PF-04418948 [Ligand Id: 5817] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3286797 (Pf-04418948) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| phosphodiesterase 3A/cGMP-inhibited 3`,5`-cyclic phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432] | ||||||||
| ChEMBL | Selectivity interaction (CEREP ligand profiling ) EUB0000351a PDE3A | B | 5.46 | pIC50 | 3500 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| BLT1 receptor/Leukotriene B4 receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3911] [GtoPdb: 267] [UniProtKB: Q15722] | ||||||||
| ChEMBL | LTB4 (h) (BLT1) CEREP ligand profiling | B | 5.32 | pKi | 4800 | nM | Ki | Data for DCP probe PF-04418948 |
| ChEMBL | Binding assay (LTB4R ) | B | 5.32 | pKi | 4800 | nM | Ki | Data for DCP probe PF-04418948 |
| ChEMBL | LTB4 (h) (BLT1) CEREP ligand profiling | B | 5.01 | pIC50 | 9700 | nM | IC50 | Data for DCP probe PF-04418948 |
| ChEMBL | Selectivity interaction (CEREP ligand profiling ) EUB0000351a LTB4R | B | 5.01 | pIC50 | 9700 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| IP receptor/Prostacyclin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119] | ||||||||
| ChEMBL | Binding assay (PTGIR) | B | 5 | pKi | >10000 | nM | Ki | Data for DCP probe PF-04418948 |
| ChEMBL | Displacement of [3H]-Iloprost from human IP receptor assessed as inhibition constant incubated for 2 hrs by TopCount NXT counter based analysis | B | 5 | pKi | >10000 | nM | Ki | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
| DP1 receptor/Prostaglandin D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258] | ||||||||
| ChEMBL | Binding affinity to human DP1 receptor expressed in CHO cells assessed as inhibition constant | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 11816-11836 [PMID:34352171] |
| ChEMBL | Antagonist activity at human DP1 receptor expressed in CHO cells incubated for 30 mins followed by agonist addition measured after 90 mins | F | 4.48 | pIC50 | >32800 | nM | IC50 | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
| DP2 receptor/Prostaglandin D2 receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4] | ||||||||
| ChEMBL | Antagonist activity at human CRTH2 receptor incubated for 30 mins followed by agonist addition measured after 90 mins | F | 4.49 | pIC50 | 32000 | nM | IC50 | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
| EP1 receptor/Prostaglandin E2 receptor EP1 subtype in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995] | ||||||||
| ChEMBL | Binding affinity to EP1 receptor (unknown origin) assessed as inhibition constant | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 11816-11836 [PMID:34352171] |
| ChEMBL | Antagonist activity at human EP1 receptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins followed by agonist addition measured after 90 mins | F | 5 | pIC50 | >10000 | nM | IC50 | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
| ChEMBL | Agonist activity at human EP1 receptor expressed in CHO cells incubated for 30 mins | F | 5 | pIC50 | >10000 | nM | IC50 | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
| EP2 receptor/Prostaglandin E2 receptor EP2 subtype in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
| ChEMBL | Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2 | B | 8.74 | pKd | 1.8 | nM | Kd | Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Binding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constant | B | 8.12 | pKi | 7.6 | nM | Ki | J Med Chem (2021) 64: 11816-11836 [PMID:34352171] |
| ChEMBL | Inhibition of binding to PTGER2 | B | 8.3 | pIC50 | 5 | nM | IC50 | Data for DCP probe PF-04418948 |
| ChEMBL | Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2 | B | 8.3 | pIC50 | 5 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Agonist activity at human EP2 receptor expressed in CHO cells incubated for 30 mins | F | 4.48 | pEC50 | >33300 | nM | EC50 | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
| EP2 receptor/Prostaglandin E2 receptor EP2 subtype in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2488] [GtoPdb: 341] [UniProtKB: Q62053] | ||||||||
| ChEMBL | Antagonist activity at EP2 receptor in C57BL/6 mouse trachea assessed as inhibition of PGE2-induced relaxation in rings of trachea pretreated for 30 mins in presence of carbachol followed by PGE2 relaxation | F | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2023) 66: 9313-9324 [PMID:37458373] |
| EP3 receptor/Prostaglandin E2 receptor EP3 subtype in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115] | ||||||||
| ChEMBL | Binding affinity to EP3 receptor (unknown origin) assessed as inhibition constant | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 11816-11836 [PMID:34352171] |
| ChEMBL | Antagonist activity at human EP3 receptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins followed by agonist addition measured after 90 mins | F | 5 | pIC50 | >10000 | nM | IC50 | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
| ChEMBL | Agonist activity at human EP3 receptor expressed in CHO cells incubated for 30 mins | F | 5 | pIC50 | >10000 | nM | IC50 | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
| EP4 receptor/Prostaglandin E2 receptor EP4 subtype in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
| ChEMBL | Binding affinity to human EP4 receptor expressed in CHO cells assessed as inhibition constant | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 11816-11836 [PMID:34352171] |
| ChEMBL | Antagonist activity at human EP4 receptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins followed by agonist addition measured after 90 mins | F | 4.48 | pIC50 | >33300 | nM | IC50 | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
| ChEMBL | Agonist activity at human EP4 receptor expressed in CHO cells incubated for 30 mins | F | 4.48 | pEC50 | >33300 | nM | EC50 | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
| FP receptor/Prostaglandin F2-alpha receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088] | ||||||||
| ChEMBL | Binding assay (PTGFR) | B | 5 | pKi | >10000 | nM | Ki | Data for DCP probe PF-04418948 |
| ChEMBL | Displacement of [3H]-Iloprost from human FP receptor assessed as inhibition constant incubated for 2 hrs by TopCount NXT counter based analysis | B | 5 | pKi | >10000 | nM | Ki | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
| Ribosyldihydronicotinamide dehydrogenase [quinone] in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083] | ||||||||
| ChEMBL | ML2 (MT3) CEREP ligand profiling | B | 6.28 | pKi | 520 | nM | Ki | Data for DCP probe PF-04418948 |
| ChEMBL | ML2 (MT3) CEREP ligand profiling | B | 6.28 | pIC50 | 530 | nM | IC50 | Data for DCP probe PF-04418948 |
| ChEMBL | Selectivity interaction (CEREP ligand profiling ) EUB0000351a NQO2 | B | 6.28 | pIC50 | 530 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731] | ||||||||
| ChEMBL | Binding assay (TBXA2R) | B | 5 | pKi | >10000 | nM | Ki | Data for DCP probe PF-04418948 |
| ChEMBL | Displacement of [3H]-Iloprost from human TP receptor assessed as inhibition constant incubated for 2 hrs by TopCount NXT counter based analysis | B | 5 | pKi | >10000 | nM | Ki | Br J Pharmacol (2011) 164: 1847-1856 [PMID:21595651] |
ChEMBL data shown on this page come from version 36:
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]
