L-732,138 [Ligand Id: 9461] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL22870 (L-732138)
  • NK1 receptor/Neurokinin 1 receptor in Human [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
  • NK1 receptor/Neurokinin 1 receptor in Rat [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600]
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  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
  • Neurokinin 2 receptor in Rabbit [ChEMBL: CHEMBL3433] [UniProtKB: P79218]
  • NK2 receptor/Neurokinin 2 receptor in Rat [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610]
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  • NK3 receptor/Neurokinin 3 receptor in Human [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
  • NK3 receptor/Neurokinin 3 receptor in Rat [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
ChEMBL Antagonistic potency for NK-1 receptor was determined in vitro, using isolated rabbit vena cava. F 8.4 pKd 3.98 nM Kd Bioorg. Med. Chem. Lett. (1997) 7: 203-208
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells B 6.87 pKi 134 nM Ki J. Med. Chem. (2007) 50: 2779-2786 [PMID:17516639]
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells B 9.14 pKi 0.73 nM Ki J. Med. Chem. (2008) 51: 1369-1376 [PMID:18266313]
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membrane by liquid scintillation counting B 9.14 pKi 0.73 nM Ki J. Med. Chem. (2008) 51: 6334-6347 [PMID:18821747]
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membrane B 9.14 pKi 0.73 nM Ki J. Med. Chem. (2009) 52: 5164-5175 [PMID:20560643]
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membranes B 9.14 pKi 0.73 nM Ki Bioorg. Med. Chem. (2009) 17: 7337-7343 [PMID:19762245]
ChEMBL Displacement of [3H]substance P frome human NK1 receptor B 9.14 pKi 0.73 nM Ki J. Med. Chem. (2010) 53: 5491-5501 [PMID:20617791]
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells B 9.14 pKi 0.73 nM Ki J. Med. Chem. (2011) 54: 2029-2038 [PMID:21366266]
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells B 6.4 pIC50 398.11 nM IC50 J. Med. Chem. (2007) 50: 2779-2786 [PMID:17516639]
ChEMBL Binding affinity against Gln165Ala mutant type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P. B 8.09 pIC50 8.1 nM IC50 J. Med. Chem. (1995) 38: 934-941 [PMID:7535362]
ChEMBL Binding affinity against wild type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P. B 8.48 pIC50 3.3 nM IC50 J. Med. Chem. (1995) 38: 934-941 [PMID:7535362]
ChEMBL Binding affinity was measured against the Tachykinin receptor 1 in CHO-expressed hNK1 using [125I]SP. B 8.49 pIC50 3.24 nM IC50 J. Med. Chem. (1998) 41: 3609-3623 [PMID:9733486]
ChEMBL Binding affinity at human Tachykinin receptor 1 expressed in CHO cells by [125 I]Trp8-substance P displacement. B 8.6 pIC50 2.5 nM IC50 J. Med. Chem. (1995) 38: 923-933 [PMID:7699709]
GtoPdb Antagonism of [125]-substance P binding, to NK1 receptors expressed in CHO cells. - 8.64 pIC50 2.3 nM IC50 J Biol Chem (1994) 269: 6587-91 [PMID:7509807]
ChEMBL Binding affinity against human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P. B 8.8 pIC50 1.6 nM IC50 J. Med. Chem. (1995) 38: 934-941 [PMID:7535362]
ChEMBL Tested against cloned human NK1 receptor by displacement of 125 I -labeled substance P expressed in CHO cells B 8.8 pIC50 1.6 nM IC50 J. Med. Chem. (1993) 36: 2044-2045 [PMID:8393115]
ChEMBL Inhibition of cloned human NK1 (Neurokinin 1) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined B 8.8 pIC50 1.6 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 2259-2262 [PMID:9873524]
ChEMBL Binding affinity towards cloned neurokinin 1 receptor, based on the displacement of [125I]-labeled substance P B 8.8 pIC50 1.6 nM IC50 J. Med. Chem. (1994) 37: 1269-1274 [PMID:7513763]
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membrane by liquid scintillation counting B 8.8 pIC50 1.58 nM IC50 J. Med. Chem. (2008) 51: 6334-6347 [PMID:18821747]
