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Assay Detail

CHEMBL3778934

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

Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-M6
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Corticotropin-releasing factor receptor 1 (CHEMBL1800)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Characterization of Multisubstituted Corticotropin Releasing Factor (CRF) Peptide Antagonists (Astressins).
Erchegyi J, Wang L, Gulyas J, Samant M, Perrin MH, Lewis K, Miller C, Vaughan J, Donaldson C, Fischer W, Low W, Yakabi S, Karasawa H, Taché Y, Rivier C, Rivier J.
J Med Chem (2016) 59 : 854 -866
PubMed 26789203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 9.14 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4299295 1 9.80
CHEMBL3774395 1 9.70
CHEMBL4299341 1 9.70
CHEMBL3774868 1 9.66
CHEMBL3775030 1 9.62
CHEMBL3774682 1 9.60
CHEMBL4299349 1 9.54
CHEMBL4299348 1 9.52
CHEMBL3775796 1 9.51
CHEMBL3775621 1 9.47
CHEMBL3775678 1 9.38
CHEMBL3775778 1 9.37
CHEMBL4299352 1 9.35
CHEMBL3775812 1 9.31
CHEMBL3775437 1 9.31
CHEMBL3774594 1 9.30
CHEMBL4299308 1 9.28
CHEMBL3774939 1 9.21
CHEMBL3775761 1 9.19
CHEMBL3774836 1 9.17
CHEMBL3775192 1 9.17
CHEMBL3774485 1 9.16
CHEMBL3774742 1 9.16
CHEMBL4299297 1 9.15
CHEMBL3774465 1 9.13
CHEMBL4299340 1 9.10
CHEMBL4299286 1 9.10
CHEMBL3774713 1 9.09
CHEMBL4299335 1 9.04
CHEMBL4299314 1 8.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4299295 Ki = 0.16 nM 9.80
CHEMBL3774395 Ki = 0.2 nM 9.70
CHEMBL4299341 Ki = 0.2 nM 9.70
CHEMBL3774868 Ki = 0.22 nM 9.66
CHEMBL3775030 Ki = 0.24 nM 9.62
CHEMBL3774682 Ki = 0.25 nM 9.60
CHEMBL4299349 Ki = 0.29 nM 9.54
CHEMBL4299348 Ki = 0.3 nM 9.52
CHEMBL3775796 Ki = 0.31 nM 9.51
CHEMBL3775621 Ki = 0.34 nM 9.47
CHEMBL3775678 Ki = 0.42 nM 9.38
CHEMBL3775778 Ki = 0.43 nM 9.37
CHEMBL4299352 Ki = 0.45 nM 9.35
CHEMBL3775812 Ki = 0.49 nM 9.31
CHEMBL3775437 Ki = 0.49 nM 9.31
CHEMBL3774594 Ki = 0.5 nM 9.30
CHEMBL4299308 Ki = 0.53 nM 9.28
CHEMBL3774939 Ki = 0.61 nM 9.21
CHEMBL3775761 Ki = 0.64 nM 9.19
CHEMBL3775192 Ki = 0.68 nM 9.17
CHEMBL3774836 Ki = 0.68 nM 9.17
CHEMBL3774485 Ki = 0.69 nM 9.16
CHEMBL3774742 Ki = 0.69 nM 9.16
CHEMBL4299297 Ki = 0.7 nM 9.15
CHEMBL3774465 Ki = 0.74 nM 9.13
CHEMBL4299340 Ki = 0.79 nM 9.10
CHEMBL4299286 Ki = 0.79 nM 9.10
CHEMBL3774713 Ki = 0.81 nM 9.09
CHEMBL4299335 Ki = 0.91 nM 9.04
CHEMBL4299314 Ki = 1.07 nM 8.97
CHEMBL4299294 Ki = 1.13 nM 8.95
CHEMBL4299355 Ki = 1.15 nM 8.94
CHEMBL4299313 Ki = 3.0 nM 8.52
CHEMBL3775830 Ki = 8.05 nM 8.09
CHEMBL3775707 Ki = 48.98 nM 7.31
CHEMBL3775831 Ki = 48.6 nM 7.31