NLX-101 [Ligand Id: 3924] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL230963 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]-methylspiperone from recombinant human D2 receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by microbeta2 scintillation counting method | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 8.6 | pKi | - | - | - | Br J Pharmacol (2009) 156: 338-53 [PMID:19154445] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by Microbeta2 scintillation counting method | B | 8.66 | pKi | 2.19 | nM | Ki | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from recombinant human 5HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by microbeta2 scintillation counting method | B | 8.66 | pKi | 2.19 | nM | Ki | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding | F | 6.41 | pEC50 | 389.05 | nM | EC50 | J Med Chem (2007) 50: 5024-5033 [PMID:17803293] |
| ChEMBL | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay | F | 6.52 | pEC50 | 302 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay | F | 6.61 | pEC50 | 245.47 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay | B | 6.71 | pEC50 | 194.98 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay | B | 6.71 | pEC50 | 194.98 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay | F | 7.22 | pEC50 | 60.26 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| ChEMBL | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay | F | 7.22 | pEC50 | 60.26 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay | B | 8.33 | pEC50 | 4.68 | nM | EC50 | J Med Chem (2019) 62: 2750-2771 [PMID:30721053] |
| ChEMBL | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay | B | 8.33 | pEC50 | 4.68 | nM | EC50 | J Med Chem (2020) 63: 10946-10971 [PMID:32883072] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity to 5HT1A receptor in rat cortex membrane | B | 8.65 | pKi | 2.24 | nM | Ki | J Med Chem (2007) 50: 5024-5033 [PMID:17803293] |
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]
