BDBM50347988 CHEMBL1800152::US9346822, 40
SMILES: COCCN(C)Cc1c(sc2n(Cc3c(F)cccc3F)c(=O)n(-c3ccccn3)c(=O)c12)-c1ccc(NC(=O)NOC)cc1
InChI Key: InChIKey=GAQYSUJKGLPTKB-UHFFFAOYSA-N
Data: 6 IC50
Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kcal/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Gonadotropin releasing hormone 1 (GnRHR1) (Homo sapiens (Human)) | BDBM50347988 (CHEMBL1800152 | US9346822, 40) | PDB KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Patents Similars | US Patent | n/a | n/a | 0.200 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceutical Company Limited US Patent | Assay Description The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at... | US Patent US9346822 (2016) BindingDB Entry DOI: 10.7270/Q2251H2F | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Gonadotropin-releasing hormone receptor (GnRH) (Macaca fascicularis (Crab-eating macaque) (Cynomol...) | BDBM50347988 (CHEMBL1800152 | US9346822, 40) | UniProtKB/TrEMBL GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Patents Similars | US Patent | n/a | n/a | 9 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceutical Company Limited US Patent | Assay Description The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at... | US Patent US9346822 (2016) BindingDB Entry DOI: 10.7270/Q2251H2F | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Gonadotropin releasing hormone 1 (GnRHR1) (Homo sapiens (Human)) | BDBM50347988 (CHEMBL1800152 | US9346822, 40) | PDB KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 0.830 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceutical Company, Ltd. Curated by ChEMBL | Assay Description Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachadonic acid release using [5,6,8,9,11,1... | J Med Chem 54: 4998-5012 (2011) Article DOI: 10.1021/jm200216q BindingDB Entry DOI: 10.7270/Q22N52MK | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Gonadotropin releasing hormone 1 (GnRHR1) (Homo sapiens (Human)) | BDBM50347988 (CHEMBL1800152 | US9346822, 40) | PDB KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 0.300 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceutical Company, Ltd. Curated by ChEMBL | Assay Description Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal... | J Med Chem 54: 4998-5012 (2011) Article DOI: 10.1021/jm200216q BindingDB Entry DOI: 10.7270/Q22N52MK | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Gonadotropin releasing hormone 1 (GnRHR1) (Homo sapiens (Human)) | BDBM50347988 (CHEMBL1800152 | US9346822, 40) | PDB KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 0.200 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceutical Company, Ltd. Curated by ChEMBL | Assay Description Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter | J Med Chem 54: 4998-5012 (2011) Article DOI: 10.1021/jm200216q BindingDB Entry DOI: 10.7270/Q22N52MK | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Gonadotropin releasing hormone 1 (GnRHR1) (Homo sapiens (Human)) | BDBM50347988 (CHEMBL1800152 | US9346822, 40) | PDB KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 13 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceutical Company, Ltd. Curated by ChEMBL | Assay Description Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachadonic acid release using [5,6,8,9,11,1... | J Med Chem 54: 4998-5012 (2011) Article DOI: 10.1021/jm200216q BindingDB Entry DOI: 10.7270/Q22N52MK | |||||||||||
More data for this Ligand-Target Pair |