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Assay Detail

CHEMBL866716

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

Binding
Displacement of [125I]galanin from human galanin Gal3 receptor
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Galanin receptor type 3 (CHEMBL2731)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Amino substituted analogs of 1-phenyl-3-phenylimino-2-indolones with potent galanin Gal3 receptor binding affinity and improved solubility.
Konkel MJ, Packiarajan M, Chen H, Topiwala UP, Jimenez H, Talisman IJ, Coate H, Walker MW.
Bioorg Med Chem Lett (2006) 16 : 3950 -3954
PubMed 16730981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.31 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL209497 1 8.30
CHEMBL209498 1 8.10
CHEMBL378991 1 7.82
CHEMBL210288 1 7.77
CHEMBL378825 1 7.68
CHEMBL211398 1 7.58
CHEMBL209642 1 7.57
CHEMBL377468 1 7.54
CHEMBL213893 1 7.47
CHEMBL383941 1 7.42
CHEMBL209476 1 7.35
CHEMBL211031 1 7.31
CHEMBL377328 1 7.16
CHEMBL211467 1 7.11
CHEMBL209481 1 7.06
CHEMBL209730 1 7.05
CHEMBL211522 1 6.54
CHEMBL425250 1 6.10
CHEMBL212224 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL209497 Ki = 5.0 nM 8.30
CHEMBL209498 Ki = 8.0 nM 8.10
CHEMBL378991 Ki = 15.0 nM 7.82
CHEMBL210288 Ki = 17.0 nM 7.77
CHEMBL378825 Ki = 21.0 nM 7.68
CHEMBL211398 Ki = 26.0 nM 7.58
CHEMBL209642 Ki = 27.0 nM 7.57
CHEMBL377468 Ki = 29.0 nM 7.54
CHEMBL213893 Ki = 34.0 nM 7.47
CHEMBL383941 Ki = 38.0 nM 7.42
CHEMBL209476 Ki = 45.0 nM 7.35
CHEMBL211031 Ki = 49.0 nM 7.31
CHEMBL377328 Ki = 70.0 nM 7.16
CHEMBL211467 Ki = 78.0 nM 7.11
CHEMBL209481 Ki = 87.0 nM 7.06
CHEMBL209730 Ki = 89.0 nM 7.05
CHEMBL211522 Ki = 290.0 nM 6.54
CHEMBL425250 Ki = 790.0 nM 6.10
CHEMBL212224 Ki = 1000.0 nM 6.00