ChEMBL ligand: CHEMBL346178 (Osanetant, SB-236984, SR-14280, SR-142801, SR142801)
NK1 receptor/Neurokinin 1 receptor in Human [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103] There should be some charts here, you may need to enable JavaScript!
NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] NK2 receptor/Neurokinin 2 receptor in Rat [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610] There should be some charts here, you may need to enable JavaScript!
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] Neurokinin 3 receptor in Guinea pig [ChEMBL: CHEMBL3799] [UniProtKB: P30098] There should be some charts here, you may need to enable JavaScript!

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	Binding Affinity of [3H]- substance P towards Tachykinin receptor 1-CHO cell membranes (n=3-8)	B	5.89	pKi	1300	nM	Ki	J Med Chem (1996) 39: 2281-2284 [PMID:8691422]
ChEMBL	Binding affinity towards cloned human Tachykinin receptor 1 (hNK-1) expressed in CHO cells using [125I][MePhe7]-NKB	B	5.89	pKi	1300	nM	Ki	J Med Chem (1999) 42: 1053-1065 [PMID:10090788]
ChEMBL	Displacement of [3H]-Substance P from human NK1R after 90 mins by scintillation counting analysis	B	6.4	pKi	398.11	nM	Ki	J Med Chem (2015) 58: 3060-3082 [PMID:25738882]
ChEMBL	Binding affinity to human NK1 receptor by radioligand binding assay	B	6.48	pKi	330	nM	Ki	Bioorg Med Chem Lett (2011) 21: 1991-1996 [PMID:21376585]
ChEMBL	Displacement of [3H]substance P from human recombinant NK1 receptor expressed in HEK293 cells	B	6.68	pKi	209.6	nM	Ki	J Med Chem (2009) 52: 7103-7112 [PMID:19817444]
ChEMBL	Displacement of radioligand [3H]SP from wild type human NK1 receptor expressed in HEK293 cells	B	6.68	pKi	209.6	nM	Ki	J Med Chem (2012) 55: 5061-5076 [PMID:22574973]
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL	Binding affinity to human NK2 receptor by radioligand binding assay	B	7.07	pKi	85	nM	Ki	Bioorg Med Chem Lett (2011) 21: 1991-1996 [PMID:21376585]
ChEMBL	Displacement of [125I]-neurokinin A from human NK2R after 90 mins by scintillation counting analysis	B	7.1	pKi	79.43	nM	Ki	J Med Chem (2015) 58: 3060-3082 [PMID:25738882]
ChEMBL	Binding Affinity of [125I]NKA towards Tachykinin receptor 2-CHO cell membranes (n=3-8)	B	7.39	pKi	40.3	nM	Ki	J Med Chem (1996) 39: 2281-2284 [PMID:8691422]
ChEMBL	Displacement of [3H]SR48968 from human recombinant NK2 receptor expressed in HEK293 cells	B	7.45	pKi	35.5	nM	Ki	J Med Chem (2009) 52: 7103-7112 [PMID:19817444]
ChEMBL	Binding affinity towards cloned human Tachykinin receptor 2 (hNK-2) expressed in CHO cells using [125I][MePhe7]-NKB	B	37	pKi	37	nM	Log Ki	J Med Chem (1999) 42: 1053-1065 [PMID:10090788]
NK2 receptor/Neurokinin 2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610]
ChEMBL	Ability to displace [125I]NKA from Tachykinin receptor 2 in rat deodenum membrane	B	9.29	pKi	0.51	nM	Ki	J Med Chem (1996) 39: 2281-2284 [PMID:8691422]
NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
ChEMBL	Competitive inhibition at human NK3 Y315F6.51 mutant expressed in HEK293 cells assessed as decrease in [MePhe7]NKB-induced [3H]IP accumulation after 20 mins	B	7.53	pKd	29.51	nM	Kd	J Med Chem (2012) 55: 5061-5076 [PMID:22574973]
ChEMBL	Competitive inhibition at wild type human NK3 expressed in HEK293 cells assessed as decrease in [MePhe7]NKB-induced [3H]IP accumulation after 20 mins	B	7.73	pKd	18.62	nM	Kd	J Med Chem (2012) 55: 5061-5076 [PMID:22574973]
ChEMBL	Antagonist activity at wild type human NK3 receptor expressed in HEK293 cells assessed as inhibition of [MePhe7]NKB-induced accumulation of [3H]inositol phosphate	F	7.73	pKd	18.62	nM	Kd	J Med Chem (2009) 52: 7103-7112 [PMID:19817444]
ChEMBL	Competitive inhibition at human NK3 H316W6.52 mutant expressed in HEK293 cells assessed as decrease in [MePhe7]NKB-induced [3H]IP accumulation after 20 mins	B	7.77	pKd	16.98	nM	Kd	J Med Chem (2012) 55: 5061-5076 [PMID:22574973]
ChEMBL	Competitive inhibition at human NK3 Y247F5.38 mutant expressed in HEK293 cells assessed as decrease in [MePhe7]NKB-induced [3H]IP accumulation after 20 mins	B	8.23	pKd	5.89	nM	Kd	J Med Chem (2012) 55: 5061-5076 [PMID:22574973]
ChEMBL	Apparent binding affinity to human NK3 receptor expressed in HEK293 cells	B	9.66	pKd	0.22	nM	Kd	J Med Chem (2009) 52: 7103-7112 [PMID:19817444]
ChEMBL	Equilibrium binding affinity to human NK3 receptor expressed in HEK293 cells	B	9.7	pKd	0.2	nM	Kd	J Med Chem (2009) 52: 7103-7112 [PMID:19817444]
