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Compound Detail

CHEMBL339385

DIADENOSINE TETRAPHOSPHATE
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Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL339385
Name DIADENOSINE TETRAPHOSPHATE
Phase Preclinical
Structure Type MOL
InChI Key YOAHKNVSNCMZGQ-XPWFQUROSA-N
8
Targets
19
Activities
2
Assay Types
5
PK Parameters
20
Publications
0
Known Names

Molecular Properties

836.4
MW (Da)
-2.45
ALogP
25
HBA
10
HBD
434.0
PSA (Ų)
0.06
QED
3
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C20H28N10O19P4
MW 836.39
Aromatic Rings 4
Heavy Atoms 53
NP-Likeness 0.69

Activity Summary

EC50 17 meas. best 6.84
IC50 2 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 2
CHEMBL4398
EC50 6.84 6.2491 145.0 11
P2X purinoceptor 1
CHEMBL2094
EC50 6.74 6.74 182.0 1
P2X purinoceptor 3
CHEMBL2998
EC50 6.3 6.3 500.0 1
P2X purinoceptor 4
CHEMBL2104
EC50 6.0 6.0 1000.0 1
Unchecked
CHEMBL612545
IC50 6.0 6.0 1000.0 1
P2Y purinoceptor 4
CHEMBL2124
EC50 5.52 5.52 3000.0 1
P2X purinoceptor 2
CHEMBL2531
EC50 4.82 4.82 15000.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 4.34 4.34 46000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.03333 hr Homo sapiens
T1/2 0.07333 hr Homo sapiens
T1/2 0.04983 hr Rattus norvegicus
T1/2 0.03333 hr Homo sapiens
T1/2 0.07333 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2Y purinoceptor 2 EC50 = 145.0 nM 6.84 Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor... 19419204
P2Y purinoceptor 2 EC50 = 167.0 nM 6.78 Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor... 19419204
P2Y purinoceptor 2 EC50 = 170.0 nM 6.77 Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutan... 19419204
P2X purinoceptor 1 EC50 = 182.0 nM 6.74 Antagonist activity against recombinant human P2X purinoceptor 1 (P2X1 ) 12213051
P2Y purinoceptor 2 EC50 = 185.0 nM 6.73 Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutan... 19419204
P2Y purinoceptor 2 EC50 = 335.0 nM 6.47 Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutan... 19419204
P2Y purinoceptor 2 EC50 = 345.0 nM 6.46 Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutan... 19419204
P2Y purinoceptor 2 EC50 = 423.0 nM 6.37 Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutan... 19419204
P2X purinoceptor 3 EC50 = 500.0 nM 6.3 Antagonist activity against recombinant human P2X purinoceptor 3 (P2X3 ) 12213051
P2Y purinoceptor 2 EC50 = 665.0 nM 6.18 Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A... 19419204
P2Y purinoceptor 2 EC50 = 720.0 nM 6.14 Evaluated for agonist activity against phospholipase C coupled recombinant human... 12213051
P2X purinoceptor 4 EC50 = 1000.0 nM 6.0 Antagonist activity against recombinant human P2X purinoceptor 4 (P2X4) 12213051
Unchecked IC50 = 1000.0 nM 6.0 Inhibition of Rous sarcoma virus p60 v-src-induced IgG phosphorylation in tumor ... 1479375
P2Y purinoceptor 2 EC50 = 1230.0 nM 5.91 Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutan... 19419204
P2Y purinoceptor 4 EC50 = 3000.0 nM 5.52 The compound was evaluated for antagonist activity against phospholipase C coupl... 12213051
P2X purinoceptor 2 EC50 = 15000.0 nM 4.82 The compound was evaluated for antagonist activity against recombinant human rec... 12213051
Proto-oncogene tyrosine-protein kinase Src IC50 = 46000.0 nM 4.34 Inhibition of p60c-src expressed in chick embryo fibroblast 1479375
P2Y purinoceptor 2 EC50 = 81000.0 nM 4.09 Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutan... 19419204

Literature References

PubMed DOI Target Context # Activities
19419204 10.1021/jm801442p P2Y purinoceptor 2 26
12672257 10.1021/jm011070z Unchecked 4
12672257 10.1021/jm011070z Rattus norvegicus 3
21757356 10.1016/j.bmc.2011.06.028 ADMET 3
26588064 10.1016/j.ejmech.2015.10.055 Plasma 2
34160227 10.1021/acs.jmedchem.1c00874 Bis(5'-adenosyl)-triphosphatase 1
12213051 10.1021/jm020046y P2Y purinoceptor 2 1
26588064 10.1016/j.ejmech.2015.10.055 Blood 1
26588064 10.1016/j.ejmech.2015.10.055 P2Y purinoceptor 12 1
26588064 10.1016/j.ejmech.2015.10.055 P2X purinoceptor 1 1
22107038 10.1021/jm2013198 ADMET 1
20175517 10.1021/jm901621h Plasma 1
20175517 10.1021/jm901621h ADMET 1
1479375 10.1021/np50089a001 Unchecked 1
1479375 10.1021/np50089a001 Proto-oncogene tyrosine-protein kinase Src 1
12213051 10.1021/jm020046y P2X purinoceptor 4 1
12213051 10.1021/jm020046y P2X purinoceptor 3 1
12213051 10.1021/jm020046y P2X purinoceptor 2 1
12213051 10.1021/jm020046y P2X purinoceptor 1 1
12213051 10.1021/jm020046y P2Y purinoceptor 4 1

Data from ChEMBL 36 via Core Engine