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Compound Detail

CHEMBL477

ADENOSINE
💊 Approved Drug
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💊 Approved Drug
Nc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL477
Name ADENOSINE
Phase Approved
Structure Type MOL
InChI Key OIRDTQYFTABQOQ-KQYNXXCUSA-N
Therapeutic ✓ Yes

Known Names

9-.beta.-d-ribofuranosyladenine Adenocard Adenocor Adenoscan Adenosine NSC-7652 SR 96225 SR-96225
27
Targets
132
Activities
4
Assay Types
5
PK Parameters
20
Publications
8
Known Names
20
Indications
1
Mechanisms

Molecular Properties

267.2
MW (Da)
-1.98
ALogP
9
HBA
4
HBD
139.5
PSA (Ų)
0.49
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1989
Availability Prescription
Chirality Single Enantiomer

Routes of Administration

Parenteral

Flags

Natural Product
USAN Stem -nosine
USAN Year 1988

Extended Properties

Molecular Formula C10H13N5O4
MW 267.25
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness 1.31

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Adenosine receptor agonist AGONIST Adenosine receptor

Indications

Cardiovascular Diseases Tachycardia, Paroxysmal Wolff-Parkinson-White Syndrome Angina, Stable Atrial Fibrillation Coronary Stenosis Myocardial Infarction Myocardial Infarction Myocardial Ischemia Neoplasms Neoplasms Tachycardia, Ventricular Cardiomyopathies Coronary Disease Pain Respiratory Distress Syndrome ST Elevation Myocardial Infarction Takotsubo Cardiomyopathy Inflammation Ischemia

