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Assay Detail

CHEMBL1768189

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

Binding
Displacement of [3H]neurotensin from human NTS1 receptor expressed in CHO cells
36
Total Activities
35
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

Neurotensin receptor type 1 (CHEMBL4123)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics.
Einsiedel J, Held C, Hervet M, Plomer M, Tschammer N, Hübner H, Gmeiner P.
J Med Chem (2011) 54 : 2915 -2923
PubMed 21446649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 6.61 9.64
Kd 1 9.23 9.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766935 1 9.64
CHEMBL1766928 1 9.62
CHEMBL407196 NEUROTENSIN 1 9.23
CHEMBL1766929 1 9.21
CHEMBL254769 1 8.80
CHEMBL258221 1 8.57
CHEMBL1766936 1 8.47
CHEMBL1766923 1 8.34
CHEMBL1766937 1 8.08
CHEMBL1766939 1 8.08
CHEMBL1766924 1 7.96
CHEMBL411195 1 7.77
CHEMBL1766925 1 7.58
CHEMBL266230 1 7.33
CHEMBL1766930 1 7.15
CHEMBL172313 1 7.00
CHEMBL253527 1 6.68
CHEMBL1766931 1 6.66
CHEMBL1766938 1 6.60
CHEMBL1766932 1 6.05
CHEMBL1766927 1 5.96
CHEMBL1766926 1 5.89
CHEMBL1766934 1 5.89
CHEMBL1766942 1 5.58
CHEMBL2369509 2 5.52
CHEMBL1766940 1 5.43
CHEMBL1766945 1 5.08
CHEMBL1766947 1 5.07
CHEMBL1766943 1 5.00
CHEMBL1766933 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766935 Ki = 0.23 nM 9.64
CHEMBL1766928 Ki = 0.24 nM 9.62
CHEMBL407196 NEUROTENSIN Kd = 0.59 nM 9.23
CHEMBL1766929 Ki = 0.61 nM 9.21
CHEMBL254769 Ki = 1.6 nM 8.80
CHEMBL258221 Ki = 2.7 nM 8.57
CHEMBL1766936 Ki = 3.4 nM 8.47
CHEMBL1766923 Ki = 4.6 nM 8.34
CHEMBL1766937 Ki = 8.4 nM 8.08
CHEMBL1766939 Ki = 8.4 nM 8.08
CHEMBL1766924 Ki = 11.0 nM 7.96
CHEMBL411195 Ki = 17.0 nM 7.77
CHEMBL1766925 Ki = 26.0 nM 7.58
CHEMBL266230 Ki = 47.0 nM 7.33
CHEMBL1766930 Ki = 71.0 nM 7.15
CHEMBL172313 Ki = 100.0 nM 7.00
CHEMBL253527 Ki = 210.0 nM 6.68
CHEMBL1766931 Ki = 220.0 nM 6.66
CHEMBL1766938 Ki = 250.0 nM 6.60
CHEMBL1766932 Ki = 890.0 nM 6.05
CHEMBL1766927 Ki = 1100.0 nM 5.96
CHEMBL1766926 Ki = 1300.0 nM 5.89
CHEMBL1766934 Ki = 1300.0 nM 5.89
CHEMBL1766942 Ki = 2600.0 nM 5.58
CHEMBL2369509 Ki = 3000.0 nM 5.52
CHEMBL2369509 Ki = 3300.0 nM 5.48
CHEMBL1766940 Ki = 3700.0 nM 5.43
CHEMBL1766945 Ki = 8300.0 nM 5.08
CHEMBL1766947 Ki = 8500.0 nM 5.07
CHEMBL1766943 Ki = 10000.0 nM 5.00
CHEMBL1766933 Ki = 13000.0 nM 4.89
CHEMBL1766825 Ki = 28000.0 nM 4.55
CHEMBL254770 Ki = 30000.0 nM 4.52
CHEMBL1766946 Ki = 32000.0 nM 4.50
CHEMBL1766941 Ki = 47000.0 nM 4.33
CHEMBL1766944 Ki = 80000.0 nM 4.10