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Compound Detail

CHEMBL235363

SUBSTANCE P
Phase I
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Phase I
CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCN=C(N)N)C(N)=O

Basic Information

ChEMBL ID CHEMBL235363
Name SUBSTANCE P
Phase Phase I
Structure Type BOTH
InChI Key ADNPLDHMAVUMIW-CUZNLEPHSA-N

Known Names

Neurokinin p Neuropeptide sp-1 Sh-oligopeptide-73 Substance p Substance p (1-11)
16
Targets
53
Activities
3
Assay Types
2
PK Parameters
20
Publications
5
Known Names
2
Indications

Molecular Properties

1347.7
MW (Da)

Drug Information

Molecule Type Protein
Chirality Single Enantiomer

Flags

Natural Product

Extended Properties

Molecular Formula C63H98N18O13S
MW 1347.66

Indications

Diabetes Mellitus, Type 1 Rhinitis, Allergic, Seasonal

Activity Summary

IC50 27 meas. best 10.15
EC50 22 meas. best 10.24
Ki 4 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
EC50 10.24 9.42 0.1 4
Substance-P receptor
CHEMBL3942
IC50 10.15 10.15 0.1 1
Substance-P receptor
CHEMBL249
IC50 9.92 9.161 0.1 10
Substance-P receptor
CHEMBL4027
IC50 9.92 9.4967 0.1 9
Oryctolagus cuniculus
CHEMBL374
EC50 9.21 9.21 0.6 1
Substance-P receptor
CHEMBL3942
EC50 9.0 8.52 1.0 3
CHO
CHEMBL613853
EC50 9.0 8.55 1.0 2
Substance-K receptor
CHEMBL4554
EC50 9.0 7.52 1.0 3
Substance-P receptor
CHEMBL4027
Ki 8.96 8.96 1.1 1
Cavia porcellus
CHEMBL369
IC50 8.8 8.8 1.6 1
Substance-P receptor
CHEMBL249
Ki 8.8 8.8 1.6 1
Cavia porcellus
CHEMBL369
EC50 8.7 8.65 2.0 2
Substance-P receptor
CHEMBL3942
Ki 7.3 7.3 50.5 1
Growth hormone secretagogue receptor type 1
CHEMBL4616
EC50 7.18 7.18 66.0 1
Substance-K receptor
CHEMBL2327
Ki 6.99 6.99 102.0 1
Neuromedin-K receptor
CHEMBL4429
IC50 6.9 6.9 125.0 1
Neuromedin-K receptor
CHEMBL3154
IC50 6.89 6.89 130.0 1
Substance-K receptor
CHEMBL2304405
IC50 6.83 6.83 148.0 1
Rattus norvegicus
CHEMBL376
EC50 6.7 6.7 200.0 1
Substance-K receptor
CHEMBL4554
IC50 6.7 6.7 200.0 1
Substance-K receptor
CHEMBL2327
IC50 6.61 6.61 245.5 1
Unchecked
CHEMBL612545
EC50 6.17 6.17 680.0 1
Neuromedin-K receptor
CHEMBL3799
IC50 6.14 6.14 717.0 1
Neuromedin-K receptor
CHEMBL4429
EC50 6.1 6.1 793.0 1
Mas-related G-protein coupled receptor member X2
CHEMBL5849
EC50 5.97 5.63 1071.5 2
Neuromedin-K receptor
CHEMBL3154
EC50 5.12 5.12 7500.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.3667 hr Mus musculus
T1/2 0.4 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor EC50 = 0.05754 nM 10.24 Antagonist activity at human recombinant NK1 receptor expressed in CHO cells ass... 19473027
Substance-P receptor IC50 = 0.07 nM 10.15 Binding affinity towards Tachykinin receptor 1 binding in guinea pig cerebral co... -
Substance-P receptor IC50 = 0.12 nM 9.92 Inhibition of [125]I-Bolton Hunter Substance P([125]I-BHSP) binding to standard ... 1370695
Substance-P receptor IC50 = 0.12 nM 9.92 Binding affinity for tachykinin receptor 1 from rat forebrain tissue, [125I]-BH-... 1851847
Substance-P receptor IC50 = 0.12 nM 9.92 Inhibition of Tachykinin receptor 1 of rat forebrain tissue 1373191
Substance-P receptor IC50 = 0.12 nM 9.92 Binding affinity against human Tachykinin receptor 1 expressed in astrocytoma UC... 14998319
Substance-P receptor IC50 = 0.12 nM 9.92 Binding affinity towards Tachykinin receptor 1 in rat cerebral cortex membranes ... -
Substance-P receptor IC50 = 0.24 nM 9.62 Compound was evaluated for the antagonistic activity against NK1 receptor -
Substance-P receptor IC50 = 0.26 nM 9.59 Inhibitory activity against binding of [125I]Bolton-Hunter SP to tachykinin NK-1... -
Substance-P receptor IC50 = 0.37 nM 9.43 Tested for inhibition of tachykinin 1 (NK1) receptor in rat brain synaptosomal m... -
Substance-P receptor IC50 = 0.4074 nM 9.39 Displacement of [125I]Lys3-substance P from rat NK1 receptor expressed in CHO ce... 18067242
Substance-P receptor EC50 = 0.6 nM 9.22 SP-induced [Ca2+] mobilization in CHO cells expressing human Tachykinin receptor... 10794691
Substance-P receptor EC50 = 0.6 nM 9.22 Agonist activity at wild type human NK1 receptor expressed in HEK293 cells asses... 22574973
Oryctolagus cuniculus EC50 = 0.61 nM 9.21 Ability to stimulate contraction of the rabbit iris sphincter smooth muscle usin... 7541836
Substance-P receptor IC50 = 0.61 nM 9.21 Antagonist activity for Tachykinin receptor 1 as displacement of [3H]-Substance ... 9871670
Substance-P receptor IC50 = 0.64 nM 9.19 Concentration required to inhibit the specific binding of [125I]BH-SP to Neuroki... 7515443
Substance-P receptor IC50 = 0.9 nM 9.05 Tested for binding affinity against H197A mutant NK1 receptor using [125]SP radi... 11052787
Substance-P receptor EC50 = 1.0 nM 9.0 Agonist activity at bfSPR to produce increase in intracellular [Ca2+] 10794691
Substance-P receptor EC50 = 1.0 nM 9.0 Agonistic activity at tachykinin receptor 1 receptor in guinea pig ileum longitu... 1694545
Substance-K receptor EC50 = 1.0 nM 9.0 Agonist activity at tachykinin receptor 2 in the rat colon muscularis mucosae 1694545

