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] 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] Neurokinin 2 receptor in Rabbit [ChEMBL: CHEMBL3433] [UniProtKB: P79218] 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] 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	8.4	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	Inhibition of [3H]SP binding to human neurokinin receptor 1 expressed in CHO cells	B	8.8	pIC50	1.6	nM	IC50	J Med Chem (2016) 59: 10865-10890 [PMID:27690430]
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	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	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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]