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Compound Detail

CHEMBL4437236

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COC(=O)Nc1ccc2c(c1)NC(=O)[C@H](C)CCC[C@H](NC(=O)c1cnn(-c3cccc(Cl)c3F)c1N)c1cc-2ccn1.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4437236
Phase Preclinical
Structure Type MOL
InChI Key IUBLYWIOJOCGNW-MJPDGKJBSA-N
Parent Compound CHEMBL4596993
Active Moiety CHEMBL4596993
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

606.1
MW (Da)
5.72
ALogP
8
HBA
4
HBD
153.3
PSA (Ų)
0.23
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H31ClF7N7O8
MW 834.10
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -1.17

Activity Summary

Ki 1 meas. best 8.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
Ki 8.47 8.47 3.4 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 15.15 ng.hr.mL-1 Rattus norvegicus
CL 45.0 mL.min-1.kg-1 Rattus norvegicus
F 4.0 % Rattus norvegicus
T1/2 0.8333 hr Homo sapiens
T1/2 1.0 hr Rattus norvegicus
T1/2 0.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31833761 10.1021/acs.jmedchem.9b01768 ADMET 11
31833761 10.1021/acs.jmedchem.9b01768 Coagulation factor XI 1
31833761 10.1021/acs.jmedchem.9b01768 Plasma 1

Data from ChEMBL 36 via Core Engine