CCG-50014 [Ligand Id: 7784] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1917204 (CCG-50014) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| regulator of G-protein signaling 16/Regulator of G-protein signaling 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3707469] [GtoPdb: 2806] [UniProtKB: O15492] | ||||||||
| ChEMBL | Inhibitory Assay: FCPIA Characterization of RGS Inhibitory Activity: CCG-50014 (FIG. 1) was originally identified as a potential inhibitor of RGS8 and RGS16 in a polyplex high throughput screen to identify inhibitors of the RGS-Gα interaction [4]. This activity was confirmed by analyzing the effect of CCG-50014 on several different RGS proteins with freshly reordered compound using multiplexed FCPIA. CCG-50014 fully inhibited several different RGS proteins including RGS4, 8, 16, and 19, but did not have activity on RGS7 or a mutated form of RGS4 that lacks cysteine residues. | B | 5.46 | pIC50 | 3500 | nM | IC50 | US-8865750-B2. Small molecule inhibitors of RGS proteins (2014) |
| regulator of G-protein signaling 19/Regulator of G-protein signaling 19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3707468] [GtoPdb: 2802] [UniProtKB: P49795] | ||||||||
| GtoPdb | - | - | 5.96 | pIC50 | 1100 | nM | IC50 | J Am Chem Soc (2018) 140: 3454-3460 [PMID:29460621] |
| ChEMBL | Inhibitory Assay: FCPIA Characterization of RGS Inhibitory Activity: CCG-50014 (FIG. 1) was originally identified as a potential inhibitor of RGS8 and RGS16 in a polyplex high throughput screen to identify inhibitors of the RGS-Gα interaction [4]. This activity was confirmed by analyzing the effect of CCG-50014 on several different RGS proteins with freshly reordered compound using multiplexed FCPIA. CCG-50014 fully inhibited several different RGS proteins including RGS4, 8, 16, and 19, but did not have activity on RGS7 or a mutated form of RGS4 that lacks cysteine residues. | B | 6.92 | pIC50 | 120 | nM | IC50 | US-8865750-B2. Small molecule inhibitors of RGS proteins (2014) |
| regulator of G-protein signaling 4/Regulator of G-protein signaling 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795091] [GtoPdb: 2811] [UniProtKB: P49798] | ||||||||
| GtoPdb | Inhibition of Gαo binding. | - | 7.52 | pIC50 | 30.1 | nM | IC50 |
Biochemistry (2011) 50: 3181-92 [PMID:21329361]; ACS Med Chem Lett (2012) 3: 146-150 [PMID:22368763] |
| ChEMBL | Inhibition of RGS4 interaction with Galpha0 protein by flow cytometry protein interaction assay | B | 7.52 | pIC50 | 30.1 | nM | IC50 | ACS Med Chem Lett (2012) 3: 146-150 [PMID:22368763] |
| ChEMBL | Inhibitory Assay: FCPIA Characterization of RGS Inhibitory Activity: CCG-50014 (FIG. 1) was originally identified as a potential inhibitor of RGS8 and RGS16 in a polyplex high throughput screen to identify inhibitors of the RGS-Gα interaction [4]. This activity was confirmed by analyzing the effect of CCG-50014 on several different RGS proteins with freshly reordered compound using multiplexed FCPIA. CCG-50014 fully inhibited several different RGS proteins including RGS4, 8, 16, and 19, but did not have activity on RGS7 or a mutated form of RGS4 that lacks cysteine residues. | B | 7.52 | pIC50 | 30 | nM | IC50 | US-8865750-B2. Small molecule inhibitors of RGS proteins (2014) |
| regulator of G-protein signaling 8/Regulator of G-protein signaling 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034803] [GtoPdb: 2813] [UniProtKB: P57771] | ||||||||
| ChEMBL | Inhibition of RGS8 interaction with Galpha0 protein by flow cytometry protein interaction assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 146-150 [PMID:22368763] |
| ChEMBL | Inhibitory Assay: FCPIA Characterization of RGS Inhibitory Activity: CCG-50014 (FIG. 1) was originally identified as a potential inhibitor of RGS8 and RGS16 in a polyplex high throughput screen to identify inhibitors of the RGS-Gα interaction [4]. This activity was confirmed by analyzing the effect of CCG-50014 on several different RGS proteins with freshly reordered compound using multiplexed FCPIA. CCG-50014 fully inhibited several different RGS proteins including RGS4, 8, 16, and 19, but did not have activity on RGS7 or a mutated form of RGS4 that lacks cysteine residues. | B | 4.96 | pIC50 | 11000 | nM | IC50 | US-8865750-B2. Small molecule inhibitors of RGS proteins (2014) |
| GtoPdb | Inhibition of Gαo binding | - | 4.96 | pIC50 | 11000 | nM | IC50 |
Biochemistry (2011) 50: 3181-92 [PMID:21329361]; ACS Med Chem Lett (2012) 3: 146-150 [PMID:22368763]; Mol Pharmacol (2019) 96: 683-691 [PMID:31543506]; J Am Chem Soc (2018) 140: 3454-3460 [PMID:29460621] |
| Replicase polyprotein 1ab in Middle East respiratory syndrome-related coronavirus (isolate UnitedKingdom/H123990006/2012) (Betacoronavirus England 1) (Humancoronavirus EMC) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295557] [UniProtKB: K9N7C7] | ||||||||
| ChEMBL | MERS_3CL Pro protease inhibition IC50 by FRET kind of response from peptide substrate | F | 5 | pIC50 | >10000 | nM | IC50 | Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen |
| CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1] | ||||||||
| ChEMBL | SARS-CoV-2 3CL-Pro protease inhibition IC50 determined by FRET kind of response from peptide substrate | F | 6.64 | pIC50 | 230 | nM | IC50 | Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen |
| ChEMBL | SARS-CoV-2 3CL-Pro protease inhibition IC50 determined by FRET kind of response from peptide substrate | F | 6.82 | pIC50 | 150 | nM | IC50 | Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen |
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]
