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ChEMBL ligand: CHEMBL434063 (GW1929) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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] |
ChEMBL | Binding affinity to PPARgamma (unknown origin) by TR-FRET based LanthaScreen competitive binding assay | B | 7.15 | pKi | 70 | nM | Ki | ACS Med Chem Lett (2022) 13: 1131-1136 [PMID:35859875] |
ChEMBL | Binding affinity to PPARgamma (unknown origin) assessed as inhibition constant by Cheng-Prusoff equation analysis | B | 8.7 | pKi | 2 | nM | Ki | J Nat Prod (2022) 85: 2804-2816 [PMID:36475432] |
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 | Binding affinity to PPARgamma (unknown origin) assessed as inhibition constant by Lanthascreen TR-FRET assay relative to control | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem (2022) 54: 116564-116564 [PMID:34922307] |
ChEMBL | Binding affinity to PPARgamma (unknown origin) by TR-FRET-based competitive binding assay | B | 9 | pKi | 1 | nM | Ki | ACS Med Chem Lett (2023) 14: 425-431 [PMID:37077388] |
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 | Agonist activity at PPARgamma LBD (unknown origin) assessed as increase in recruitment of coactivator RAP250 to PPARgamma LBD by TR-FRET-based nuclear receptor coactivator assay | B | 7 | pEC50 | 100 | nM | EC50 | ACS Med Chem Lett (2023) 14: 425-431 [PMID:37077388] |
ChEMBL | Partial agonist activity at PPARgamma (unknown origin) assessed as increase in fluorescein labeled PRIP/RAP250 coactivator peptide requirement by Lanthascreen TR-FRET assay | B | 7.3 | pEC50 | 50 | nM | EC50 | J Nat Prod (2022) 85: 2804-2816 [PMID:36475432] |
ChEMBL | Agonist activity at PPARgamma (unknown origin) assessed as increase in fluorescein labeled PRIP/RAP250 coactivator peptide requirement by Lanthascreen TR-FRET assay | B | 7.4 | pEC50 | 40 | nM | EC50 | Bioorg Med Chem (2022) 54: 116564-116564 [PMID:34922307] |
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 human PPAR-gamma | B | 7.92 | pEC50 | 12 | nM | EC50 | J Med Chem (2016) 59: 9201-9214 [PMID:27652492] |
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 | 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 | Agonist activity at PPARgamma (unknown origin) assessed as increase in fluorescein labeled TRAP220/DRIP-2 coactivator peptide requirement by Lanthascreen TR-FRET assay | B | 8.3 | pEC50 | 5 | nM | EC50 | Bioorg Med Chem (2022) 54: 116564-116564 [PMID:34922307] |
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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]