ChEMBL ligand: CHEMBL441225 (CP-99994)
NK1 receptor/Neurokinin 1 receptor in Human [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103] Neurokinin 1 receptor in Guinea pig [ChEMBL: CHEMBL3942] [UniProtKB: P30547] There should be some charts here, you may need to enable JavaScript!
Neurokinin 2 receptor in Rabbit [ChEMBL: CHEMBL3433] [UniProtKB: P79218] There should be some charts here, you may need to enable JavaScript!
NK3 receptor/Neurokinin 3 receptor in Rat [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177] 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	Antagonistic potency for NK-1 receptor was determined in vitro, using isolated rabbit vena cava.	F	8.9	pKd	1.26	nM	Kd	Bioorg Med Chem Lett (1997) 7: 203-208
ChEMBL	In vitro binding affinity for the Tachykinin receptor 1 in human IM-9 cell using [125I]BH-SP of the compound.	B	5	pKi	>10000	nM	Ki	J Med Chem (1992) 35: 4911-4913 [PMID:1282570]
ChEMBL	In vitro binding affinity towards human NK-1 receptor in IM-9 cells using [3H]SP of substance P antagonist	B	8.82	pKi	1.5	nM	Ki	Bioorg Med Chem Lett (1994) 4: 1865-1868
ChEMBL	Binding affinity measured by displacement of tritiated radiolabeled substance P from cloned human NK1 receptor expressed in CHO cell membranes	B	9.1	pKi	0.79	nM	Ki	Bioorg Med Chem Lett (1995) 5: 2671-2676
ChEMBL	In vitro binding affinity for the Tachykinin receptor 1 in human IM-9 cell using [125I]BH-SP of the compound.	B	9.32	pKi	0.48	nM	Ki	J Med Chem (1992) 35: 4911-4913 [PMID:1282570]
ChEMBL	Compound was evaluated for binding affinity towards neurokinin NK1 receptor.	B	9.4	pKi	0.4	nM	Ki	Bioorg Med Chem Lett (1996) 6: 13-16
ChEMBL	Binding affinity was carried out with NK 1 receptors from U-373MG human astrocytoma cell line	B	9.4	pKi	0.4	nM	Ki	Bioorg Med Chem Lett (1996) 6: 161-164
ChEMBL	Binding affinity to Tachykinin receptor 1 stably expressed in chinese hamster ovary (CHO) cells	B	9.6	pKi	0.25	nM	Ki	J Med Chem (1995) 38: 4985-4992 [PMID:8544174]
ChEMBL	In vitro binding affinity against human NK1 receptor expressed in CHO cells using [3H]-substance P as radioligand	B	9.6	pKi	0.25	nM	Ki	Bioorg Med Chem Lett (1995) 5: 1271-1274
GtoPdb	-	-	9.7	pKi	-	-	-	J Pharmacol Exp Ther (1997) 281: 1303-11 [PMID:9190866]; Eur J Pharmacol (2002) 450: 191-202 [PMID:12206858]
ChEMBL	In vitro inhibitory activity against human NK1 receptor was determined	B	9.77	pKi	0.17	nM	Ki	Bioorg Med Chem Lett (1995) 5: 2671-2676
ChEMBL	In vitro binding affinity for the Tachykinin receptor 1 in human IM-9 cell using [125I]BH-SP of the compound.	B	9.77	pKi	0.17	nM	Ki	J Med Chem (1992) 35: 4911-4913 [PMID:1282570]
ChEMBL	Binding affinity towards human Tachykinin receptor 1 by the displacement of [125I]- Substance P in CHO Cells	B	9	pIC50	1	nM	IC50	Bioorg Med Chem Lett (1994) 4: 1917-1920
ChEMBL	Displacement of [3H]substance P from NK1 human receptor expressed in IM9 cells	B	9.2	pIC50	0.63	nM	IC50	Bioorg Med Chem Lett (2007) 17: 6887-6890 [PMID:17967540]
ChEMBL	Inhibition of substance P binding to Tachykinin receptor 1 in Chinese hamster ovary cells	B	9.22	pIC50	0.6	nM	IC50	J Med Chem (2004) 47: 5381-5392 [PMID:15481976]
ChEMBL	Displacement of [125I]- Substance P from human Neurokinin 1 (hNK1) receptor expressed in CHO cells	B	9.22	pIC50	0.6	nM	IC50	Bioorg Med Chem Lett (1995) 5: 209-212
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	9.3	pIC50	0.5	nM	IC50	J Med Chem (1995) 38: 934-941 [PMID:7535362]
ChEMBL	Binding affinity towards Neurokinin -1(NK-1) receptor of human by using [125I]- Tyr8 substance P as a radioligand in CHO cells	B	9.3	pIC50	0.5	nM	IC50	Bioorg Med Chem Lett (1995) 5: 1345-1350
ChEMBL	Displacement of [125 I]-Tyr8 SP from the cloned human Tachykinin receptor 1 expressed in CHO cells	B	9.3	pIC50	0.5	nM	IC50	J Med Chem (1996) 39: 2907-2914 [PMID:8709125]
ChEMBL	Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells	B	9.3	pIC50	0.5	nM	IC50	J Med Chem (1996) 39: 1760-1762 [PMID:8627597]
ChEMBL	Antagonist activity for Tachykinin receptor 1 as displacement of [3H]-Substance P in human IM-9 cells	F	9.31	pIC50	0.49	nM	IC50	Bioorg Med Chem Lett (1998) 8: 281-284 [PMID:9871670]
ChEMBL	Inhibition of [125I]-BH-Substance P binding to tachykinin receptor 1 in human IM-9 cells	B	9.7	pIC50	0.2	nM	IC50	J Med Chem (1995) 38: 3106-3120 [PMID:7543579]
ChEMBL	Antagonist activity at NK1 receptor	F	9.77	pIC50	0.17	nM	IC50	J Med Chem (2011) 54: 2467-2476 [PMID:21413804]
ChEMBL	Binding affinity was measured against the Tachykinin receptor 1 in human IM-9 cells using [3H]SP as ligand.	B	9.77	pIC50	0.17	nM	IC50	J Med Chem (1998) 41: 3609-3623 [PMID:9733486]
Neurokinin 1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3942] [UniProtKB: P30547]
ChEMBL	Evaluated for the binding affinity towards NK1 receptor in the striatal membranes of guinea pig	B	9.57	pKi	0.27	nM	Ki	J Med Chem (1993) 36: 3197-3201 [PMID:7693945]
ChEMBL	Evaluated for the binding affinity towards NK1 receptor in the striatal membranes of guinea pig	B	9.77	pKi	0.17	nM	Ki	J Med Chem (1993) 36: 3197-3201 [PMID:7693945]
ChEMBL	In vitro binding affinity against Tachykinin receptor 1 in guinea pig ileum using organ bath assay	B	8.54	pIC50	2.9	nM	IC50	Bioorg Med Chem Lett (2001) 11: 705-709 [PMID:11266174]
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	4	pKd	>100000	nM	Kd	Bioorg Med Chem Lett (1997) 7: 203-208
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	4	pKd	>100000	nM	Kd	Bioorg Med Chem Lett (1997) 7: 203-208

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]