ATC Classification

C01EB10
adenosine
Level 1: CARDIOVASCULAR SYSTEM
Level 2: CARDIAC THERAPY

Activity Summary

IC50 44 meas. best 8.94
EC50 40 meas. best 9.92
Ki 35 meas. best 8.3
Kd 13 meas. best 7.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Canis familiaris
CHEMBL373
EC50 9.92 9.92 0.1 1
Adenosine receptor A3
CHEMBL256
IC50 8.94 8.94 1.1 1
Adenosine receptor A1
CHEMBL226
IC50 8.63 8.63 2.3 1
Adenosine A2 receptor
CHEMBL2094117
Ki 8.3 7.72 5.0 3
Adenosine receptor A1
CHEMBL318
Ki 8.29 7.2386 5.1 7
Adenosine receptor A3
CHEMBL256
EC50 7.87 6.6683 13.5 6
Adenosine receptor A2a
CHEMBL251
Kd 7.76 7.76 17.3 1
Adenosine receptor A2a
CHEMBL251
Ki 7.7 6.8933 20.0 3
Adenosine receptor A2a
CHEMBL251
EC50 7.6 5.98 25.1 7
Adenosine receptor A2a
CHEMBL302
Ki 7.52 7.52 30.0 1
Adenosine receptor A1
CHEMBL226
EC50 7.41 6.5075 39.0 8
Adenosine A2 receptor
CHEMBL2094257
EC50 7.29 7.29 51.3 2
Adenosine receptor A2b
CHEMBL255
EC50 7.28 4.9543 52.5 7
Adenosine receptor A3
CHEMBL3360
Ki 7.0 7.0 100.0 1
Unchecked
CHEMBL612545
IC50 6.82 5.294 150.0 5
Adenosine receptor A3
CHEMBL256
Ki 6.54 6.54 290.0 1
Adenosine receptor A1
CHEMBL226
Kd 6.53 6.53 295.1 1
HEp-2
CHEMBL614735
IC50 6.16 5.43 700.0 2
Adenosine receptor A3
CHEMBL256
Kd 6.13 6.13 740.0 1
Unchecked
CHEMBL612545
EC50 6.12 6.12 759.0 1
Adenosine receptor A1
CHEMBL226
Ki 6.09 6.09 812.8 1
Unchecked
CHEMBL612545
Ki 6.03 6.03 930.0 1
Sodium/nucleoside cotransporter 1
CHEMBL5551
Ki 5.75 5.75 1800.0 1
Adenosine receptor A1
CHEMBL318
Kd 5.71 5.71 1949.8 1
Solute carrier family 28 member 3
CHEMBL5707
Ki 5.68 5.68 2100.0 1
Solute carrier family 28 member 3
CHEMBL5707
IC50 5.48 5.48 3300.0 1
Adenosine receptor A1
CHEMBL2304404
EC50 5.47 5.47 3388.4 2
Mitogen-activated protein kinase kinase kinase 7
CHEMBL5776
Kd 5.36 4.915 4400.0 2
Sodium/nucleoside cotransporter 2
CHEMBL5780
Ki 5.28 5.28 5300.0 1
Sodium/nucleoside cotransporter 1
CHEMBL5551
IC50 5.26 5.26 5500.0 1
Sodium/nucleoside cotransporter 2
CHEMBL5780
IC50 5.26 5.26 5500.0 1
Homo sapiens
CHEMBL372
IC50 5.23 5.225 5940.0 2
Adenosine kinase
CHEMBL2982
Ki 5.05 5.05 8900.0 1
HeLa
CHEMBL399
IC50 4.97 4.485 10800.0 2
Equilibrative nucleoside transporter 1
CHEMBL1997
Ki 4.92 4.92 12000.0 1
cAMP-dependent protein kinase A
CHEMBL2111446
Ki 4.82 4.82 15000.0 1
Equilibrative nucleoside transporter 1
CHEMBL1997
IC50 4.77 4.77 17000.0 1
HepG2
CHEMBL395
IC50 4.73 4.73 18460.0 1
Phosphatidylinositol 4-kinase, PI4K
CHEMBL2096619
Ki 4.72 4.72 19200.0 1
Rattus norvegicus
CHEMBL376
IC50 4.58 4.58 26000.0 1
Phosphatidylinositol 4-kinase, PI4K
CHEMBL2096619
IC50 4.52 4.52 30300.0 1
Glyceraldehyde-3-phosphate dehydrogenase
CHEMBL2284
IC50 4.46 4.46 35000.0 1
Unchecked
CHEMBL612545
Kd 4.46 4.46 35000.0 1
Equilibrative nucleoside transporter 1
CHEMBL1997
EC50 4.2 4.2 63000.0 1
Histone-lysine N-methyltransferase, H3 lysine-79 specific
CHEMBL1795117
IC50 4.0 4.0 100000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 3.0 uL.min-1.(10^6cells)-1 Rattus norvegicus
Ka 100000000.0 M-1 -
T1/2 0.006944 hr -
T1/2 0.008333 hr Bos taurus
T1/2 0.008333 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Canis familiaris EC50 = 0.12 nM 9.92 Coronary vasoactivity in dogs 3018244
Adenosine receptor A3 IC50 = 1.148 nM 8.94 Agonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells asse... 26756468
Adenosine receptor A1 IC50 = 2.344 nM 8.63 Agonist activity at human Adenosine A1 receptor transfected in CHO-K1 cells asse... 26756468
Adenosine A2 receptor Ki = 5.0 nM 8.3 Binding affinity for Adenosine A2 receptor in corpora striata of rats using [3H]... 2374150
Adenosine receptor A1 Ki = 5.1 nM 8.29 Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor 2258897
Adenosine receptor A1 Ki = 10.0 nM 8.0 Evaluated for the binding affinity towards the Adenosine A1 receptor in corpora ... 2374150
Adenosine receptor A1 Ki = 10.0 nM 8.0 Displacement of [3H]R-PIA from rat brain membrane Adenosine A1 receptor 10841798
Adenosine receptor A1 Ki = 12.8 nM 7.89 Affinity for Adenosine A1 receptor determined by [3H]N6-cyclohexyladenosine bind... -
Adenosine receptor A1 Ki = 12.8 nM 7.89 Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of ... 2754691
Adenosine receptor A3 EC50 = 13.49 nM 7.87 Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assess... 36270633
Adenosine receptor A2a Kd = 17.3 nM 7.76 Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F... 35859869
Adenosine receptor A2a Ki = 20.0 nM 7.7 Binding affinity to A2A adenosine receptor 22104008
Adenosine receptor A2a EC50 = 25.12 nM 7.6 Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells asses... 36270633
Adenosine receptor A2a Ki = 30.0 nM 7.52 Displacement of specific [3H]-CGS- 21680 binding to adenosine A2A receptor in ra... 10841798
Adenosine A2 receptor Ki = 37.0 nM 7.43 Affinity for Adenosine A2 receptor determined by [3H]NECA binding to rat striata... -
Adenosine A2 receptor Ki = 37.0 nM 7.43 Inhibition of binding of [3H]NECA to adenosine A2 receptor of rat striatal membr... 2754691
Adenosine receptor A1 EC50 = 39.0 nM 7.41 Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibit... 22738238
Adenosine A2 receptor EC50 = 51.29 nM 7.29 Coronary arteries vasodilation at the adenosine A2 receptor in langendorff guine... 2016707
Adenosine A2 receptor EC50 = 51.29 nM 7.29 Concentration required for coronary arteries vasodilation at the A2 adenosine re... 2016708
Adenosine receptor A2b EC50 = 52.48 nM 7.28 Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells asses... 36270633

Literature References

PubMed DOI Target Context # Activities
16472241 10.2174/1570163043334794 Hepatotoxicity 18
22194678 10.1371/journal.pcbi.1002310 Hepatotoxicity 14
3585910 10.1021/jm00389a005 ADMET 12
15267242 10.1021/jm031143+ Cavia porcellus 12
36270633 10.1021/acs.jmedchem.2c01414 Adenosine receptor A1 12
7783159 10.1021/jm00012a028 CHO-K1-BH4 10
20421393 10.1128/aac.00010-10 Equilibrative nucleoside transporter 1 9
3585910 10.1021/jm00389a005 Mus musculus 9
20421393 10.1128/aac.00010-10 Unchecked 7
20421393 10.1128/aac.00010-10 Equilibrative nucleoside transporter 2 7
4045916 10.1021/jm00148a002 Coxsackievirus B4 6
4045916 10.1021/jm00148a002 Vesicular stomatitis virus 6
7365748 10.1021/jm00177a021 Canis familiaris 6
- 10.6019/CHEMBL5058564 Fibroblast 6
26756468 10.1021/acs.jmedchem.5b01402 Adenosine receptor A1 6
3862866 10.1021/jm00148a018 Erythroleukemia cell line 6
26394068 10.1021/acs.jnatprod.5b00573 Toll-like receptor 4 6
7328577 10.1021/jm00142a009 L1210 6
23084893 10.1016/j.bmcl.2012.09.088 Streptavidin 5
19943620 10.1021/np9006298 MCF7 5

Data from ChEMBL 36 via Core Engine