GW1929 [Ligand Id: 2703] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL434063 (GW1929)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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  • CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
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  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 5.06 pKi 8730 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 4.82 pIC50 14966 nM IC50 DrugMatrix in vitro pharmacology data
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) B 4.68 pKi 20915 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) B 4.43 pIC50 37254 nM IC50 DrugMatrix in vitro pharmacology data
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.09 pKi 8093 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 4.84 pIC50 14318 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.04 pKi 9086 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 4.7 pIC50 19903 nM IC50 DrugMatrix in vitro pharmacology data
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 4.78 pKi 16564 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 4.66 pIC50 22080 nM IC50 DrugMatrix in vitro pharmacology data
CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
ChEMBL DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) B 5.26 pKi 5455 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) B 4.96 pIC50 10910 nM IC50 DrugMatrix in vitro pharmacology data
CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712]
ChEMBL DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.4 pIC50 4000 nM IC50 DrugMatrix in vitro pharmacology data
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 5.95 pKi 1131 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 5.49 pIC50 3209 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 4.97 pKi 10767 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 4.87 pIC50 13551 nM IC50 DrugMatrix in vitro pharmacology data
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) B 4.96 pIC50 10896 nM IC50 DrugMatrix in vitro pharmacology data
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.32 pKi 4836 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 4.84 pIC50 14509 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 4.4 pKi 39975 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 4.39 pIC50 40308 nM IC50 DrugMatrix in vitro pharmacology data
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
ChEMBL The compound was tested in vitro for inhibiting the 50% binding of Peroxisome proliferator activated receptor alpha B 5.5 pKi <5.5 uM Log Ki J. Med. Chem. (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL Displacement of pan-PPAR fluormone from PPARalpha LBD by TR-FRET based LanthaScreen assay B 4.26 pEC50 55300 nM EC50 J. Med. Chem. (2012) 55: 4978-4989 [PMID:22582973]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL The compound was tested in vitro for inhibiting the 50% binding of Peroxisome proliferator activated receptor delta B 6.15 pKi 6.15 uM Log Ki J. Med. Chem. (1998) 41: 5020-5036 [PMID:9836620]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA) B 6.98 pKi 104.71 nM Ki J. Med. Chem. (1998) 41: 5020-5036 [PMID:9836620]
GtoPdb - - 8.8 pKi - - - Diabetes (1999) 48: 1415-24 [PMID:10389847]
ChEMBL Tested for its ability to bind to Peroxisome proliferator activated receptor gamma using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA) B 8.84 pKi 8.84 uM Log Ki J. Med. Chem. (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA) B 8.85 pKi 1.41 nM Ki J. Med. Chem. (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARgamma LBD by TR-FRET assay B 10.3 pKi 0.05 nM Ki J Med Chem (2017) 60: 7459-7475 [PMID:28799755]
ChEMBL Ability to promote differentiation of C3H10T1/2 stem cells to adipocytes using lipogenesis assay mediated through activation of Peroxisome proliferator activated receptor gamma F 6 pEC50 <1000 nM EC50 J. Med. Chem. (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells F 6.41 pEC50 389.05 nM EC50 J. Med. Chem. (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL Competitive binding affinity to GST-tagged human PPARgamma LBD incubated for 1 to 6 hrs by TR-FRET assay B 6.89 pEC50 130 nM EC50 Bioorg Med Chem (2020) 28: 115226-115226 [PMID:31806266]
ChEMBL Partial agonist activity at PPARgamma LBD (unknown origin) assessed as increase in recruitment of coactivator peptide C33 by TR-FRET assay B 6.96 pEC50 110 nM EC50 Bioorg Med Chem (2020) 28: 115226-115226 [PMID:31806266]
ChEMBL Binding affinity to PPARgamma LBD by fluorescence polarization based competitive binding assay B 7.59 pEC50 26 nM EC50 J. Med. Chem. (2012) 55: 4978-4989 [PMID:22582973]
ChEMBL Ability to promote differentiation of C3H10T1/2 stem cells to adipocytes using lipogenesis assay mediated through activation of Peroxisome proliferator activated receptor gamma F 7.74 pEC50 18.2 nM EC50 J. Med. Chem. (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL Agonist activity at PPARgamma LBD (unknown origin) assessed as increase in recruitment of coactivator peptide fluorescein-TRAP220/DRIP by TR-FRET assay B 7.77 pEC50 17 nM EC50 J Med Chem (2020) 63: 16012-16027 [PMID:33325691]
ChEMBL Agonist activity at PPARgamma (unknown origin) by Alpha Screen assay B 7.92 pEC50 12 nM EC50 MedChemComm (2019) 10: 1412-1419 [PMID:31673308]
ChEMBL Agonist activity at human PPAR-gamma B 7.92 pEC50 12 nM EC50 J Med Chem (2016) 59: 9201-9214 [PMID:27652492]
ChEMBL Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells F 8.04 pEC50 9.12 nM EC50 J. Med. Chem. (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells F 8.04 pEC50 9.12 nM EC50 J. Med. Chem. (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL Agonist activity for Human PPAR gamma receptor in transcriptional activation assay F 8.21 pEC50 6.2 nM EC50 J. Med. Chem. (2000) 43: 527-550 [PMID:10691680]
ChEMBL Agonist activity at human PPARgamma expressed in african green monkey CV1 cells by Gal4 transactivation assay F 8.22 pEC50 6 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
ChEMBL Displacement of pan-PPAR fluormone from PPARgamma LBD by TR-FRET based LanthaScreen assay B 8.43 pEC50 3.7 nM EC50 J. Med. Chem. (2012) 55: 4978-4989 [PMID:22582973]
ChEMBL Agonist activity at PPARgamma (unknown origin) B 8.83 pEC50 1.47 nM EC50 J Med Chem (2020) 63: 10908-10920 [PMID:32886507]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
ChEMBL Compound was tested functionally in vitro for inducing 50% of the maximum alkaline phosphatase activity (Transactivation) against murine Peroxisome proliferator activated receptor gamma using transfection assay in CV-1 cells F 7.88 pEC50 13.18 nM EC50 J. Med. Chem. (1998) 41: 5020-5036 [PMID:9836620]
ChEMBL Agonist activity for murine PPAR gamma receptor in transcriptional activation assay F 7.89 pEC50 13 nM EC50 J. Med. Chem. (2000) 43: 527-550 [PMID:10691680]
ChEMBL Agonist activity at mouse PPARgamma expressed in african green monkey CV1 cells by Gal4 transactivation assay F 7.89 pEC50 13 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 5.4 pKi 3994 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 4.51 pIC50 30622 nM IC50 DrugMatrix in vitro pharmacology data
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) B 5.53 pIC50 2953 nM IC50 DrugMatrix in vitro pharmacology data

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]