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Compound Detail

CHEMBL131890

ATPGAMMAS
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Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(O)(O)=S)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL131890
Name ATPGAMMAS
Phase Preclinical
Structure Type MOL
InChI Key NLTUCYMLOPLUHL-KQYNXXCUSA-N
10
Targets
12
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

523.2
MW (Da)
-1.51
ALogP
14
HBA
7
HBD
262.1
PSA (Ų)
0.19
QED
3
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C10H16N5O12P3S
MW 523.25
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness 1.21

Activity Summary

EC50 12 meas. best 7.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 11
CHEMBL4867
EC50 7.2 6.36 63.1 2
P2X purinoceptor 5
CHEMBL2495
EC50 6.22 6.22 600.0 1
P2X purinoceptor 3
CHEMBL2998
EC50 6.16 6.16 690.0 1
P2X purinoceptor 6
CHEMBL2122
EC50 5.89 5.89 1300.0 1
P2Y purinoceptor 12
CHEMBL2188
EC50 5.89 5.89 1300.0 1
P2Y purinoceptor 1
CHEMBL5720
EC50 5.89 5.89 1300.0 1
P2X purinoceptor 2
CHEMBL2135
EC50 5.82 5.82 1500.0 1
P2Y purinoceptor 2
CHEMBL4398
EC50 5.76 5.76 1720.0 2
P2X purinoceptor 1
CHEMBL2094
EC50 5.64 5.64 2300.0 1
P2X purinoceptor 4
CHEMBL2818
EC50 5.64 5.64 2300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2Y purinoceptor 11 EC50 = 63.1 nM 7.2 Agonist activity at P2Y11 receptor expressed in 1321N1 cells assessed as cytosol... 17941622
P2X purinoceptor 5 EC50 = 600.0 nM 6.22 Antagonist activity against recombinant rat P2X purinoceptor 5 (P2X5) 12213051
P2X purinoceptor 3 EC50 = 690.0 nM 6.16 Antagonist activity against recombinant human P2X purinoceptor 3 (P2X3 ) 12213051
P2Y purinoceptor 1 EC50 = 1300.0 nM 5.89 Evaluated for agonist activity against phospholipase C coupled P2Y purinoceptor ... 12213051
P2Y purinoceptor 12 EC50 = 1300.0 nM 5.89 Antagonist activity against phospholipase C coupled rat P2Y purinoceptor 12 (P2Y... 12213051
P2X purinoceptor 6 EC50 = 1300.0 nM 5.89 Antagonist activity against recombinant rat P2X purinoceptor 6 (P2X6 ) 12213051
P2X purinoceptor 2 EC50 = 1500.0 nM 5.82 Antagonist activity against recombinant rat receptor P2X purinoceptor 2 (P2X2) a... 12213051
P2Y purinoceptor 2 EC50 = 1720.0 nM 5.76 Evaluated for agonist activity against phospholipase C coupled recombinant human... 12213051
P2Y purinoceptor 2 EC50 = 1720.0 nM 5.76 Agonist activity at human N-terminal HA-tagged P2Y2 receptor expressed in 1321N1... 29254895
P2X purinoceptor 1 EC50 = 2300.0 nM 5.64 Antagonist activity against recombinant human P2X purinoceptor 1 (P2X1 ) 12213051
P2X purinoceptor 4 EC50 = 2300.0 nM 5.64 Antagonist activity against recombinant rat P2X purinoceptor 4 (P2X4) at 30 uM, ... 12213051
P2Y purinoceptor 11 EC50 = 3000.0 nM 5.52 Agonist activity against phospholipase C coupled human P2Y purinoceptor 11 (P2Y1... 12213051

Literature References

PubMed DOI Target Context # Activities
23751098 10.1021/jm400197m NON-PROTEIN TARGET 2
12213051 10.1021/jm020046y P2Y purinoceptor 1 1
12213051 10.1021/jm020046y P2Y purinoceptor 2 1
12213051 10.1021/jm020046y P2Y purinoceptor 11 1
12213051 10.1021/jm020046y P2Y purinoceptor 12 1
12213051 10.1021/jm020046y P2X purinoceptor 1 1
12213051 10.1021/jm020046y P2X purinoceptor 2 1
12213051 10.1021/jm020046y P2X purinoceptor 3 1
12213051 10.1021/jm020046y P2X purinoceptor 4 1
12213051 10.1021/jm020046y P2X purinoceptor 5 1
12213051 10.1021/jm020046y P2X purinoceptor 6 1
17941622 10.1021/jm070043r P2Y purinoceptor 11 1
29254895 10.1016/j.bmc.2017.11.043 P2Y purinoceptor 2 1

Data from ChEMBL 36 via Core Engine