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Assay Detail

CHEMBL2434417

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

Binding
Binding affinity at human 5HT1A receptor
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
Del Bello F, Diamanti E, Giannella M, Mammoli V, Mattioli L, Titomanlio F, Piergentili A, Quaglia W, Lanza M, Sabatini C, Caselli G, Poggesi E, Pigini M.
ACS Med Chem Lett (2013) 4 : 875 -879
PubMed 24900763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.54 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 8.47
CHEMBL2089156 1 8.24
CHEMBL1276220 1 8.22
CHEMBL1276218 1 8.14
CHEMBL1956195 CYCLOMETHYLINE 1 7.98
CHEMBL2431282 1 7.86
CHEMBL1956197 1 7.83
CHEMBL495095 ALLYPHENYLINE 1 7.55
CHEMBL13852 CIRAZOLINE 2.0 1 7.46
CHEMBL1276140 1 7.45
CHEMBL2089155 1 7.40
CHEMBL14107 1 7.15
CHEMBL2431280 1 7.10
CHEMBL13917 1 7.10
CHEMBL2431281 1 7.08
CHEMBL1956192 1 6.83
CHEMBL2431279 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 3.388 nM 8.47
CHEMBL2089156 Ki = 5.754 nM 8.24
CHEMBL1276220 Ki = 6.026 nM 8.22
CHEMBL1276218 Ki = 7.244 nM 8.14
CHEMBL1956195 CYCLOMETHYLINE Ki = 10.47 nM 7.98
CHEMBL2431282 Ki = 13.8 nM 7.86
CHEMBL1956197 Ki = 14.79 nM 7.83
CHEMBL495095 ALLYPHENYLINE Ki = 28.18 nM 7.55
CHEMBL13852 CIRAZOLINE Ki = 34.67 nM 7.46
CHEMBL1276140 Ki = 35.48 nM 7.45
CHEMBL2089155 Ki = 39.81 nM 7.40
CHEMBL14107 Ki = 70.79 nM 7.15
CHEMBL2431280 Ki = 79.43 nM 7.10
CHEMBL13917 Ki = 79.43 nM 7.10
CHEMBL2431281 Ki = 83.18 nM 7.08
CHEMBL1956192 Ki = 147.91 nM 6.83
CHEMBL2431279 Ki = 562.34 nM 6.25