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Assay Detail

CHEMBL807959

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

Binding
Inhibition of binding of [125I]SP to the CHO cell line expressing human Tachykinin receptor 1
ChEMBL ↗
63
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Identification of a series of 3-(benzyloxy)-1-azabicyclo[2.2.2]octane human NK1 antagonists.
Swain CJ, Seward EM, Cascieri MA, Fong TM, Herbert R, MacIntyre DE, Merchant KJ, Owen SN, Owens AP, Sabin V.
J Med Chem (1995) 38 : 4793 -4805
PubMed 7490729 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 63 7.57 10.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431690 — — 1 10.07
CHEMBL49638 — — 1 9.70
CHEMBL22194 L-709210 — 1 9.70
CHEMBL357012 — — 2 9.59
CHEMBL263795 — — 1 9.49
CHEMBL16192 CP-96345 — 2 9.10
CHEMBL341863 — — 1 9.05
CHEMBL145800 — — 2 8.82
CHEMBL145535 — — 2 8.80
CHEMBL359206 — — 3 8.49
CHEMBL356518 — — 2 8.46
CHEMBL145265 — — 3 8.41
CHEMBL142477 — — 1 8.12
CHEMBL145077 — — 2 8.08
CHEMBL423019 — — 1 7.70
CHEMBL145050 — — 1 7.48
CHEMBL142855 — — 1 7.44
CHEMBL145030 — — 1 7.43
CHEMBL145360 — — 1 7.43
CHEMBL146552 — — 1 7.25
CHEMBL142638 — — 1 7.21
CHEMBL146223 — — 1 7.21
CHEMBL145801 — — 1 7.17
CHEMBL145414 — — 1 7.10
CHEMBL344970 — — 1 7.07
CHEMBL145308 — — 1 7.03
CHEMBL145022 — — 1 6.99
CHEMBL145799 — — 1 6.97
CHEMBL145552 — — 1 6.97
CHEMBL144996 — — 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431690 — IC50 = 0.085 nM 10.07
CHEMBL49638 — IC50 = 0.2 nM 9.70
CHEMBL22194 L-709210 IC50 = 0.2 nM 9.70
CHEMBL357012 — IC50 = 0.26 nM 9.59
CHEMBL263795 — IC50 = 0.32 nM 9.49
CHEMBL16192 CP-96345 IC50 = 0.8 nM 9.10
CHEMBL341863 — IC50 = 0.9 nM 9.05
CHEMBL357012 — IC50 = 0.9 nM 9.05
CHEMBL145800 — IC50 = 1.5 nM 8.82
CHEMBL145535 — IC50 = 1.6 nM 8.80
CHEMBL145800 — IC50 = 1.9 nM 8.72
CHEMBL145535 — IC50 = 2.7 nM 8.57
CHEMBL359206 — IC50 = 3.2 nM 8.49
CHEMBL356518 — IC50 = 3.5 nM 8.46
CHEMBL145265 — IC50 = 3.9 nM 8.41
CHEMBL142477 — IC50 = 7.5 nM 8.12
CHEMBL145077 — IC50 = 8.3 nM 8.08
CHEMBL356518 — IC50 = 9.0 nM 8.05
CHEMBL16192 CP-96345 IC50 = 9.0 nM 8.05
CHEMBL145077 — IC50 = 9.3 nM 8.03
CHEMBL145265 — IC50 = 10.0 nM 8.00
CHEMBL423019 — IC50 = 20.0 nM 7.70
CHEMBL359206 — IC50 = 23.0 nM 7.64
CHEMBL145050 — IC50 = 33.0 nM 7.48
CHEMBL142855 — IC50 = 36.0 nM 7.44
CHEMBL145360 — IC50 = 37.0 nM 7.43
CHEMBL145030 — IC50 = 37.0 nM 7.43
CHEMBL146552 — IC50 = 56.0 nM 7.25
CHEMBL146223 — IC50 = 62.0 nM 7.21
CHEMBL142638 — IC50 = 62.0 nM 7.21
CHEMBL145801 — IC50 = 67.0 nM 7.17
CHEMBL145414 — IC50 = 80.0 nM 7.10
CHEMBL344970 — IC50 = 86.0 nM 7.07
CHEMBL145308 — IC50 = 93.0 nM 7.03
CHEMBL145022 — IC50 = 103.0 nM 6.99
CHEMBL145799 — IC50 = 107.0 nM 6.97
CHEMBL145552 — IC50 = 106.0 nM 6.97
CHEMBL144996 — IC50 = 110.0 nM 6.96
CHEMBL435564 — IC50 = 120.0 nM 6.92
CHEMBL296228 — IC50 = 125.0 nM 6.90
CHEMBL424307 — IC50 = 127.0 nM 6.90
CHEMBL358589 — IC50 = 150.0 nM 6.82
CHEMBL145500 — IC50 = 172.0 nM 6.76
CHEMBL444872 — IC50 = 197.0 nM 6.71
CHEMBL145008 — IC50 = 246.0 nM 6.61
CHEMBL145514 — IC50 = 252.0 nM 6.60
CHEMBL145051 — IC50 = 300.0 nM 6.52
CHEMBL297068 — IC50 = 300.0 nM 6.52
CHEMBL359206 — IC50 = 353.0 nM 6.45
CHEMBL142919 — IC50 = 370.0 nM 6.43