Literature References

PubMed DOI Target Context # Activities
38015459 10.1021/acs.jmedchem.3c01434 Unchecked 25
6177855 10.1021/jm00343a012 Cavia porcellus 9
6177855 10.1021/jm00343a012 Oryctolagus cuniculus 8
6183430 10.1021/jm00353a008 Cavia porcellus 8
2413208 10.1021/jm00148a029 Cavia porcellus 6
950660 10.1021/jm00228a028 No relevant target 6
28288109 10.1038/nchembio.2334 Mas-related G-protein coupled receptor member X2 4
6183430 10.1021/jm00353a008 Oryctolagus cuniculus 4
11052787 10.1021/jm000316h Substance-P receptor 4
34266235 10.1021/acs.jmedchem.0c02051 Unchecked 3
6177855 10.1021/jm00343a012 Rattus norvegicus 3
10794691 10.1021/jm000093v Substance-P receptor 3
2413208 10.1021/jm00148a029 Oryctolagus cuniculus 3
950660 10.1021/jm00228a028 Molecular identity unknown 3
- 10.1016/S0960-894X(01)81197-5 Substance-P receptor 3
950660 10.1021/jm00228a028 Ileum 3
2459385 10.1021/jm00118a007 Mus musculus 3
6177855 10.1021/jm00343a012 Canis familiaris 3
7515443 10.1021/jm00037a009 Cavia porcellus 2
9871763 10.1016/s0960-894x(98)00215-7 Neuromedin-K receptor 2

Data from ChEMBL 36 via Core Engine