24(S)-hydroxycholesterol [Ligand Id: 2750] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL171804 (24(S)-Hydroxychloesterol, 24(S)-Hydroxycholesterol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907604] [GtoPdb: 455, 456] [UniProtKB: Q05586, Q12879] | ||||||||
| ChEMBL | Positive allosteric modulation of recombinant human GluN1/GluN2A receptor expressed in Xenopus laevis oocytes assessed as increase in glycine/L-glutamate-induced channel current at -80 mV holding potential by two-electrode voltage clamp method | B | 6.52 | pEC50 | 300 | nM | EC50 | J Med Chem (2019) 62: 7526-7542 [PMID:31390523] |
| ChEMBL | Positive allosteric modulation of recombinant human GluN1/GluN2A receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by IonWork two-electrode voltage clamp method | B | 6.82 | pEC50 | 150 | nM | EC50 | J Med Chem (2019) 62: 7526-7542 [PMID:31390523] |
| ChEMBL | Positive allosteric modulation of recombinant human GluN1/GluN2A receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by whole cell patch clamp method | B | 6.82 | pEC50 | 150 | nM | EC50 | J Med Chem (2022) 65: 9063-9075 [PMID:35785990] |
| GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455, 456] [UniProtKB: P35439, Q00959] | ||||||||
| ChEMBL | Positive allosteric modulation of recombinant rat GluN1/GluN2A receptor expressed in Xenopus laevis oocytes assessed as increase in glycine/L-glutamate-induced channel current at -80 mV holding potential by two-electrode voltage clamp method | B | 6.19 | pEC50 | 650 | nM | EC50 | J Med Chem (2019) 62: 7526-7542 [PMID:31390523] |
| GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455, 457] [UniProtKB: Q05586, Q13224] | ||||||||
| ChEMBL | Positive allosteric modulation of recombinant human GluN1/GluN2B receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by IonWork two-electrode voltage clamp method | B | 6.28 | pEC50 | 530 | nM | EC50 | J Med Chem (2019) 62: 7526-7542 [PMID:31390523] |
| Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133] | ||||||||
| GtoPdb | - | - | 5.4 | pEC50 | - | - | - | J Biol Chem (1997) 272: 3137-40 [PMID:9013544] |
| ChEMBL | Concentration required for half maximal activity was calculated in human nuclear oxysterol receptor liver X receptor-alpha in LiSA. | B | 6.89 | pEC50 | 130 | nM | EC50 | J Med Chem (2001) 44: 886-897 [PMID:11300870] |
| RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449] | ||||||||
| ChEMBL | Displacement of 25-[3H]hydroxycholesterol from GST-tagged ROR gamma ligand binding domain (unknown origin) expressed in Escherichia coli BL21 gold (DE3) cells by radioligand competition assay | B | 8 | pKi | 10 | nM | Ki | Medchemcomm (2013) 4: 764-776 |
| Liver X receptor-β in Human [GtoPdb: 601] [UniProtKB: P55055] | ||||||||
| GtoPdb | - | - | 5.5 | pEC50 | - | - | - | J Biol Chem (1997) 272: 3137-40 [PMID:9013544] |
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]
