BDBM50122654 1-(4-(1-(2,6-difluorobenzyl)-5-((benzyl(methyl)amino)methyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea::1-{4-[5-[(Benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydro-thieno[2,3-d]pyrimidin-6-yl]-phenyl}-3-methoxy-urea::CHEMBL22055::N-[4-(3-phenyl-5-(N-benzyl-N-methyl-aminomethyl)-1-(2,6-difluorobenzyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl]-N'-methoxyurea::TAK-013::sufugolix
SMILES CONC(=O)Nc1ccc(cc1)-c1sc2n(Cc3c(F)cccc3F)c(=O)n(-c3ccccc3)c(=O)c2c1CN(C)Cc1ccccc1
InChI Key InChIKey=UCQSBGOFELXYIN-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 99 hits for monomerid = 50122654
Affinity DataIC50: 2.30nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FMore data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QMore data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KMore data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LMore data for this Ligand-Target Pair
Affinity DataIC50: 23.4nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306AMore data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27AMore data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EMore data for this Ligand-Target Pair
Affinity DataIC50: 0.800nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KMore data for this Ligand-Target Pair
Affinity DataIC50: 0.600nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FMore data for this Ligand-Target Pair
Affinity DataIC50: 0.800nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LMore data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117AMore data for this Ligand-Target Pair
Affinity DataIC50: 1.90nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EMore data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315AMore data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DMore data for this Ligand-Target Pair
Affinity DataIC50: 0.600nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293AMore data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305AMore data for this Ligand-Target Pair
Affinity DataIC50: 470nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121AMore data for this Ligand-Target Pair
Affinity DataIC50: 0.600nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51AMore data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189AMore data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295AMore data for this Ligand-Target Pair
Affinity DataIC50: 1.10nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QMore data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KMore data for this Ligand-Target Pair
Affinity DataIC50: 0.100nMAssay Description:Binding affinity at human GnRH receptorMore data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+3nMAssay Description:Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in rat anterior pituitariesMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0600nMAssay Description:Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanMore data for this Ligand-Target Pair
Affinity DataIC50: 0.600nMAssay Description:Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO)...More data for this Ligand-Target Pair
Affinity DataIC50: 0.100nMAssay Description:Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyMore data for this Ligand-Target Pair
Affinity DataIC50: 0.100nMAssay Description:Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0600nMAssay Description:Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,1...More data for this Ligand-Target Pair
Affinity DataIC50: 1.60nMAssay 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...More data for this Ligand-Target Pair
Affinity DataIC50: 270nMAssay Description:Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,1...More data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumMore data for this Ligand-Target Pair
Affinity DataIC50: 1.90nMAssay Description:Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,1...More data for this Ligand-Target Pair
TargetGonadotropin-releasing hormone receptor(Rhesus macaque)
Neurocrine Biosciences
Curated by ChEMBL
Neurocrine Biosciences
Curated by ChEMBL
Affinity DataIC50: 0.600nMAssay Description:Binding affinity at monkey GnRH receptorMore data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QMore data for this Ligand-Target Pair
Affinity DataIC50: 24nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 110nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 24nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 100nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 190nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 0.800nMAssay Description:Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 12nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 120nMAssay Description:Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsMore data for this Ligand-Target Pair