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Assay Detail

CHEMBL812171

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

Binding
Displacement of [125I]-labeled substance P from the cloned Tachykinin receptor 1
26
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I.
Elliott JM, Castro JL, Chicchi GG, Cooper LC, Dinnell K, Hollingworth GJ, Ridgill MP, Rycroft W, Kurtz MM, Shaw DE, Swain CJ, Tsao KL, Yang L.
Bioorg Med Chem Lett (2002) 12 : 1755 -1758
PubMed 12067554 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 8.30 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296583 1 9.54
CHEMBL2115007 1 9.47
CHEMBL49176 3 9.46
CHEMBL50867 1 9.36
CHEMBL300014 1 9.31
CHEMBL295685 1 9.21
CHEMBL296397 1 9.20
CHEMBL2115006 1 9.15
CHEMBL51417 1 9.12
CHEMBL422931 1 9.02
CHEMBL2115005 1 8.77
CHEMBL2115004 1 8.60
CHEMBL2115010 1 8.38
CHEMBL296629 1 8.28
CHEMBL2115008 1 8.20
CHEMBL49175 1 7.40
CHEMBL2115454 1 7.23
CHEMBL2115450 1 7.09
CHEMBL2115451 1 7.07
CHEMBL2115009 1 6.92
CHEMBL46103 1 6.89
CHEMBL2115449 1 6.85
CHEMBL51893 1 6.82
CHEMBL2115452 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296583 IC50 = 0.29 nM 9.54
CHEMBL2115007 IC50 = 0.34 nM 9.47
CHEMBL49176 IC50 = 0.35 nM 9.46
CHEMBL50867 IC50 = 0.44 nM 9.36
CHEMBL300014 IC50 = 0.49 nM 9.31
CHEMBL295685 IC50 = 0.62 nM 9.21
CHEMBL296397 IC50 = 0.63 nM 9.20
CHEMBL2115006 IC50 = 0.7 nM 9.15
CHEMBL51417 IC50 = 0.75 nM 9.12
CHEMBL49176 IC50 = 0.77 nM 9.11
CHEMBL422931 IC50 = 0.95 nM 9.02
CHEMBL49176 IC50 = 1.5 nM 8.82
CHEMBL2115005 IC50 = 1.7 nM 8.77
CHEMBL2115004 IC50 = 2.5 nM 8.60
CHEMBL2115010 IC50 = 4.2 nM 8.38
CHEMBL296629 IC50 = 5.3 nM 8.28
CHEMBL2115008 IC50 = 6.3 nM 8.20
CHEMBL49175 IC50 = 40.0 nM 7.40
CHEMBL2115454 IC50 = 59.0 nM 7.23
CHEMBL2115450 IC50 = 82.0 nM 7.09
CHEMBL2115451 IC50 = 85.0 nM 7.07
CHEMBL2115009 IC50 = 120.0 nM 6.92
CHEMBL46103 IC50 = 130.0 nM 6.89
CHEMBL2115449 IC50 = 140.0 nM 6.85
CHEMBL51893 IC50 = 150.0 nM 6.82
CHEMBL2115452 IC50 = 250.0 nM 6.60