PF-04418948 [Ligand Id: 5817] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3286797 (Pf-04418948)
  • BLT1 receptor/Leukotriene B4 receptor 1 in Human [ChEMBL: CHEMBL3911] [GtoPdb: 267] [UniProtKB: Q15722]
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  • phosphodiesterase 3A/Phosphodiesterase 3A in Human [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
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  • DP1 receptor/Prostanoid DP receptor in Human [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
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  • EP1 receptor/Prostanoid EP1 receptor in Human [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
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  • EP2 receptor/Prostanoid EP2 receptor in Human [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
  • EP2 receptor/Prostanoid EP2 receptor in Mouse [ChEMBL: CHEMBL2488] [GtoPdb: 341] [UniProtKB: Q62053]
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  • EP3 receptor/Prostanoid EP3 receptor in Human [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
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  • EP4 receptor/Prostanoid EP4 receptor in Human [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
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  • FP receptor/Prostanoid FP receptor in Human [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088]
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  • IP receptor/Prostanoid IP receptor in Human [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
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  • TP receptor/Thromboxane A2 receptor in Human [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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
phosphodiesterase 3A/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
DP1 receptor/Prostanoid DP 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]
EP1 receptor/Prostanoid EP1 receptor 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]
EP2 receptor/Prostanoid EP2 receptor 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
EP2 receptor/Prostanoid EP2 receptor 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/Prostanoid EP3 receptor 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]
EP4 receptor/Prostanoid EP4 receptor 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]
FP receptor/Prostanoid FP 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
IP receptor/Prostanoid IP 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
Quinone reductase 2 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 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]