mevidalen [Ligand Id: 10506] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3421729 (Ly3154207, LY-3154207, LY3154207, Mevidalen) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay | F | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
| ChEMBL | Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay | F | 8.64 | pEC50 | 2.3 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
| GtoPdb | Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC20 concentration of dopamine in HEK293 cells transiently expressing human D1 receptors. | - | 8.64 | pEC50 | 2.3 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
| ChEMBL | Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay | F | 8.95 | pEC50 | 1.11 | nM | EC50 | J Med Chem (2019) 62: 128-140 [PMID:30525590] |
| D1 receptor/Dopamine D1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616] | ||||||||
| ChEMBL | Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay | F | 7.21 | pEC50 | 62.1 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
| GtoPdb | Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC20 concentration of dopamine in HEK293 cells transiently expressing mouse D1 receptors. | - | 7.21 | pEC50 | 62 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Positive allosteric modulator activity at human D5 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity to 5-HT1A receptor (unknown origin) by radioligand displacement assay | B | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (2019) 62: 8711-8732 [PMID:31532644] |
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]
