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Compound Detail

CHEMBL290077

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Nc1nc(F)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL290077
Phase Preclinical
Structure Type MOL
InChI Key HBUBKKRHXORPQB-UUOKFMHZSA-N
5
Targets
26
Activities
3
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

285.2
MW (Da)
-1.84
ALogP
9
HBA
4
HBD
139.5
PSA (Ų)
0.47
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H12FN5O4
MW 285.24
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness 1.06

Activity Summary

EC50 13 meas. best 7.16
IC50 11 meas. best 5.86
Ki 2 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 7.16 6.6729 70.0 7
Adenosine receptor A3
CHEMBL256
Ki 7.0 7.0 99.0 1
BJ
CHEMBL614358
EC50 6.91 6.395 124.0 4
Unchecked
CHEMBL612545
IC50 5.86 4.9878 1370.0 9
Jurkat
CHEMBL397
IC50 5.63 5.63 2350.0 1
Adenosine receptor A3
CHEMBL256
EC50 5.58 5.58 2660.0 1
Unchecked
CHEMBL612545
Ki 5.57 5.57 2710.0 1
Heat shock factor protein 1
CHEMBL5313
EC50 5.26 5.26 5464.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 70.0 nM 7.16 PUBCHEM_BIOASSAY: Luminescence Cell-Based HTS Dose Confirmation to Identify Inhi... -
Unchecked EC50 = 84.0 nM 7.08 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response to Identify Inhibitors o... -
Adenosine receptor A3 Ki = 99.0 nM 7.0 Affinity for human Adenosine A3 receptor expressed in CHO cell 12238926
BJ EC50 = 124.0 nM 6.91 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 199.0 nM 6.7 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response to Identify Inhibitors o... -
Unchecked EC50 = 242.0 nM 6.62 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked EC50 = 300.0 nM 6.52 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Unchecked EC50 = 350.0 nM 6.46 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
BJ EC50 = 348.0 nM 6.46 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Dose Response to Characterize Compound... -
BJ EC50 = 460.0 nM 6.34 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 674.0 nM 6.17 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 1354.0 nM 5.87 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
Unchecked IC50 = 1370.0 nM 5.86 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS chemical inhibitors of both... -
Jurkat IC50 = 2350.0 nM 5.63 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS of chemical inhibitors of b... -
Adenosine receptor A3 EC50 = 2660.0 nM 5.58 Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster o... 12238926
Unchecked IC50 = 2649.0 nM 5.58 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Inhibitors of Mycobacterium... -
Unchecked Ki = 2710.0 nM 5.57 Displacement of [2,8-3H]-adenosine from Trypanosoma brucei AT1/P2 expressed in b... 24283924
Unchecked IC50 = 3757.0 nM 5.42 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -
Heat shock factor protein 1 EC50 = 5464.0 nM 5.26 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Unchecked IC50 = 7240.0 nM 5.14 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS chemical inhibitors of bot... -

Literature References

PubMed DOI Target Context # Activities
12238926 10.1021/jm020211+ Adenosine receptor A3 3
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
6620307 10.1021/jm00364a023 Adenosine deaminase 1
6620307 10.1021/jm00364a023 Bos taurus 1
24283924 10.1021/jm401530a Unchecked 1
24283924 10.1021/jm401530a Trypanosoma brucei brucei 1
28933546 10.1021/acs.jmedchem.7b01066 Unchecked 1

Data from ChEMBL 36 via Core Engine