pamiparib [Ligand Id: 12345] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL4112930 (Bgb-290, BGB-290, Pamiparib) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 PARP1 (unknown origin) | B | 8.19 | pIC50 | 6.5 | nM | IC50 | J Med Chem (2023) 66: 14095-14115 [PMID:37843892] |
| 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 PARP-1 (unknown origin) | B | 9.08 | pIC50 | 0.83 | nM | IC50 | J Med Chem (2016) 59: 9575-9598 [PMID:27416328] |
| 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) |
| ChEMBL | Inhibition of PARP2 (unknown origin) | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2023) 66: 14095-14115 [PMID:37843892] |
| ChEMBL | Inhibition of PARP-2 (unknown origin) | B | 9.96 | pIC50 | 0.11 | nM | IC50 | J Med Chem (2016) 59: 9575-9598 [PMID:27416328] |
| 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 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]
