paltusotine [Ligand Id: 14237] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL5267842 (Crn00808, CRN-00808, CRN00808, Paltusotine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| SST1 receptor/Somatostatin receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1917] [GtoPdb: 355] [UniProtKB: P30872] | ||||||||
| ChEMBL | Agonist activity at human SST1 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 6 | pEC50 | >1000 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| SST2 receptor/Somatostatin receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1804] [GtoPdb: 356] [UniProtKB: P30874] | ||||||||
| ChEMBL | cAMP Assay : Four days prior to the assay, 5,000 Chinese hamster ovary cells (CHO-K1, ATCC #CCL-61) stably expressing the human SSTR2 are plated in each well of a 96-well tissue culture-treated plate in Ham's F12 growth media (ThermoFisher #10-080-CM) supplemented with 10% donor bovine serum (Gemini Bio-Products #100-506), 100 U/mL penicillin; 100 ug/mL streptomycin; 2 mM L-glutamine (Gemini Bio-Products #400-110) and 0.2 mg/mL hygromycin B (GoldBio #31282-04-9). The cells are cultured at 37° C., 5% CO2 and 95% humidity. On the day of the assay, the media is aspirated and the cells are treated with 50 μL of 1.6 μM NKH477 (Sigma #N3290) plus various dilutions of compounds of the invention in assay buffer [1× Hank's Balanced Salt Solution (ThermoFisher #SH3058802), 0.5 mM HEPES pH 7.4, 0.1% bovine serum albumin, 0.2 mM 3-Isobutyl-1-methylxanthine (IBMX, VWR #200002-790)]. The cells are incubated for 20 minutes at 37° C. (the final concentration of the compounds of the invention are typically 0-10,000 nM). The cells are treated with 50 μL of lysis buffer (HRTF cAMP kit, Cisbio). The lysate is transferred to 384-well plates and cAMP detection and visualization antibodies are added and incubated for 1-24 hours at room temperature. The time-resolved fluorescent signal is read with a Tecan M1000Pro multiplate reader. The intracellular cAMP concentrations are calculated by regression to a standard curve and are plotted vs. the concentration of the compounds of the invention and the EC50 of the compounds are calculated using standard methods. All data manipulations are in GraphPad Prism v6. | B | 8 | pEC50 | <10 | nM | EC50 | US-10351547-B2. Somatostatin modulators and uses thereof (2019) |
| ChEMBL | cAMP Assay: Four days prior to the assay, 5,000 Chinese hamster ovary cells (CHO-K1, ATCC #CCL-61) stably expressing the human SSTR2 are plated in each well of a 96-well tissue culture-treated plate in Ham's F12 growth media (ThermoFisher #10-080-CM) supplemented with 10% donor bovine serum (Gemini Bio-Products #100-506), 100 U/mL penicillin; 100 ug/mL streptomycin; 2 mM L-glutamine (Gemini Bio-Products #400-110) and 0.2 mg/mL hygromycin B (GoldBio #31282-04-9). The cells are cultured at 37° C., 5% CO2 and 95% humidity. On the day of the assay, the media is aspirated and the cells are treated with 50 μL of 1.6 μM NKH477 (Sigma #N3290) plus various dilutions of compounds of the invention in assay buffer [1× Hank's Balanced Salt Solution (ThermoFisher #SH3058802), 0.5 mM HEPES pH 7.4, 0.1% bovine serum albumin, 0.2 mM 3-Isobutyl-1-methylxanthine (IBMX, VWR #200002-790)]. The cells are incubated for 20 minutes at 37° C. (the final concentration of the compounds of the invention are typically 0-10,000 nM). The cells are treated with 50 μL of lysis buffer (HRTF cAMP kit, Cisbio). The lysate is transferred to 384-well plates and cAMP detection and visualization antibodies are added and incubated for 1-24 hours at room temperature. The time-resolved fluorescent signal is read with a Tecan M1000Pro multiplate reader. | B | 8 | pEC50 | <10 | nM | EC50 | US-10464918-B2. Process of making somatostatin modulators (2019) |
| ChEMBL | cAMP Assay: Four days prior to the assay, 5,000 Chinese hamster ovary cells (CHO-K1, ATCC # CCL-61) stably expressing the human SSTR2 are plated in each well of a 96-well tissue culture-treated plate in Ham's F12 growth media (ThermoFisher #10-080-CM) supplemented with 10% donor bovine serum (Gemini Bio-Products #100-506), 100 U/mL penicillin; 100 ug/mL streptomycin; 2 mM L-glutamine (Gemini Bio-Products #400-110) and 0.2 mg/mL hygromycin B (GoldBio #31282-04-9). The cells are cultured at 37° C., 5% CO2 and 95% humidity. On the day of the assay, the media is aspirated and the cells are treated with 50 μL of 1.6 μM NKH477 (Sigma # N3290) plus various dilutions of compounds of the invention in assay buffer [1× Hank's Balanced Salt Solution (ThermoFisher # SH3058802), 0.5 mM HEPES pH 7.4, 0.1% bovine serum albumin, 0.2 mM 3-Isobutyl-1-methylxanthine (IBMX, VWR #200002-790)]. The cells are incubated for 20 minutes at 37° C. (the final concentration of the compounds of the invention are typically 0-10,000 nM). The cells are treated with 50 μL of lysis buffer (HRTF cAMP kit, Cisbio). The lysate is transferred to 384-well plates and cAMP detection and visualization antibodies are added and incubated for 1-24 hours at room temperature. The time-resolved fluorescent signal is read with a Tecan M1000Pro multiplate reader. | B | 8 | pEC50 | <10 | nM | EC50 | US-10597377-B2. Somatostatin modulators and uses thereof (2020) |
| ChEMBL | Agonist activity at human SST2 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 9.6 | pEC50 | 0.25 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| GtoPdb | - | - | 9.6 | pEC50 | 0.25 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| ChEMBL | Agonist activity at human SST2 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 9.6 | pEC50 | 0.25 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| Somatostatin receptor type 2 in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5291563] [UniProtKB: Q49LX6] | ||||||||
| ChEMBL | Agonist activity at dog SST2 receptor | B | 8.18 | pEC50 | 6.6 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| SST2 receptor/Somatostatin receptor type 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2978] [GtoPdb: 356] [UniProtKB: P30680] | ||||||||
| GtoPdb | - | - | 8.92 | pEC50 | 1.2 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| ChEMBL | Agonist activity at rat SST2 receptor | B | 8.92 | pEC50 | 1.2 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| SST3 receptor/Somatostatin receptor type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2028] [GtoPdb: 357] [UniProtKB: P32745] | ||||||||
| ChEMBL | Agonist activity at human SST3 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 6 | pEC50 | >1000 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| SST4 receptor/Somatostatin receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1853] [GtoPdb: 358] [UniProtKB: P31391] | ||||||||
| ChEMBL | Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 6 | pEC50 | 1000 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
| SST5 receptor/Somatostatin receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1792] [GtoPdb: 359] [UniProtKB: P35346] | ||||||||
| ChEMBL | Agonist activity at human SST5 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay | B | 6 | pEC50 | >1000 | nM | EC50 | ACS Med Chem Lett (2023) 14: 66-74 [PMID:36655128] |
ChEMBL data shown on this page come from version 36:
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]
