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GW 1929 (CID 6518171) - Compound BioActivity Data
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BioActivity Outcomes:
Active(43)
 
 
Inactive(189)
 
 
Inconclusive(47)
 
 
Unspecified(145)
 
 
Top Targets:
7TM GPCR Srx(20)
 
 
 
 
 
p450(20)
 
 
 
 
 
7TM GPCR Srsx(15)
 
 
 
NR LBD PPAR(12)
 
 
 
 
PLN02808(7)
 
 
BioAssay Types:
Confirmatory(213)
 
 
 
 
 
Literature(52)
 
 
 
 
Screening(12)
 
 
Summary(1)
 
 
BioActivity Types:
Potency(169)
 
 
 
 
 
IC50(119)
 
 
 
EC50(7)
 
 
 
Ki(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 351    Data Row: 424   Total Pages: 9   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103391063]
EC50 0.0037Displacement of pan-PPAR fluormone from PPARgamma LBD by TR-FRET based LanthaScreen assay [AID675851, Type: Literature]
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2
[SID103391063]
EC50 0.006Agonist activity at human PPARgamma expressed in african green monkey CV1 cells by Gal4 transactivation assay [AID459526, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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3
[SID103391063]
EC50 0.0062Agonist activity for Human PPAR gamma receptor in transcriptional activation assay [AID91246, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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4
[SID103391063]
EC50 0.013Agonist activity for murine PPAR gamma receptor in transcriptional activation assay [AID141913, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432235]
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5
[SID103391063]
EC50 0.013Agonist activity at mouse PPARgamma expressed in african green monkey CV1 cells by Gal4 transactivation assay [AID459534, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432235]
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6
[SID103391063]
EC50 0.026Binding affinity to PPARgamma LBD by fluorescence polarization based competitive binding assay [AID675850, Type: Literature]
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7
[SID11114172]
Potency 0.0316qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2D6 [AID891, Type: confirmatory]cytochrome P450 2D6 isoform 1 [Homo sapiens] [gi:40805836]
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8
[SID11111229]
Potency 1.9953qHTS Assay for Identification of Small Molecule Antagonists for Hypoxia Response Element Signaling Pathway [AID915, Type: confirmatory]hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) [Homo sapiens] [gi:32879895]
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9
[SID103391063]
IC50 2.953DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) [AID625229, Type: other]Thromboxane-A synthase [gi:254763392]
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10
[SID103391063]
IC50 3.209DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) [AID625161, Type: other]Delta-type opioid receptor [gi:311033488]
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11
[SID11114172]
Potency 3.9811qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C19 [AID899, Type: confirmatory]cytochrome P450 2C19 precursor [Homo sapiens] [gi:4503219]
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12
[SID103391063]
IC50 4DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625248, Type: other]Cytochrome P450 2C9 [gi:6686268]
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13
[SID103391063]
IC50 7.45DRUGMATRIX: Phosphodiesterase PDE4 enzyme inhibition (substrate: [3H]cAMP + cAMP) [AID625166, Type: other]
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14
[SID103391063]
IC50 7.94328Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay [AID524796, Type: Literature]
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15
[SID50104927]
Potency 8.9125qHTS for differential inhibitors of proliferation of Plasmodium falciparum line 7G8 [AID1815, Type: confirmatory]
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16
[SID50104927]
Potency 8.9125qHTS for differential inhibitors of proliferation of Plasmodium falciparum line W2 [AID1883, Type: confirmatory]
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17
[SID103391063]
IC50 10Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay [AID524791, Type: Literature]
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18
[SID103391063]
IC50 10Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay [AID524794, Type: Literature]
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19
[SID11111229]
Potency 10qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C9 [AID883, Type: confirmatory]cytochrome P450 2C9 precursor [Homo sapiens] [gi:13699818]
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20
[SID103391063]
IC50 10.896DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) [AID625184, Type: other]Epidermal growth factor receptor [gi:2811086]
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21
[SID103391063]
IC50 10.91DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) [AID625145, Type: other]Cysteinyl leukotriene receptor 1 [gi:20138087]
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22
[SID103391063]
IC50 13.551DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625256, Type: other]Sodium-dependent dopamine transporter [gi:266667]
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23
[SID103391063]
IC50 14.318DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) [AID625196, Type: other]Adenosine receptor A3 [gi:1351831]
