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enprofylline (CID 1676) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(22)
 
 
Inactive(1204)
 
 
Inconclusive(25)
 
 
Unspecified(36)
 
 
Top Targets:
7TM GPCR Srsx(40)
 
 
 
 
7TM GPCR Srx(32)
 
 
alkPPc(14)
 
 
Tryp SPc(14)
 
 
Bcl-2 like(12)
 
 
BioAssay Types:
Screening(587)
 
 
 
Confirmatory(524)
 
 
 
 
Literature(126)
 
 
 
 
Summary(16)
 
 
BioActivity Types:
Potency(438)
 
 
 
 
IC50(45)
 
 
Ki(28)
 
 
 
EC50(13)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1012    Data Row: 1287   Total Pages: 26   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103188003]
Ki 4.73Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand [AID33176, Type: Literature]
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2
[SID103188003]
Ki 4.73Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells [AID266271, Type: Literature]Adenosine receptor A2b [gi:112938]
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3
[SID103188003]
Ki 6.4Binding affinity to human adenosine A2B receptor [AID372139, Type: Literature]Adenosine receptor A2b [gi:112938]
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4
[SID103188003]
EC50 7.2Effective concentration required in vitro for tracheal muscle (from male Hartley guinea pigs) relaxation [AID73739, Type: Literature]
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5
[SID103188003]
EC50 7.2Relexant activity on the spontaneous tone of isolated guinea pig tracheal ring chains. [AID74022, Type: Literature]
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6
[SID103188003]
Ki 32Binding affinity at Adenosine A1 receptor in rat brain cortical membrane using [3H]N6-R-phenylisopropyladenosine (R-PIA) as radioligand [AID31881, Type: Literature]
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7
[SID103188003]
Ki 32Binding affinity to human adenosine A2A receptor [AID372138, Type: Literature]Adenosine receptor A2a [gi:543740]
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8
[SID103188003]
Ki 32Binding affinity to rat adenosine A2A receptor [AID372142, Type: Literature]Adenosine receptor A2a [gi:8928539]
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9
[SID103188003]
Ki 42Displacement of [3H]CPX from human adenosine A3 receptor expressed in CHO cells [AID266272, Type: Literature]Adenosine receptor A1 [gi:231473]
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10
[SID103188003]
Ki 43.1Inhibition of cyclic AMP-phosphodiesterase ( PDE) in the supernatant of tracheal muscle homogenate [AID220054, Type: Literature]
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11
[SID103188003]
Ki 43.1Inhibition of c-AMP phosphodiesterase activity in guinea pig tracheal muscle [AID219846, Type: Literature]cAMP-specific 3',5'-cyclic phosphodiesterase 4B [gi:729163]
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12
[SID103188003]
Ki 43.1Inhibition of c-AMP phosphodiesterase activity in guinea pig tracheal muscle [AID219846, Type: Literature]cAMP-specific 3',5'-cyclic phosphodiesterase 4D [gi:12644392]
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13
[SID103188003]
Ki 43.1Inhibition of c-AMP phosphodiesterase activity in guinea pig tracheal muscle [AID219846, Type: Literature]cAMP-specific 3',5'-cyclic phosphodiesterase 4C [gi:20141263]
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14
[SID103188003]
Ki 43.1Inhibition of c-AMP phosphodiesterase activity in guinea pig tracheal muscle [AID219846, Type: Literature]cAMP-specific 3',5'-cyclic phosphodiesterase 4A [gi:116242706]
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15
[SID103188003]
Ki 44Binding affinity to human adenosine A1 receptor [AID372137, Type: Literature]Adenosine receptor A1 [gi:231473]
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16
[SID103188003]
Inhibition against A2B-Adenosine Receptor in mouse NIH 3T3 fibroblast cell membranes [AID7695, Type: Literature]Adenosine receptor A2b [gi:341940164]
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17
[SID103188003]
Effective concentration required in vitro for heart stimulation (right atrium) in guinea pig [AID75916, Type: Literature]
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18
[SID103188003]
Positive chronotropic effect on isolated guinea pig right atrium (heart stimulation). [AID75917, Type: Literature]Adenosine receptor A1 [gi:1351830]
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19
[SID103188003]
Inhibition against Adenosine A1 receptor of rat fat cell membranes [AID31695, Type: Literature]Adenosine receptor A1 [gi:2827766]
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20
[SID855784]
qHTS Assay for Spectroscopic Profiling in A350 Spectral Region [AID590, Type: other]
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21
[SID855784]
Aqueous Solubility from MLSMR Stock Solutions [AID1996, Type: other]
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22
[SID85209069]
Ligands of nucleotide-like (Class A) GPCRs [AID2061, Type: other]
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23
[SID103188003]
Ki 55Binding affinity for Adenosine A1 receptor from rat brain using [3H]-PIA as radioligand [AID31860, Type: Literature]
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24
[SID103188003]
