1,10-Phenanthroline [Ligand Id: 12425] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL415879 (1,10-Phenanthroline) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Beta-lactamase VIM-1 in Pseudomonas aeruginosa (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287601] [UniProtKB: Q9XAY4] | ||||||||
| ChEMBL | Inhibition of Pseudomonas aeruginosa VIM-1 beta-lactamase after 10 mins | B | 4.14 | pIC50 | 73000 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 3589-3596 [PMID:18644957] |
| CCR1/C-C chemokine receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246] | ||||||||
| ChEMBL | Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs | B | 4.1 | pIC50 | 79432.82 | nM | IC50 | J Med Chem (2012) 55: 8164-8177 [PMID:22957890] |
| ChEMBL | Displacement of [125I]-CCL3 from human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs | B | 4.13 | pIC50 | 74000 | nM | IC50 | J Med Chem (2012) 55: 8164-8177 [PMID:22957890] |
| ChEMBL | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis | F | 5.2 | pEC50 | 6309.57 | nM | EC50 | J Med Chem (2012) 55: 8164-8177 [PMID:22957890] |
| ChEMBL | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis | F | 5.23 | pEC50 | 5900 | nM | EC50 | J Med Chem (2012) 55: 8164-8177 [PMID:22957890] |
| CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681] | ||||||||
| ChEMBL | Displacement of [125I]-CCL3 from human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs | B | 4.28 | pIC50 | 53000 | nM | IC50 | J Med Chem (2012) 55: 8164-8177 [PMID:22957890] |
| ChEMBL | Displacement of [125I]-CCL3 from human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs | B | 4.3 | pIC50 | 50118.72 | nM | IC50 | J Med Chem (2012) 55: 8164-8177 [PMID:22957890] |
| ChEMBL | Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis | F | 5.3 | pEC50 | 5011.87 | nM | EC50 | J Med Chem (2012) 55: 8164-8177 [PMID:22957890] |
| ChEMBL | Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis | F | 5.31 | pEC50 | 4900 | nM | EC50 | J Med Chem (2012) 55: 8164-8177 [PMID:22957890] |
| CCR8/C-C chemokine receptor type 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4596] [GtoPdb: 65] [UniProtKB: P51685] | ||||||||
| ChEMBL | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis | F | 5.4 | pEC50 | 3981.07 | nM | EC50 | J Med Chem (2012) 55: 8164-8177 [PMID:22957890] |
| ChEMBL | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis | F | 5.41 | pEC50 | 3900 | nM | EC50 | J Med Chem (2012) 55: 8164-8177 [PMID:22957890] |
| Class B carbapenemase VIM-13 in Pseudomonas aeruginosa (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287600] [UniProtKB: Q2HY42] | ||||||||
| ChEMBL | Inhibition of Pseudomonas aeruginosa VIM-13 beta-lactamase after 10 mins | B | 4.16 | pIC50 | 69300 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 3589-3596 [PMID:18644957] |
| MMP13/Matrix metalloproteinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452] | ||||||||
| ChEMBL | In vitro MMP-8 Assay: The synthetic octapeptide substrate, containing the collagenase-susceptible glycine-isoleucine peptide bond, was incubated (37° C.) with commercially-available chromatrographically-purified human neutrophil collagenase (MMP-8) in the presence of 1 mM Ca++ and the tripeptide degradation fragment and undegraded substrate were separated and measured by HPLC (Waters Alliance 2695 System with a reverse phase C-18 column). | B | 5.4 | pIC50 | 4000 | nM | IC50 | US-9187406-B2. Curcumin analogues as zinc chelators and their uses (2015) |
| MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253] | ||||||||
| ChEMBL | In vitro MMP-8 Assay: The synthetic octapeptide substrate, containing the collagenase-susceptible glycine-isoleucine peptide bond, was incubated (37° C.) with commercially-available chromatrographically-purified human neutrophil collagenase (MMP-8) in the presence of 1 mM Ca++ and the tripeptide degradation fragment and undegraded substrate were separated and measured by HPLC (Waters Alliance 2695 System with a reverse phase C-18 column). | B | 4.15 | pIC50 | 70000 | nM | IC50 | US-9187406-B2. Curcumin analogues as zinc chelators and their uses (2015) |
| MMP8/Matrix metalloproteinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894] | ||||||||
| ChEMBL | In vitro MMP-8 Assay: The synthetic octapeptide substrate, containing the collagenase-susceptible glycine-isoleucine peptide bond, was incubated (37° C.) with commercially-available chromatrographically-purified human neutrophil collagenase (MMP-8) in the presence of 1 mM Ca++ and the tripeptide degradation fragment and undegraded substrate were separated and measured by HPLC (Waters Alliance 2695 System with a reverse phase C-18 column). | B | 4.46 | pIC50 | 35000 | nM | IC50 | US-9187406-B2. Curcumin analogues as zinc chelators and their uses (2015) |
| ChEMBL | In vitro MMP-8 Assay: The synthetic octapeptide substrate, containing the collagenase-susceptible glycine-isoleucine peptide bond, was incubated (37° C.) with commercially-available chromatrographically-purified human neutrophil collagenase (MMP-8) in the presence of 1 mM Ca++ and the tripeptide degradation fragment and undegraded substrate were separated and measured by HPLC (Waters Alliance 2695 System with a reverse phase C-18 column). | B | 5 | pIC50 | 10000 | nM | IC50 | US-9187406-B2. Curcumin analogues as zinc chelators and their uses (2015) |
| MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780] | ||||||||
| ChEMBL | In vitro MMP-8 Assay: The synthetic octapeptide substrate, containing the collagenase-susceptible glycine-isoleucine peptide bond, was incubated (37° C.) with commercially-available chromatrographically-purified human neutrophil collagenase (MMP-8) in the presence of 1 mM Ca++ and the tripeptide degradation fragment and undegraded substrate were separated and measured by HPLC (Waters Alliance 2695 System with a reverse phase C-18 column). | B | 5.05 | pIC50 | 9000 | nM | IC50 | US-9187406-B2. Curcumin analogues as zinc chelators and their uses (2015) |
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]
