.19 nM 9.72 Inhibition of human factor 10a 18550370
Coagulation factor X Ki = 0.19 nM 9.72 Inhibition of human factor 10a 18054227
Coagulation factor X Ki = 0.19 nM 9.72 Inhibition of human factor 10a 18159923
Coagulation factor X Ki = 0.19 nM 9.72 Binding affinity to human factor 10a 16434195
Coagulation factor X Ki = 0.19 nM 9.72 Binding affinity to rabbit factor 10a 16434195
Coagulation factor X Ki = 0.19 nM 9.72 Binding affinity to human F10a 16730984
Coagulation factor X Ki = 0.19 nM 9.72 Binding affinity to human factor Xa 16963264
Coagulation factor X Ki = 0.19 nM 9.72 Binding affinity to human F10a 17914785
Coagulation factor X Ki = 0.19 nM 9.72 Binding affinity to rabbit F10a 17914785
Coagulation factor X Ki = 1.6 nM 8.8 Inhibition of human factor 10a 18159923
Oryctolagus cuniculus EC50 = 340.0 nM 6.47 Antithrombotic activity against iv dosed rabbit arterio-venous shunt model asses... 19046881
Oryctolagus cuniculus IC50 = 340.0 nM 6.47 Antithrombotic potency in rabbit arteriovenous shunt thrombosis model 17914785
Oryctolagus cuniculus IC50 = 340.0 nM 6.47 Inhibition of thrombus formation in rabbit arteriovenous shunt thrombosis model 17914785
Oryctolagus cuniculus IC50 = 340.0 nM 6.47 Inhibition of thrombus formation in rabbit AV shunt thrombosis model 16963264
Oryctolagus cuniculus IC50 = 340.0 nM 6.47 Antithrombotic activity in rabbit arterio-venous shunt thrombosis model 16730984
Oryctolagus cuniculus IC50 = 340.0 nM 6.47 Antithrombotic activity in iv dosed rabbit arterio-venous shunt model 16434195
Prothrombin Ki = 540.0 nM 6.27 Binding affinity to human thrombin 16434195

Literature References

PubMed DOI Target Context # Activities
16730984 10.1016/j.bmcl.2006.02.069 Canis familiaris 4
16963264 10.1016/j.bmcl.2006.08.027 Canis familiaris 4
17914785 10.1021/jm070245n Canis familiaris 4
16434195 10.1016/j.bmcl.2006.01.010 Canis familiaris 4
19046881 10.1016/j.bmcl.2008.11.049 Canis familiaris 4
18054227 10.1016/j.bmcl.2007.11.040 Canis familiaris 4
17933529 10.1016/j.bmcl.2007.09.091 Canis familiaris 4
18550370 10.1016/j.bmcl.2008.05.095 Canis familiaris 4
19046881 10.1016/j.bmcl.2008.11.049 Plasma 3
20503967 10.1021/jm100146h Canis familiaris 3
17914785 10.1021/jm070245n Oryctolagus cuniculus 2
16434195 10.1016/j.bmcl.2006.01.010 Coagulation factor X 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
16434195 10.1016/j.bmcl.2006.01.010 Coagulation factor VII 2
16434195 10.1016/j.bmcl.2006.01.010 Oryctolagus cuniculus 2
17914785 10.1021/jm070245n Coagulation factor X 2
16963264 10.1016/j.bmcl.2006.08.027 Unchecked 2
18159923 10.1021/jm701217r Coagulation factor X 2
18159923 10.1021/jm701217r Unchecked 2
16434195 10.1016/j.bmcl.2006.01.010 NON-PROTEIN TARGET 2

Data from ChEMBL 36 via Core Engine