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Assay Detail

CHEMBL809494

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of [125I]-BH-Substance P binding to tachykinin receptor 1 in human IM-9 cells
ChEMBL ↗
46
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type IM-9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Substance-P receptor (CHEMBL249) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel, potent, and orally active substance P antagonists: synthesis and antagonist activity of N-benzylcarboxamide derivatives of pyrido[3,4-b]pyridine.
Natsugari H, Ikeura Y, Kiyota Y, Ishichi Y, Ishimaru T, Saga O, Shirafuji H, Tanaka T, Kamo I, Doi T.
J Med Chem (1995) 38 : 3106 -3120
PubMed 7543579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 7.67 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441225 CP-99994 — 1 9.70
CHEMBL107482 — — 1 9.68
CHEMBL415705 — — 1 9.60
CHEMBL107172 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (3,5-BIS-TRIFLUOROMETHYL-BENZYL)-METHYL-AMIDE (STRUCTURAL MIX) — 2 9.47
CHEMBL106864 — — 1 9.40
CHEMBL104301 — — 1 8.96
CHEMBL317896 — — 1 8.92
CHEMBL106087 — — 1 8.89
CHEMBL110679 — — 1 8.60
CHEMBL107848 — — 1 8.60
CHEMBL105629 — — 1 8.47
CHEMBL319874 — — 1 8.47
CHEMBL322718 — — 1 8.38
CHEMBL106904 — — 1 8.36
CHEMBL317870 — — 1 8.29
CHEMBL104370 — — 1 8.08
CHEMBL104225 — — 1 7.89
CHEMBL104165 — — 1 7.80
CHEMBL104737 — — 1 7.80
CHEMBL106326 — — 1 7.72
CHEMBL104060 — — 1 7.72
CHEMBL108126 — — 1 7.64
CHEMBL107959 — — 1 7.64
CHEMBL106609 — — 1 7.55
CHEMBL320231 — — 1 7.52
CHEMBL104513 — — 1 7.50
CHEMBL322714 — — 1 7.50
CHEMBL107145 — — 1 7.47
CHEMBL107689 — — 1 7.47
CHEMBL108164 — — 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441225 CP-99994 IC50 = 0.2 nM 9.70
CHEMBL107482 — IC50 = 0.21 nM 9.68
CHEMBL415705 — IC50 = 0.25 nM 9.60
CHEMBL107172 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (3,5-BIS-TRIFLUOROMETHYL-BENZYL)-METHYL-AMIDE (STRUCTURAL MIX) IC50 = 0.34 nM 9.47
CHEMBL106864 — IC50 = 0.4 nM 9.40
CHEMBL104301 — IC50 = 1.1 nM 8.96
CHEMBL317896 — IC50 = 1.2 nM 8.92
CHEMBL106087 — IC50 = 1.3 nM 8.89
CHEMBL110679 — IC50 = 2.5 nM 8.60
CHEMBL107848 — IC50 = 2.5 nM 8.60
CHEMBL319874 — IC50 = 3.4 nM 8.47
CHEMBL105629 — IC50 = 3.4 nM 8.47
CHEMBL322718 — IC50 = 4.2 nM 8.38
CHEMBL106904 — IC50 = 4.4 nM 8.36
CHEMBL317870 — IC50 = 5.1 nM 8.29
CHEMBL107172 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (3,5-BIS-TRIFLUOROMETHYL-BENZYL)-METHYL-AMIDE (STRUCTURAL MIX) IC50 = 7.0 nM 8.15
CHEMBL104370 — IC50 = 8.4 nM 8.08
CHEMBL104225 — IC50 = 13.0 nM 7.89
CHEMBL104165 — IC50 = 16.0 nM 7.80
CHEMBL104737 — IC50 = 16.0 nM 7.80
CHEMBL106326 — IC50 = 19.0 nM 7.72
CHEMBL104060 — IC50 = 19.0 nM 7.72
CHEMBL108126 — IC50 = 23.0 nM 7.64
CHEMBL107959 — IC50 = 23.0 nM 7.64
CHEMBL106609 — IC50 = 28.0 nM 7.55
CHEMBL320231 — IC50 = 30.0 nM 7.52
CHEMBL104513 — IC50 = 32.0 nM 7.50
CHEMBL322714 — IC50 = 32.0 nM 7.50
CHEMBL107145 — IC50 = 34.0 nM 7.47
CHEMBL107689 — IC50 = 34.0 nM 7.47
CHEMBL108164 — IC50 = 54.0 nM 7.27
CHEMBL104277 — IC50 = 66.0 nM 7.18
CHEMBL326889 — IC50 = 68.0 nM 7.17
CHEMBL269781 — IC50 = 110.0 nM 6.96
CHEMBL421591 — IC50 = 110.0 nM 6.96
CHEMBL107618 — IC50 = 140.0 nM 6.85
CHEMBL104435 — IC50 = 250.0 nM 6.60
CHEMBL104345 — IC50 = 460.0 nM 6.34
CHEMBL107220 — IC50 = 470.0 nM 6.33
CHEMBL104654 — IC50 = 480.0 nM 6.32
CHEMBL107283 — IC50 = 600.0 nM 6.22
CHEMBL319932 — IC50 = 800.0 nM 6.10
CHEMBL107619 — IC50 = 840.0 nM 6.08
CHEMBL108010 — IC50 = 860.0 nM 6.07
CHEMBL104075 — IC50 = 1500.0 nM 5.82
CHEMBL321979 — IC50 = 3600.0 nM 5.44