pamiparib [Ligand Id: 12345] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4112930 (Bgb-290, BGB-290, Pamiparib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| poly(ADP-ribose) polymerase 1/Poly [ADP-ribose] polymerase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3105] [GtoPdb: 2771] [UniProtKB: P09874] | ||||||||
| ChEMBL | Inhibition of human PARP-1 catalytic domain (662 to 1011 residues) expressed in Escherichia coli BL21(DE3) cells pre-incubated for 30 mins before addition of activated DNA and NAD by fluorescence based assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| GtoPdb | - | - | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| ChEMBL | PARP-1 Enzymatic Assay: PARP-1 enzymatic assay was conducted using a method modified from HT F Homogeneous PARP Inhibition Assay Kit (Trevigen). 8.8 nM PARP-1 was pre-incubated with different concentrations of compounds in a buffer containing 100 mM Tris-HCl pH 8.0, 100 mM NaCl, 20 mM MgCl2, and 1% DMSO for 30 min at RT. The auto-PARylation reaction was initiated by addition of 500 nM NAD and 20 ng/ul activated DNA (Sigma) and incubated at RT for 40 min. The remaining NAD was detected by incubation with cycling assay solution containing 1% ethanol, 0.30 U/ml alcohol dehydrogenase, 25 uM resazurin, and 0.25 U/ml diaphorase for 50 min at RT. The concentration of NAD is proportional to the fluorescence signal at Ex 540 nm/Em 590 nm. | B | 9.05 | pIC50 | 0.9 | nM | IC50 | US-9260440-B2. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors (2016) |
| ChEMBL | Inhibition of human PARP-1 catalytic domain (662 to 1011 residues) expressed in Escherichia coli BL21(DE3) cells incubated for 0.5 hrs by fluorescence polarization assay based DNA trapping activity assay | B | 7.89 | pEC50 | 13 | nM | EC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| ChEMBL | Inhibition of PARP-1 in human HeLa cells incubated for 18 hrs in presence of H2O2 | B | 9.7 | pEC50 | 0.2 | nM | EC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| poly(ADP-ribose) polymerase family member 10/Poly [ADP-ribose] polymerase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2429708] [GtoPdb: 3267] [UniProtKB: Q53GL7] | ||||||||
| ChEMBL | Inhibition of PARP-10 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| poly(ADP-ribose) polymerase family member 11/Poly [ADP-ribose] polymerase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2380189] [GtoPdb: 3268] [UniProtKB: Q9NR21] | ||||||||
| ChEMBL | Inhibition of PARP-11 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| Poly [ADP-ribose] polymerase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2429709] [UniProtKB: Q9H0J9] | ||||||||
| ChEMBL | Inhibition of PARP-12 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay | B | 5.62 | pIC50 | 2400 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| poly(ADP-ribose) polymerase 2/Poly [ADP-ribose] polymerase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5366] [GtoPdb: 2772] [UniProtKB: Q9UGN5] | ||||||||
| ChEMBL | Inhibition of PARP-2 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay | B | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| GtoPdb | - | - | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| ChEMBL | PARP-2 and PARP-3 Enzymatic Assay: PARP-2 and PARP-3 enzymatic assays were conducted using commercial PARP-2/PARP-3 Chemiluminescent Assay Kit (BPS Biosciences) and the protocols with the kits. Briefly, histones were coated in a high binding plate first, and incubated with PARP-2 or PARP-3, and increasing concentrations of compounds for 0.5 h. Then, biotinylated NAD and activated DNA were added to the wells. The biotinylated PARylation product was measured by adding streptavidin-HRP and HRP substrates which produce chemiluminescence. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9260440-B2. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors (2016) |
| poly (ADP-ribose) polymerase 3/Poly [ADP-ribose] polymerase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5083] [GtoPdb: 2864] [UniProtKB: Q9Y6F1] | ||||||||
| ChEMBL | PARP-2 and PARP-3 Enzymatic Assay: PARP-2 and PARP-3 enzymatic assays were conducted using commercial PARP-2/PARP-3 Chemiluminescent Assay Kit (BPS Biosciences) and the protocols with the kits. Briefly, histones were coated in a high binding plate first, and incubated with PARP-2 or PARP-3, and increasing concentrations of compounds for 0.5 h. Then, biotinylated NAD and activated DNA were added to the wells. The biotinylated PARylation product was measured by adding streptavidin-HRP and HRP substrates which produce chemiluminescence. | B | 6.73 | pIC50 | 185 | nM | IC50 | US-9260440-B2. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors (2016) |
| ChEMBL | Inhibition of PARP-3 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay | B | 7.17 | pIC50 | 68 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| Poly [ADP-ribose] polymerase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2380187] [UniProtKB: Q2NL67] | ||||||||
| ChEMBL | Inhibition of PARP-6 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| Poly [ADP-ribose] polymerase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3091262] [UniProtKB: Q8N3A8] | ||||||||
| ChEMBL | Inhibition of PARP-8 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay | B | 5.08 | pIC50 | 8400 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| Organic anion transporter 1/Solute carrier family 22 member 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8] | ||||||||
| ChEMBL | Inhibition of OAT1 (unknown origin) | B | 4.32 | pIC50 | 47800 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| Organic anion transporter 3/Solute carrier family 22 member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7] | ||||||||
| ChEMBL | Inhibition of OAT3 (unknown origin) | B | 4.62 | pIC50 | 23900 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6] | ||||||||
| ChEMBL | Inhibition of OATP1B1 (unknown origin) | B | 4.71 | pIC50 | 19400 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| OATP1B3/Solute carrier organic anion transporter family member 1B3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743121] [GtoPdb: 1221] [UniProtKB: Q9NPD5] | ||||||||
| ChEMBL | Inhibition of OATP1B3 (unknown origin) | B | 4.71 | pIC50 | 19400 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| tankyrase/Tankyrase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6164] [GtoPdb: 3108] [UniProtKB: O95271] | ||||||||
| ChEMBL | Inhibition of TNKS-1 (unknown origin) pre-incubated for 30 mins before addition of NAD by chemiluminescent assay | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| tankyrase 2/Tankyrase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6154] [GtoPdb: 3109] [UniProtKB: Q9H2K2] | ||||||||
| ChEMBL | Tankyrase-2 Enzymatic Assay: Tankyrase-2 enzymatic assay was conducted using commercial Tankyrase-2 Chemiluminescent Assay Kit (BPS Biosciences) and the protocol with the kit. GST-fused tankyrase-2 (recombinant protein expressed and purified from Bacluovirus) were coated on a GSH-precoated plate first, and incubated with increasing concentrations of compounds for 0.5 h. Then, biotinylated NAD was added to the wells. The biotinylated auto-PARylation product was measured by adding streptavidin-HRP and HRP substrates which produce chemiluminescence. | B | 6.12 | pIC50 | 766 | nM | IC50 | US-9260440-B2. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors (2016) |
| ChEMBL | Inhibition of TNKS-2 (unknown origin) pre-incubated for 30 mins before addition of NAD by chemiluminescent assay | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| TCDD inducible poly(ADP-ribose) polymerase/TCDD-inducible poly [ADP-ribose] polymerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2380188] [GtoPdb: 3266] [UniProtKB: Q7Z3E1] | ||||||||
| ChEMBL | Inhibition of PARP-7 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
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]