Ki 60.7Affinity against adenosine A1 receptor in the brain membranes by the displacement of [3H]CPX. [AID32155, Type: Literature]Adenosine receptor A1 [gi:1351830]
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25
[SID103188003]
Ki 60.7Binding affinity against adenosine A1 receptor of cerebral cortex using [3H]CPX as a radioligand [AID32159, Type: Literature]Adenosine receptor A1 [gi:1351830]
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26
[SID103188003]
Ki 65Binding affinity to rat adenosine A3 receptor [AID372144, Type: Literature]Adenosine receptor A3 [gi:2506479]
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27
[SID103188003]
Ki 81Inhibition of 1 nM [3H]- N6-(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat cerebral cortical membranes [AID32491, Type: Literature]
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28
[SID103188003]
Ki 81.3Displacement of [3H]ZM-241385 from human adenosine A2a receptor expressed in HEK cells [AID266273, Type: Literature]Adenosine receptor A2a [gi:543740]
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29
[SID103188003]
Ki 89Antagonism of N-ethylcarboxamido adenosine-stimulated adenylate cyclase associated with stimulation of Adenosine A2 receptor of rat PC12 membranes [AID33897, Type: Literature]
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30
[SID103188003]
Ki 90.6Affinity against adenosine A2 receptor in the brain membranes measured by the displacement of [3H]-CPX [AID30500, Type: Literature]
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31
[SID103188003]
Ki 90.6Binding affinity against adenosine A2 receptor of striatal membrane using [3H]CGS-21680 as a radioligand [AID30624, Type: Literature]
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32
[SID103188003]
Ki 92.6Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells [AID266274, Type: Literature]Adenosine receptor A3 [gi:1351831]
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33
[SID103188003]
Ki 130Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via adenosine A2 receptor in human platelet membranes. [AID30797, Type: Literature]
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34
[SID103188003]
Ki 137Binding affinity against Adenosine A2 receptor in rat striatal membranes using [3H]5'-(N-ethylcarboxamido)-adenosine (NECA) as the ligand [AID30807, Type: Literature]
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35
[SID103188003]
Ki 137Binding affinity for Adenosine A2 receptor from rat striatum using [3H]NECA as radioligand [AID33434, Type: Literature]
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36
[SID103188003]
Ki 156Binding affinity to rat adenosine A1 receptor [AID372141, Type: Literature]Adenosine receptor A1 [gi:2827766]
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37
[SID103188003]
Ki 158Binding affinity to human adenosine A3 receptor [AID372140, Type: Literature]Adenosine receptor A3 [gi:1351831]
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38
[SID103188003]
Positive chronotropic effect, 15% increase in heart rate of male Hartley guinea pigs on intraduodenal administration (mean of 3-5 animals) [AID221857, Type: Literature]
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39
[SID103188003]
Bronchodilatory effect, 50% inhibition of spasmogen-induced response in male Hartley guinea pigs on intraduodenal administration [AID221859, Type: Literature]
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40
[SID103188003]
In vivo positive chronotropic effect on isolated guinea pig right atrium [AID223359, Type: Literature]
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41
[SID103188003]
In vivo reduction of acetylcholine-induced bronchospasm in guinea pigs by intraduodenal dose [AID223360, Type: Literature]
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42
[SID103188003]
Ratio of stimulatory activity in right atrium to relaxant activity in tracheal muscle [AID227877, Type: Literature]
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43
[SID103188003]
Bronchoselectivity, ratio of positive chronotropic action (ED15) to bronchodilator action (ED50) [AID233052, Type: Literature]
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44
[SID103188003]
Bronchoselectivity expressed as ratio of stimulatory activity in the right atrium (EC15) to relaxant activity in the tracheal muscle (EC50) [AID233055, Type: Literature]
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45
[SID103188003]
Total body clearance in human [AID425652, Type: Literature]
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46
[SID103188003]
Renal clearance in human [AID425653, Type: Literature]
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47
[SID855784]
Potency qHTS for Inhibitors of Human Acid Sphingomyelinase Assay: Native Substrate [AID624178, Type: confirmatory]acid sphingomyelinase [Homo sapiens] [gi:179095]
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48
[SID103188003]
Lipophilicity, log D of the compound [AID453203, Type: Literature]
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49
[SID103188003]
Permeability in human skin after 48 hrs by Franz cell permeability assay [AID453204, Type: Literature]
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50
[SID26751510]
qHTS profiling for inhibitors of Plasmodium falciparum proliferation [AID504749, Type: Literature]
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