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Compound Detail

CHEMBL173941

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Nc1nc(N2CCN(Cc3c(F)cc(F)cc3F)CC2)nc2nc(-c3ccco3)nn12

Basic Information

ChEMBL ID CHEMBL173941
Phase Preclinical
Structure Type MOL
InChI Key MHPYRFGHBLNOJV-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
2
PK Parameters
8
Publications
0
Known Names

Molecular Properties

430.4
MW (Da)
2.10
ALogP
9
HBA
1
HBD
101.6
PSA (Ų)
0.53
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H17F3N8O
MW 430.39
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -2.00

Activity Summary

Ki 4 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL302
Ki 8.52 8.52 3.0 3
Adenosine receptor A1
CHEMBL318
Ki 5.89 5.89 1300.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 3.0 % Rattus norvegicus
T1/2 0.9 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15294001 10.1021/jm0498405 Rattus norvegicus 4
15771443 10.1021/jm0498396 Adenosine receptor A2a 1
15771443 10.1021/jm0498396 Adenosine receptor A1 1
15341934 10.1016/j.bmcl.2004.07.048 Adenosine receptor A2a 1
15294001 10.1021/jm0498405 Adenosine receptor A2a 1
15294001 10.1021/jm0498405 Adenosine receptor A1 1
15294001 10.1021/jm0498405 Mus musculus 1
15294001 10.1021/jm0498405 ADMET 1

Data from ChEMBL 36 via Core Engine