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Assay Detail

CHEMBL3056380

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

Binding
Binding affinity to I2 imidazoline binding site (unknown origin)
25
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Alpha2-Adrenergic Receptors in Intestinal Epithelial Cells: Mechanisms of Signaling, Role, and Regulation
Nicolotti O, Carotti A, Carrieri A, Pigini M, Gentili F, Brasili L, Giannella M, Quaglia W, Piergentili A, Bousquet P, Dontenwill M
Med Chem Res (2004) 13 : 170 -189
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.50 9.07
pKi 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266155 BENAZOLINE 1 9.07
CHEMBL14640 1 9.05
CHEMBL275970 TRACIZOLINE 1 8.74
CHEMBL14210 PHENYZOLINE 1 8.60
CHEMBL13852 CIRAZOLINE 2.0 1 8.41
CHEMBL93845 1 8.22
CHEMBL13881 PHENAMAZOLINE 2.0 1 7.48
CHEMBL761 NAPHAZOLINE 4.0 1 7.00
CHEMBL2092860 1 7.00
CHEMBL94022 1 6.91
CHEMBL2092861 1 6.84
CHEMBL13789 1 6.52
CHEMBL501690 1 6.48
CHEMBL337862 1 6.09
CHEMBL134 CLONIDINE 4.0 1 6.02
CHEMBL289480 RILMENIDINE 4.0 1 5.96
CHEMBL1907831 1 5.60
CHEMBL416893 1 5.54
CHEMBL396013 1 5.14
CHEMBL1907832 1 4.90
CHEMBL242265 1 4.31
CHEMBL2261603 1 4.00
CHEMBL288951 1 4.00
CHEMBL360803 PI-CLONIDINE 1 4.00
CHEMBL1162356 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266155 BENAZOLINE Ki = 0.8511 nM 9.07
CHEMBL14640 Ki = 0.8913 nM 9.05
CHEMBL275970 TRACIZOLINE Ki = 1.82 nM 8.74
CHEMBL14210 PHENYZOLINE Ki = 2.512 nM 8.60
CHEMBL13852 CIRAZOLINE Ki = 3.89 nM 8.41
CHEMBL93845 Ki = 6.026 nM 8.22
CHEMBL13881 PHENAMAZOLINE Ki = 33.11 nM 7.48
CHEMBL761 NAPHAZOLINE Ki = 100.0 nM 7.00
CHEMBL2092860 Ki = 100.0 nM 7.00
CHEMBL94022 Ki = 123.03 nM 6.91
CHEMBL2092861 Ki = 144.54 nM 6.84
CHEMBL13789 Ki = 302.0 nM 6.52
CHEMBL501690 Ki = 331.13 nM 6.48
CHEMBL337862 Ki = 812.83 nM 6.09
CHEMBL134 CLONIDINE Ki = 954.99 nM 6.02
CHEMBL289480 RILMENIDINE Ki = 1096.48 nM 5.96
CHEMBL1907831 Ki = 2511.89 nM 5.60
CHEMBL416893 Ki = 2884.03 nM 5.54
CHEMBL396013 Ki = 7244.36 nM 5.14
CHEMBL1907832 Ki = 12589.25 nM 4.90
CHEMBL242265 Ki = 48977.88 nM 4.31
CHEMBL2261603 Ki = 100000.0 nM 4.00
CHEMBL288951 Ki = 100000.0 nM 4.00
CHEMBL360803 PI-CLONIDINE Ki = 100000.0 nM 4.00
CHEMBL1162356 pKi - -