leuprolide [Ligand Id: 1175] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1201199 (ABBOTT-43818 FREE BASE, CKD-841, Leuporelin, (-)-leuprolide, Leuprolide, Leuprorelin, Leuprorelina, Leuproreline, Leuprorelin slow release, NSC-377526, TAP-144 FREE BASE) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968] | ||||||||
| GtoPdb | - | - | 9.1 | pKi | 0.79 | nM | Ki | Endocrinology (2007) 148: 857-67 [PMID:17095587] |
| ChEMBL | Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2006) 49: 3809-3825 [PMID:16789738] |
| ChEMBL | The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (1998) 41: 4190-4195 [PMID:9784092] |
| ChEMBL | Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2006) 49: 3809-3825 [PMID:16789738] |
| ChEMBL | Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis | B | 9.54 | pIC50 | 0.29 | nM | IC50 | Medchemcomm (2015) 6: 1656-1665 |
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969] | ||||||||
| ChEMBL | The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (1998) 41: 4190-4195 [PMID:9784092] |
| GtoPdb | - | - | 9.1 | pIC50 | - | - | - | Endocrinology (1994) 135: 315-20 [PMID:8013367] |
| ChEMBL | The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (1998) 41: 4190-4195 [PMID:9784092] |
| ChEMBL | Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2006) 49: 3809-3825 [PMID:16789738] |
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]
