neurokinin A [Ligand Id: 2089] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL217406
  • 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]
  • Neurokinin 1 receptor in Guinea pig [ChEMBL: CHEMBL3942] [UniProtKB: P30547]
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  • NK3 receptor/Neurokinin 3 receptor in Human [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
  • NK3 receptor in Mouse [GtoPdb: 362] [UniProtKB: P47937]
  • 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 Compound was evaluated for affinity towards human tachykinin NK-1 receptor expressed in CHO cells B 6.2 pKi 630 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 1369-1374 [PMID:9871768]
GtoPdb - - 9.3 pKi - - - Br J Pharmacol (2002) 135: 266-74 [PMID:11786503];
FEBS Lett (1996) 399: 264-266 [PMID:8985159];
FEBS Lett (1992) 296: 241-4 [PMID:1311270];
J Pharmacol Exp Ther (1997) 281: 1303-11 [PMID:9190866]
NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600]
ChEMBL Tested for inhibition of tachykinin 1 (NK1) receptor in rat brain synaptosomal membranes using [125I]BH-SP as radioligand B 7.49 pIC50 32 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 447-450
ChEMBL Binding affinity towards Tachykinin receptor 1 in rat cerebral cortex membranes was determined by using 125 [I]-BHSP as radioligand B 7.51 pIC50 31 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 559-564
Neurokinin 1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3942] [UniProtKB: P30547]
ChEMBL Binding affinity towards Tachykinin receptor 1 binding in guinea pig cerebral cortex membranes was determined using [3H]SP as the radioligand B 8.46 pIC50 3.5 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 559-564
ChEMBL In vitro agonistic activity against tachykinin receptor 1 of guinea pig ileum longitudinal smooth muscle. F 7.86 pEC50 13.7 nM EC50 J. Med. Chem. (1992) 35: 4195-4204 [PMID:1331460]
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL Binding affinity against F293A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 7.4 pKd 40 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against F112A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 7.97 pKd 10.7 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against Q166A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 8.18 pKd 6.6 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against Y206F human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 8.23 pKd 5.9 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against T171A human neurokinin-2 receptor (hNK-2R) using [125I]-NKA as a radioligand B 8.23 pKd 5.9 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against Y269F human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 8.28 pKd 5.3 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against Q109A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 8.49 pKd 3.2 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against Y266F human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 8.55 pKd 2.8 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against S164A human neurokinin-2 receptor (hNK-2R) using [125I]-NKA as a radioligand B 8.6 pKd 2.5 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against wild type human Wild-type tachykinin receptor 2 (hNK-2R) using [125I]NKA as a radioligand B 8.62 pKd 2.4 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against F168A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 8.64 pKd 2.3 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against I202F human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 8.68 pKd 2.1 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against Y289F human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 8.7 pKd 2 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against S170A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 8.72 pKd 1.9 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Binding affinity against Y107A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand B 9.3 pKd 0.5 nM KD/Ki J. Med. Chem. (2002) 45: 3418-3429 [PMID:12139452]
ChEMBL Displacement of [3H]GR100679 from NK2 receptor (unknown origin) expressed in CHO/T cells B 8.92 pKi 1.2 nM Ki J. Med. Chem. (2014) 57: 8187-8203 [PMID:24983484]
GtoPdb - - 9.1 pKi - - - Br J Pharmacol (2002) 135: 266-74 [PMID:11786503];
J Pharmacol Exp Ther (1997) 281: 1303-11 [PMID:9190866];
Biochem Biophys Res Commun (1993) 191: 1172-7 [PMID:7682062];
Biochem Pharmacol (2001) 61: 55-60 [PMID:11137709]
ChEMBL The compound was tested for competition binding with [3H]NKA against the CHO cells from cloned human Tachykinin receptor 2 B 9.15 pKi 0.71 nM Ki J. Med. Chem. (1999) 42: 3004-3007 [PMID:10425111]
ChEMBL Tested for the binding affinity to human NK2 receptor expressed in Sf-9 insect larval cells using 0.1 nM 2-[125 I] iodohistidyl neurokinin A F 8.11 pIC50 7.7 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 715-718
ChEMBL Inhibitory activity against human Tachykinin receptor 2 B 8.77 pIC50 1.7 nM IC50 J. Med. Chem. (1999) 42: 3004-3007 [PMID:10425111]
Neurokinin 2 receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304405] [UniProtKB: P51144]
ChEMBL Competitive inhibition of [125I]NKA binding to hamster urinary bladder Tachykinin receptor 2 B 9 pIC50 1 nM IC50 J. Med. Chem. (1992) 35: 3949-3955 [PMID:1331450]
NK2 receptor/Neurokinin 2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610]
ChEMBL Allosteric modulation of rat NK2 receptor expressed in HEK293 cells assessed as cAMP production by radioimmunoassay B 7.19 pEC50 64.8 nM EC50 J. Med. Chem. (2009) 52: 5999-6011 [PMID:19746979]
ChEMBL In vitro agonistic activity against tachykinin receptor 2 of rat colon muscularis mucosae. F 8.77 pEC50 1.7 nM EC50 J. Med. Chem. (1992) 35: 4195-4204 [PMID:1331460]
ChEMBL Allosteric modulation of rat NK2 receptor expressed in HEK293 cells assessed as increase in intracellular calcium level by spectrofluorimetry F 9.26 pEC50 0.55 nM EC50 J. Med. Chem. (2009) 52: 5999-6011 [PMID:19746979]
Neurokinin 2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2647] [UniProtKB: Q64077]
ChEMBL Evaluated for the binding affinity against NK2 receptor B 5.43 pKi 3700 nM Ki J. Med. Chem. (1993) 36: 3197-3201 [PMID:7693945]
NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
GtoPdb - - 6.3 pKi - - - J Pharmacol Exp Ther (1997) 281: 1303-11 [PMID:9190866];
Eur J Pharmacol (2001) 413: 143-50 [PMID:11226387]
ChEMBL Compound was evaluated for its ability to displace [3H]NKB binding in hNK3 receptors expressed in CHO cells B 7.35 pIC50 45 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 1343-1348 [PMID:9871763]
ChEMBL Compound was evaluated for concentration-dependent and oscillatory increase in [Ca2+], caused by activation of hNK3 receptors in CHO cells F 7.28 pEC50 53 nM EC50 Bioorg. Med. Chem. Lett. (1998) 8: 1343-1348 [PMID:9871763]
GtoPdb - - 7.4 pEC50 40 nM EC50 FEBS Lett (1992) 299: 90-5 [PMID:1312036]
NK3 receptor in Mouse [GtoPdb: 362] [UniProtKB: P47937]
GtoPdb - - 6.1 pKi - - - Eur J Pharmacol (2001) 413: 143-50 [PMID:11226387]
NK3 receptor/Neurokinin 3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177]
ChEMBL In vitro agonistic activity against tachykinin receptor 3 of everted rat protal vein. F 6.25 pEC50 563 nM EC50 J. Med. Chem. (1992) 35: 4195-4204 [PMID:1331460]

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]