GtoPdb	-	-	9.9	pKd	0.13	nM	Kd
ChEMBL	Displacement of radioligand [3H]osanetant at human NK3 Y315F6.51 mutant expressed in HEK293 cells	B	7.97	pKi	10.8	nM	Ki	J Med Chem (2012) 55: 5061-5076 [PMID:22574973]
ChEMBL	Displacement of radioligand [3H]osanetant at human NK3 H316W mutant expressed in HEK293 cells	B	8.32	pKi	4.8	nM	Ki	J Med Chem (2012) 55: 5061-5076 [PMID:22574973]
ChEMBL	Displacement of radioligand [3H]osanetant at human NK3 Y247W mutant expressed in HEK293 cells	B	8.68	pKi	2.1	nM	Ki	J Med Chem (2012) 55: 5061-5076 [PMID:22574973]
ChEMBL	Binding affinity to human NK3 receptor by radioligand binding assay	B	8.72	pKi	1.9	nM	Ki	Bioorg Med Chem Lett (2011) 21: 1991-1996 [PMID:21376585]
ChEMBL	Displacement of [3H]-SB222200 from recombinant human NK3R expressed in CHO cell membranes after 90 mins by scintillation counting analysis	B	8.8	pKi	1.58	nM	Ki	J Med Chem (2015) 58: 3060-3082 [PMID:25738882]
ChEMBL	Binding affinity towards cloned human Tachykinin receptor 3 (hNK-3) expressed in CHO cells using [125I][MePhe7]-NKB	B	8.92	pKi	1.2	nM	Ki	J Med Chem (1999) 42: 1053-1065 [PMID:10090788]
ChEMBL	Binding Affinity of [125I]-MePhe7-NKB towards Tachykinin receptor 3-CHO cell membranes(n=3-8)	B	8.92	pKi	1.2	nM	Ki	J Med Chem (1996) 39: 2281-2284 [PMID:8691422]
ChEMBL	Displacement of [3H]osanetant from wild type human NK3 receptor expressed in HEK293 cells	B	9.22	pKi	0.6	nM	Ki	J Med Chem (2012) 55: 5061-5076 [PMID:22574973]
ChEMBL	Displacement of radioligand [3H]osanetant at human NK3 Y247F mutant expressed in HEK293 cells	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2012) 55: 5061-5076 [PMID:22574973]
ChEMBL	Displacement of [3H]osanetant from human recombinant NK3 receptor expressed in HEK293 cells	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2009) 52: 7103-7112 [PMID:19817444]
ChEMBL	Displacement of radioligand [3H]osanetant at human NK3 H316F mutant expressed in HEK293 cells	B	9.4	pKi	0.4	nM	Ki	J Med Chem (2012) 55: 5061-5076 [PMID:22574973]
ChEMBL	Binding affinity to NK3 receptor (unknown origin)	B	9.7	pKi	0.2	nM	Ki	Bioorg Med Chem Lett (2014) 24: 510-514 [PMID:24374277]
ChEMBL	Tachykinin receptor 3 binding affinity was determined by incubation with CHO cells expressing human NK3 receptors	B	9.1	pIC50	0.8	nM	IC50	Bioorg Med Chem Lett (1997) 7: 555-560
ChEMBL	Compound was tested for binding affinity against human Tachykinin receptor 3 in CHO cells	B	9.68	pIC50	0.21	nM	IC50	Bioorg Med Chem Lett (1995) 5: 1773-1778
NK3 receptor/Neurokinin 3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177]
ChEMBL	Binding affinity to rat NK3 receptor by radioligand binding assay	B	7.24	pKi	57	nM	Ki	Bioorg Med Chem Lett (2011) 21: 1991-1996 [PMID:21376585]
ChEMBL	Displacement of [3H]-SB222200 from rat NK3R after 90 mins by scintillation counting analysis	B	7.25	pKi	56	nM	Ki	J Med Chem (2015) 58: 3060-3082 [PMID:25738882]
ChEMBL	Displacement of [3H]-SB222200 from rat NK3R after 90 mins by scintillation counting analysis	B	7.3	pKi	50.12	nM	Ki	J Med Chem (2015) 58: 3060-3082 [PMID:25738882]
Neurokinin 3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3799] [UniProtKB: P30098]
ChEMBL	Antagonist activity at wild type guinea pig NK3 receptor A1142.58T mutant expressed in HEK293 cells assessed as inhibition of [MePhe7]NKB-induced accumulation of [3H]inositol phosphate	F	8.5	pKd	3.16	nM	Kd	J Med Chem (2009) 52: 7103-7112 [PMID:19817444]
ChEMBL	Equilibrium binding affinity to guinea pig NK3 receptor expressed in HEK293 cells	B	9.82	pKd	0.15	nM	Kd	J Med Chem (2009) 52: 7103-7112 [PMID:19817444]
ChEMBL	Apparent binding affinity to guinea pig NK3 receptor expressed in HEK293 cells	B	10.1	pKd	0.08	nM	Kd	J Med Chem (2009) 52: 7103-7112 [PMID:19817444]
ChEMBL	Displacement of [3H]osanetant from guinea pig recombinant NK3 receptor A1142.58T expressed in HEK293 cells	B	9.1	pKi	0.8	nM	Ki	J Med Chem (2009) 52: 7103-7112 [PMID:19817444]
ChEMBL	Displacement of [3H]osanetant from guinea pig recombinant NK3 receptor expressed in HEK293 cells	B	9.22	pKi	0.6	nM	Ki	J Med Chem (2009) 52: 7103-7112 [PMID:19817444]
ChEMBL	Ability to displace [3H]senktide succinyl-[Asp9MePhe8]-SP (6-13)} from Tachykinin receptor 3 of guinea pig cerebral cortex membrane	B	6.49	pIC50	320	nM	IC50	J Med Chem (1996) 39: 2281-2284 [PMID:8691422]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]