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 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]