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells B 8.8 pIC50 -8.8 - logIC50 J. Med. Chem. (2008) 51: 1369-1376 [PMID:18266313]
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membrane B 8.83 pIC50 1.48 nM IC50 J. Med. Chem. (2009) 52: 5164-5175 [PMID:20560643]
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membranes B 8.83 pIC50 1.48 nM IC50 Bioorg. Med. Chem. (2009) 17: 7337-7343 [PMID:19762245]
ChEMBL Displacement of [3H]substance P frome human NK1 receptor B 8.83 pIC50 1.48 nM IC50 J. Med. Chem. (2010) 53: 5491-5501 [PMID:20617791]
ChEMBL Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells B 8.83 pIC50 1.48 nM IC50 J. Med. Chem. (2011) 54: 2029-2038 [PMID:21366266]
NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600]
ChEMBL Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membranes B 6.87 pKi 134 nM Ki Bioorg. Med. Chem. (2009) 17: 7337-7343 [PMID:19762245]
ChEMBL Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cells B 6.89 pKi 130 nM Ki J. Med. Chem. (2008) 51: 1369-1376 [PMID:18266313]
ChEMBL Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membrane by liquid scintillation counting B 6.89 pKi 130 nM Ki J. Med. Chem. (2008) 51: 6334-6347 [PMID:18821747]
ChEMBL Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membrane B 6.89 pKi 130 nM Ki J. Med. Chem. (2009) 52: 5164-5175 [PMID:20560643]
ChEMBL Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cells B 6.89 pKi 130 nM Ki J. Med. Chem. (2011) 54: 2029-2038 [PMID:21366266]
GtoPdb - - 6.34 pIC50 ~460 nM IC50 J Biol Chem (1994) 269: 6587-91 [PMID:7509807]
ChEMBL Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membrane by liquid scintillation counting B 6.4 pIC50 398.11 nM IC50 J. Med. Chem. (2008) 51: 6334-6347 [PMID:18821747]
ChEMBL Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membrane B 6.4 pIC50 398.11 nM IC50 J. Med. Chem. (2009) 52: 5164-5175 [PMID:20560643]
ChEMBL Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membranes B 6.4 pIC50 398.11 nM IC50 Bioorg. Med. Chem. (2009) 17: 7337-7343 [PMID:19762245]
ChEMBL Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cells B 6.4 pIC50 398.11 nM IC50 J. Med. Chem. (2011) 54: 2029-2038 [PMID:21366266]
ChEMBL Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cells B 6.4 pIC50 -6.4 - logIC50 J. Med. Chem. (2008) 51: 1369-1376 [PMID:18266313]
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL Inhibition of cloned human NK2 (Neurokinin 2) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined B 5.3 pIC50 >5000 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 2259-2262 [PMID:9873524]
ChEMBL Binding affinity to the NK2 receptor assayed by displacement of [125I]-Neurokinin A B 5.3 pIC50 >5000 nM IC50 J. Med. Chem. (1994) 37: 1269-1274 [PMID:7513763]
Neurokinin 2 receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3433] [UniProtKB: P79218]
ChEMBL Antagonistic potency for NK-2 receptor was determined in vitro, using isolated rabbit pulmonary artery. F 5.2 pKd 6309.57 nM Kd Bioorg. Med. Chem. Lett. (1997) 7: 203-208
NK2 receptor/Neurokinin 2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610]
ChEMBL Displacement of [3H]substance P frome rat NK2 receptor B 6.87 pKi 134 nM Ki J. Med. Chem. (2010) 53: 5491-5501 [PMID:20617791]
ChEMBL Displacement of [3H]substance P frome rat NK2 receptor B 6.4 pIC50 398.11 nM IC50 J. Med. Chem. (2010) 53: 5491-5501 [PMID:20617791]
NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
ChEMBL Affinity to NK3 receptors assayed by displacement of [125I]-Bolton-Hunter labeled eledoisin radioligand B 5.3 pIC50 >5000 nM IC50 J. Med. Chem. (1994) 37: 1269-1274 [PMID:7513763]
NK3 receptor/Neurokinin 3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177]
ChEMBL Antagonistic potency for NK-3 receptor was determined in vitro, using isolated rat portal vein. F 5.2 pKd 6309.57 nM Kd Bioorg. Med. Chem. Lett. (1997) 7: 203-208

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]