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24
[SID103391063]
IC50 14.509DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) [AID625227, Type: other]Substance-K receptor [gi:229462950]
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25
[SID103391063]
IC50 14.966DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) [AID625194, Type: other]Adenosine receptor A1 [gi:231473]
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26
[SID103391063]
IC50 19.36DRUGMATRIX: Phosphodiesterase PDE3 enzyme inhibition (substrate: [3H]cAMP + cAMP) [AID625165, Type: other]
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27
[SID103391063]
IC50 19.903DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) [AID625202, Type: other]Alpha-2B adrenergic receptor [gi:27151763]
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28
[SID103391063]
IC50 22.08DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) [AID625206, Type: other]Beta-3 adrenergic receptor [gi:461604]
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29
[SID11114172]
Potency 25.1189qHTS Assay for Inhibitors of HSD17B4, hydroxysteroid (17-beta) dehydrogenase 4 [AID893, Type: confirmatory]Chain B, The Structure Of Wild-Type Human Hadh2 (17beta-Hydroxysteroid Dehydrogenase Type 10) Bound To Nad+ At 1.2 A [gi:122921311]
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30
[SID11114172]
Potency 25.1189qHTS Assay for Inhibitors of HSD17B4, hydroxysteroid (17-beta) dehydrogenase 4 [AID893, Type: confirmatory]Chain A, The Structure Of Wild-Type Human Hadh2 (17beta-Hydroxysteroid Dehydrogenase Type 10) Bound To Nad+ At 1.2 A [gi:122921310]
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31
[SID103391063]
IC50 30.622DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) [AID625172, Type: other]Progesterone receptor [gi:75071465]
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32
[SID11114172]
Potency 31.6228qHTS Assay for Inhibitors of GCN5L2 [AID504327, Type: confirmatory]histone acetyltransferase KAT2A [Homo sapiens] [gi:153791535]
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33
[SID103391063]
IC50 37.254DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) [AID625195, Type: other]Adenosine receptor A2a [gi:543740]
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34
[SID103391063]
IC50 40.308DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625207, Type: other]Sodium-dependent noradrenaline transporter [gi:128616]
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35
[SID103391063]
Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay [AID503296, Type: Literature]
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36
[SID103391063]
Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with retinoid X-receptor alpha by EYFP based reporter gene assay [AID503297, Type: Literature]
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37
[SID103391063]
The compound was tested in vitro for inhibiting the 50% binding of Peroxisome proliferator activated receptor delta [AID156783, Type: Literature]
View
38
[SID103391063]
The compound was tested in vitro for inhibiting the 50% binding of Peroxisome proliferator activated receptor alpha [AID156448, Type: Literature]
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39
[SID103391063]
Tested for its ability to bind to Peroxisome proliferator activated receptor gamma using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA) [AID157274, Type: Literature]
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40
[SID11114172]
Cytochrome panel assay with activity outcomes [AID1851_3, Type: other]cytochrome P450 3A4 isoform 1 [Homo sapiens] [gi:13435386]
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41
[SID11114172]
Cytochrome panel assay with activity outcomes [AID1851_1, Type: other]cytochrome P450 2C19 precursor [Homo sapiens] [gi:4503219]
View
42
[SID11114172]
qHTS Assay for Tau Filament Binding [AID596, Type: confirmatory]Microtubule-associated protein tau [Homo sapiens] [gi:92096784]
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43
[SID11114172]
Cytochrome panel assay with activity outcomes [AID1851_2, Type: other]cytochrome P450 2D6 isoform 2 [Homo sapiens] [gi:68509921]
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44
[SID11111229]
Potency 25.1189qHTS Assay for Agonists of the Thyroid Stimulating Hormone Receptor [AID926, Type: confirmatory]thyroid stimulating hormone receptor [Homo sapiens] [gi:38016895]
View
45
[SID103391063]
EC50 55.3Displacement of pan-PPAR fluormone from PPARalpha LBD by TR-FRET based LanthaScreen assay [AID675854, Type: Literature]
View
46
[SID103391063]
Ki 113240Agonist activity at PPARgamma [AID599141, Type: Literature]
View
47
[SID103391063]
IC50 DRUGMATRIX: Nicotinic Acetylcholine radioligand binding (ligand: [125I] Epibatidine) [AID625158, Type: other]
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48
[SID103391063]
DRUGMATRIX: Phorbol Ester radioligand binding (ligand: [3H] PDBu) [AID625164, Type: other]
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49
[SID103391063]
Antiproliferative activity against human PC3 cells at 3 uM after 120 hrs by MTT assay relative to DMSO [AID503319, Type: Literature]
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50
[SID103391063]
Ability to promote differentiation of C3H10T1/2 stem cells to adipocytes using lipogenesis assay mediated through activation of Peroxisome proliferator activated receptor gamma [AID157120, Type: Literature]
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