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Assay Detail

CHEMBL4140911

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

Binding
Displacement of [3H] substance P from recombinant human NK1 receptor expressed in CHO cells after 90 mins by scintillation counting method
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines.
Abe M, Seto M, Gogliotti RG, Loch MT, Bollinger KA, Chang S, Engelberg EM, Luscombe VB, Harp JM, Bubser M, Engers DW, Jones CK, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW.
ACS Med Chem Lett (2017) 8 : 1110 -1115
PubMed 29057060 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 6.19 6.19
IC50 1 5.47 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4160748 2 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4160748 Ki = 650.0 nM 6.19
CHEMBL4160748 IC50 = 3400.0 nM 5.47