BAY1214784 [Ligand Id: 12784] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4537788 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Inhibition of CB1 receptor (unknown origin) | B | 5.47 | pIC50 | 3400 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968] | ||||||||
| ChEMBL | Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay | B | 8.01 | pKd | 9.83 | nM | Kd | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| ChEMBL | Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay | B | 8.26 | pKd | 5.52 | nM | Kd | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| ChEMBL | Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| ChEMBL | Binding assay (Tag Lite) | B | 7.57 | pIC50 | 27 | nM | IC50 | Data for DCP probe BAY-784 |
| ChEMBL | Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| ChEMBL | Mechanistic assay measuring cellular IP1 | F | 7.68 | pIC50 | 21 | nM | IC50 | Data for DCP probe BAY-784 |
| GtoPdb | Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay | - | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969] | ||||||||
| ChEMBL | Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG expressed in HEK293 cells assessed as reduction in channel inward tail current by whole cell voltage clamp assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Inhibition of MAPK3 (unknown origin) | B | 5.31 | pIC50 | 4900 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Inhibition of MAPK14 (unknown origin) | B | 4.97 | pIC50 | 10700 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of Sigma 2 | B | 5.96 | pKi | 1107.9 | nM | Ki | Data for DCP probe BAY-784 |
| ChEMBL | GPCRScan assay: inhibition of Sigma 2 | B | 5.96 | pKi | 1096.48 | nM | Ki | Data for DCP probe BAY-784 |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
