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Assay Detail

CHEMBL698300

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Binding
Binding affinity for imidazoline receptor I-2 in rabbit kidney homogenate (relative to [3H]-Idazoxan radioligand)
ChEMBL ↗
119
Total Activities
119
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Kidney
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Nischarin (CHEMBL3923) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3D-QSAR CoMFA study on imidazolinergic I(2) ligands: a significant model through a combined exploration of structural diversity and methodology.
Baurin N, Vangrevelinghe E, Morin-Allory L, Mérour JY, Renard P, Payard M, Guillaumet G, Marot C.
J Med Chem (2000) 43 : 1109 -1122
PubMed 10737743 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 119 7.03 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266155 BENAZOLINE — 1 9.20
CHEMBL14097 — — 1 9.10
CHEMBL14640 — — 1 9.00
CHEMBL14107 — — 1 8.90
CHEMBL13698 — — 1 8.80
CHEMBL404505 — — 1 8.80
CHEMBL418536 — — 1 8.80
CHEMBL14012 FENOXAZOLINE 2.0 1 8.70
CHEMBL279200 — — 1 8.70
CHEMBL275970 TRACIZOLINE — 1 8.70
CHEMBL13987 — — 1 8.70
CHEMBL14210 PHENYZOLINE — 1 8.60
CHEMBL13887 — — 1 8.60
CHEMBL266861 — — 1 8.60
CHEMBL13343 — — 1 8.60
CHEMBL267801 — — 1 8.50
CHEMBL13631 — — 1 8.50
CHEMBL13892 — — 1 8.40
CHEMBL276276 — — 1 8.40
CHEMBL14203 — — 1 8.40
CHEMBL13852 CIRAZOLINE 2.0 1 8.40
CHEMBL276487 — — 1 8.30
CHEMBL13633 — — 1 8.30
CHEMBL14528 — — 1 8.30
CHEMBL268945 — — 1 8.30
CHEMBL268734 — — 1 8.20
CHEMBL13917 — — 1 8.20
CHEMBL10316 IDAZOXAN 3.0 1 8.10
CHEMBL14028 — — 1 8.10
CHEMBL269197 — — 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266155 BENAZOLINE Ki = 0.631 nM 9.20
CHEMBL14097 — Ki = 0.7943 nM 9.10
CHEMBL14640 — Ki = 1.0 nM 9.00
CHEMBL14107 — Ki = 1.259 nM 8.90
CHEMBL418536 — Ki = 1.585 nM 8.80
CHEMBL404505 — Ki = 1.585 nM 8.80
CHEMBL13698 — Ki = 1.585 nM 8.80
CHEMBL13987 — Ki = 1.995 nM 8.70
CHEMBL275970 TRACIZOLINE Ki = 1.995 nM 8.70
CHEMBL14012 FENOXAZOLINE Ki = 1.995 nM 8.70
CHEMBL279200 — Ki = 1.995 nM 8.70
CHEMBL13887 — Ki = 2.512 nM 8.60
CHEMBL266861 — Ki = 2.512 nM 8.60
CHEMBL13343 — Ki = 2.512 nM 8.60
CHEMBL14210 PHENYZOLINE Ki = 2.512 nM 8.60
CHEMBL13631 — Ki = 3.162 nM 8.50
CHEMBL267801 — Ki = 3.162 nM 8.50
CHEMBL13892 — Ki = 3.981 nM 8.40
CHEMBL13852 CIRAZOLINE Ki = 3.981 nM 8.40
CHEMBL14203 — Ki = 3.981 nM 8.40
CHEMBL276276 — Ki = 3.981 nM 8.40
CHEMBL268945 — Ki = 5.012 nM 8.30
CHEMBL14528 — Ki = 5.012 nM 8.30
CHEMBL13633 — Ki = 5.012 nM 8.30
CHEMBL276487 — Ki = 5.012 nM 8.30
CHEMBL268734 — Ki = 6.31 nM 8.20
CHEMBL13917 — Ki = 6.31 nM 8.20
CHEMBL14028 — Ki = 7.943 nM 8.10
CHEMBL10316 IDAZOXAN Ki = 7.943 nM 8.10
CHEMBL269197 — Ki = 7.943 nM 8.10
CHEMBL13824 — Ki = 10.0 nM 8.00
CHEMBL266386 — Ki = 10.0 nM 8.00
CHEMBL273408 — Ki = 10.0 nM 8.00
CHEMBL274784 — Ki = 10.0 nM 8.00
CHEMBL14174 — Ki = 10.0 nM 8.00
CHEMBL278221 — Ki = 10.0 nM 8.00
CHEMBL13809 — Ki = 10.0 nM 8.00
CHEMBL13743 — Ki = 15.85 nM 7.80
CHEMBL266863 — Ki = 15.85 nM 7.80
CHEMBL13886 — Ki = 25.12 nM 7.60
CHEMBL13715 — Ki = 25.12 nM 7.60
CHEMBL14267 — Ki = 31.62 nM 7.50
CHEMBL13881 PHENAMAZOLINE Ki = 31.62 nM 7.50
CHEMBL13955 — Ki = 31.62 nM 7.50
CHEMBL14235 — Ki = 39.81 nM 7.40
CHEMBL274548 — Ki = 39.81 nM 7.40
CHEMBL14422 — Ki = 39.81 nM 7.40
CHEMBL13689 — Ki = 39.81 nM 7.40
CHEMBL13639 — Ki = 50.12 nM 7.30
CHEMBL14015 — Ki = 50.12 nM 7.30