Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL814485

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

Binding
Displacement of [3H]-substance P from human NK1 receptor expressed in CHO cells
ChEMBL ↗
51
Total Activities
51
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

Discovery of orally bioavailable NK1 receptor antagonists.
Genicot C, Christophe B, Collart P, Gillard M, Goossens L, Hénichart JP, Lassoie MA, Moureau F, Neuwels M, Nicolas JM, Pasau P, Quéré L, Ryckmans T, Stiernet F, Taverne T, Van Keulen BJ.
Bioorg Med Chem Lett (2003) 13 : 437 -442
PubMed 12565946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 51 8.01 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL435796 — — 1 9.00
CHEMBL108200 — — 1 9.00
CHEMBL138824 — — 1 8.90
CHEMBL136347 — — 1 8.90
CHEMBL109937 — — 1 8.80
CHEMBL419742 — — 1 8.80
CHEMBL336305 — — 1 8.80
CHEMBL140080 — — 1 8.80
CHEMBL108889 — — 1 8.80
CHEMBL139750 — — 1 8.70
CHEMBL139088 — — 1 8.70
CHEMBL342266 — — 1 8.70
CHEMBL336251 — — 1 8.60
CHEMBL423913 — — 1 8.60
CHEMBL136504 — — 1 8.50
CHEMBL136360 — — 1 8.50
CHEMBL107875 — — 1 8.50
CHEMBL342443 — — 1 8.50
CHEMBL337789 — — 1 8.50
CHEMBL321892 — — 1 8.30
CHEMBL136213 — — 1 8.30
CHEMBL109183 — — 1 8.20
CHEMBL108422 — — 1 8.20
CHEMBL344847 — — 1 8.20
CHEMBL136709 — — 1 8.10
CHEMBL342602 — — 1 8.10
CHEMBL139150 — — 1 8.10
CHEMBL432627 — — 1 8.10
CHEMBL139531 — — 1 8.00
CHEMBL139499 — — 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL435796 — Ki = 1.0 nM 9.00
CHEMBL108200 — Ki = 1.0 nM 9.00
CHEMBL136347 — Ki = 1.259 nM 8.90
CHEMBL138824 — Ki = 1.259 nM 8.90
CHEMBL108889 — Ki = 1.585 nM 8.80
CHEMBL140080 — Ki = 1.585 nM 8.80
CHEMBL336305 — Ki = 1.585 nM 8.80
CHEMBL419742 — Ki = 1.585 nM 8.80
CHEMBL109937 — Ki = 1.585 nM 8.80
CHEMBL139750 — Ki = 1.995 nM 8.70
CHEMBL139088 — Ki = 1.995 nM 8.70
CHEMBL342266 — Ki = 1.995 nM 8.70
CHEMBL336251 — Ki = 2.512 nM 8.60
CHEMBL423913 — Ki = 2.512 nM 8.60
CHEMBL337789 — Ki = 3.162 nM 8.50
CHEMBL136360 — Ki = 3.162 nM 8.50
CHEMBL107875 — Ki = 3.162 nM 8.50
CHEMBL342443 — Ki = 3.162 nM 8.50
CHEMBL136504 — Ki = 3.162 nM 8.50
CHEMBL321892 — Ki = 5.012 nM 8.30
CHEMBL136213 — Ki = 5.012 nM 8.30
CHEMBL109183 — Ki = 6.31 nM 8.20
CHEMBL108422 — Ki = 6.31 nM 8.20
CHEMBL344847 — Ki = 6.31 nM 8.20
CHEMBL432627 — Ki = 7.943 nM 8.10
CHEMBL342602 — Ki = 7.943 nM 8.10
CHEMBL136709 — Ki = 7.943 nM 8.10
CHEMBL139150 — Ki = 7.943 nM 8.10
CHEMBL139531 — Ki = 10.0 nM 8.00
CHEMBL139499 — Ki = 10.0 nM 8.00
CHEMBL320535 — Ki = 12.59 nM 7.90
CHEMBL139382 — Ki = 15.85 nM 7.80
CHEMBL139859 — Ki = 15.85 nM 7.80
CHEMBL140302 — Ki = 15.85 nM 7.80
CHEMBL138716 — Ki = 15.85 nM 7.80
CHEMBL136291 — Ki = 15.85 nM 7.80
CHEMBL344265 — Ki = 19.95 nM 7.70
CHEMBL108822 — Ki = 25.12 nM 7.60
CHEMBL136187 — Ki = 31.62 nM 7.50
CHEMBL138839 — Ki = 39.81 nM 7.40
CHEMBL320544 — Ki = 50.12 nM 7.30
CHEMBL136389 — Ki = 63.1 nM 7.20
CHEMBL138335 — Ki = 63.1 nM 7.20
CHEMBL109514 — Ki = 79.43 nM 7.10
CHEMBL136279 — Ki = 100.0 nM 7.00
CHEMBL111304 — Ki = 100.0 nM 7.00
CHEMBL138056 — Ki = 125.89 nM 6.90
CHEMBL138682 — Ki = 158.49 nM 6.80
CHEMBL111303 — Ki = 199.53 nM 6.70
CHEMBL136850 — Ki = 251.19 nM 6.60