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Assay Detail

CHEMBL812541

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

Binding
Binding affinity towards human Tachykinin receptor 1 expressed in CHO cells by the displacement of [125 I] substance P
24
Total Activities
24
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

Acyclic NK-1 antagonists: 2-benzhydryl-2-aminoethyl ethers
Williams BJ, Teall M, Mc Kenna J, Harrison T, Swain CJ, Cascieri MA, Sadowski S, Strader C, Baker R
Bioorg Med Chem Lett (1994) 4 : 1903 -1908
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.86 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56038 1 9.28
CHEMBL28055 1 9.07
CHEMBL283356 L-706125 1 9.00
CHEMBL53901 1 8.66
CHEMBL55823 1 8.36
CHEMBL56427 1 8.26
CHEMBL55476 1 8.17
CHEMBL417784 1 8.03
CHEMBL56372 1 8.01
CHEMBL281940 1 7.97
CHEMBL56442 1 7.96
CHEMBL59380 1 7.95
CHEMBL56814 1 7.90
CHEMBL299275 1 7.88
CHEMBL53846 1 7.85
CHEMBL56811 1 7.77
CHEMBL59310 1 7.68
CHEMBL55796 1 7.26
CHEMBL264376 1 7.12
CHEMBL55635 1 7.11
CHEMBL418114 1 7.09
CHEMBL417766 1 7.03
CHEMBL55651 1 6.82
CHEMBL56176 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56038 IC50 = 0.53 nM 9.28
CHEMBL28055 IC50 = 0.85 nM 9.07
CHEMBL283356 L-706125 IC50 = 1.0 nM 9.00
CHEMBL53901 IC50 = 2.2 nM 8.66
CHEMBL55823 IC50 = 4.4 nM 8.36
CHEMBL56427 IC50 = 5.5 nM 8.26
CHEMBL55476 IC50 = 6.8 nM 8.17
CHEMBL417784 IC50 = 9.3 nM 8.03
CHEMBL56372 IC50 = 9.7 nM 8.01
CHEMBL281940 IC50 = 10.7 nM 7.97
CHEMBL56442 IC50 = 11.0 nM 7.96
CHEMBL59380 IC50 = 11.3 nM 7.95
CHEMBL56814 IC50 = 12.7 nM 7.90
CHEMBL299275 IC50 = 13.3 nM 7.88
CHEMBL53846 IC50 = 14.0 nM 7.85
CHEMBL56811 IC50 = 17.0 nM 7.77
CHEMBL59310 IC50 = 21.0 nM 7.68
CHEMBL55796 IC50 = 55.0 nM 7.26
CHEMBL264376 IC50 = 75.0 nM 7.12
CHEMBL55635 IC50 = 77.0 nM 7.11
CHEMBL418114 IC50 = 82.0 nM 7.09
CHEMBL417766 IC50 = 93.0 nM 7.03
CHEMBL55651 IC50 = 150.0 nM 6.82
CHEMBL56176 IC50 = 367.0 nM 6.43