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Assay Detail

CHEMBL1049258

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

Binding
Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells
ChEMBL ↗
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cannabinoid receptor 1 (CHEMBL218) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, cannabinoid receptor affinity, molecular modeling studies and in vivo pharmacological evaluation of new substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides. 2. Effect of the 3-carboxamide substituent on the affinity and selectivity profile.
Silvestri R, Ligresti A, La Regina G, Piscitelli F, Gatti V, Brizzi A, Pasquini S, Lavecchia A, Allarà M, Fantini N, Carai MA, Novellino E, Colombo G, Di Marzo V, Corelli F.
Bioorg Med Chem (2009) 17 : 5549 -5564
PubMed 19595596 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 57 7.04 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285932 — — 1 8.64
CHEMBL573546 — — 1 8.47
CHEMBL272203 — — 1 8.25
CHEMBL576549 — — 1 8.25
CHEMBL575382 — — 1 8.25
CHEMBL111 RIMONABANT 4.0 1 7.92
CHEMBL579249 — — 1 7.92
CHEMBL574480 — — 1 7.85
CHEMBL572887 — — 1 7.70
CHEMBL410727 — — 1 7.55
CHEMBL575184 — — 1 7.52
CHEMBL578848 — — 1 7.51
CHEMBL575395 — — 1 7.44
CHEMBL574036 — — 1 7.39
CHEMBL577165 — — 1 7.30
CHEMBL574046 — — 1 7.30
CHEMBL574971 — — 1 7.27
CHEMBL574052 — — 1 7.25
CHEMBL574499 — — 1 7.25
CHEMBL572860 — — 1 7.25
CHEMBL575193 — — 1 7.16
CHEMBL576366 — — 1 7.16
CHEMBL574270 — — 1 7.10
CHEMBL575401 — — 1 7.10
CHEMBL579247 — — 1 7.08
CHEMBL572854 — — 1 7.05
CHEMBL576140 — — 1 7.02
CHEMBL577361 — — 1 7.00
CHEMBL576977 — — 1 7.00
CHEMBL573796 — — 1 6.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285932 — Ki = 2.3 nM 8.64
CHEMBL573546 — Ki = 3.4 nM 8.47
CHEMBL576549 — Ki = 5.6 nM 8.25
CHEMBL575382 — Ki = 5.6 nM 8.25
CHEMBL272203 — Ki = 5.6 nM 8.25
CHEMBL111 RIMONABANT Ki = 12.0 nM 7.92
CHEMBL579249 — Ki = 12.0 nM 7.92
CHEMBL574480 — Ki = 14.0 nM 7.85
CHEMBL572887 — Ki = 20.0 nM 7.70
CHEMBL410727 — Ki = 28.0 nM 7.55
CHEMBL575184 — Ki = 30.0 nM 7.52
CHEMBL578848 — Ki = 31.0 nM 7.51
CHEMBL575395 — Ki = 36.0 nM 7.44
CHEMBL574036 — Ki = 41.0 nM 7.39
CHEMBL574046 — Ki = 50.0 nM 7.30
CHEMBL577165 — Ki = 50.0 nM 7.30
CHEMBL574971 — Ki = 54.0 nM 7.27
CHEMBL574052 — Ki = 56.0 nM 7.25
CHEMBL574499 — Ki = 56.0 nM 7.25
CHEMBL572860 — Ki = 56.0 nM 7.25
CHEMBL575193 — Ki = 70.0 nM 7.16
CHEMBL576366 — Ki = 70.0 nM 7.16
CHEMBL574270 — Ki = 80.0 nM 7.10
CHEMBL575401 — Ki = 80.0 nM 7.10
CHEMBL579247 — Ki = 84.0 nM 7.08
CHEMBL572854 — Ki = 90.0 nM 7.05
CHEMBL576140 — Ki = 96.0 nM 7.02
CHEMBL577361 — Ki = 100.0 nM 7.00
CHEMBL576977 — Ki = 99.0 nM 7.00
CHEMBL573796 — Ki = 112.0 nM 6.95
CHEMBL574032 — Ki = 117.0 nM 6.93
CHEMBL572613 — Ki = 120.0 nM 6.92
CHEMBL574722 — Ki = 140.0 nM 6.85
CHEMBL574965 — Ki = 144.0 nM 6.84
CHEMBL573805 — Ki = 150.0 nM 6.82
CHEMBL577791 — Ki = 156.0 nM 6.81
CHEMBL574031 — Ki = 157.0 nM 6.80
CHEMBL574970 — Ki = 165.0 nM 6.78
CHEMBL575178 — Ki = 218.0 nM 6.66
CHEMBL574959 — Ki = 227.0 nM 6.64
CHEMBL575186 — Ki = 240.0 nM 6.62
CHEMBL575163 — Ki = 310.0 nM 6.51
CHEMBL574053 — Ki = 340.0 nM 6.47
CHEMBL573098 — Ki = 345.0 nM 6.46
CHEMBL578003 — Ki = 368.0 nM 6.43
CHEMBL585177 — Ki = 380.0 nM 6.42
CHEMBL574045 — Ki = 390.0 nM 6.41
CHEMBL573099 — Ki = 560.0 nM 6.25
CHEMBL572620 — Ki = 560.0 nM 6.25
CHEMBL576142 — Ki = 840.0 nM 6.08