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Assay Detail

CHEMBL616337

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

Binding
Binding affinity against 5-hydroxytryptamine 1A receptor in rat cerebral cortical membrane using [3H]-8-OH-DPAT as radioligand.
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1,9-Alkano-bridged 2,3,4,5-tetrahydro-1H-3-benzazepines with affinity for the alpha 2-adrenoceptor and the 5-HT1A receptor.
Clark RD, Weinhardt KK, Berger J, Fisher LE, Brown CM, MacKinnon AC, Kilpatrick AT, Spedding M.
J Med Chem (1990) 33 : 633 -641
PubMed 2153822 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 40 7.17 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL155823 1 8.30
CHEMBL345810 1 8.20
CHEMBL156585 1 8.10
CHEMBL160918 1 8.10
CHEMBL345214 1 8.00
CHEMBL1200399 BUSPIRONE HYDROCHLORIDE 4.0 1 7.90
CHEMBL1203597 1 7.90
CHEMBL1202288 1 7.80
CHEMBL346122 1 7.80
CHEMBL160607 1 7.70
CHEMBL1203631 1 7.70
CHEMBL1202289 1 7.60
CHEMBL156229 1 7.60
CHEMBL1203603 1 7.60
CHEMBL1203625 1 7.60
CHEMBL1202291 1 7.50
CHEMBL1203624 1 7.50
CHEMBL348058 1 7.50
CHEMBL1203595 1 7.40
CHEMBL1203623 1 7.30
CHEMBL1203600 1 7.30
CHEMBL1203598 1 7.30
CHEMBL346276 1 7.30
CHEMBL1203644 1 7.20
CHEMBL348273 1 7.10
CHEMBL158505 1 7.10
CHEMBL123349 1 7.00
CHEMBL1237145 1 7.00
CHEMBL1202290 1 7.00
CHEMBL160186 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL155823 Ki = 5.012 nM 8.30
CHEMBL345810 Ki = 6.31 nM 8.20
CHEMBL160918 Ki = 7.943 nM 8.10
CHEMBL156585 Ki = 7.943 nM 8.10
CHEMBL345214 Ki = 10.0 nM 8.00
CHEMBL1200399 BUSPIRONE HYDROCHLORIDE Ki = 12.59 nM 7.90
CHEMBL1203597 Ki = 12.59 nM 7.90
CHEMBL346122 Ki = 15.85 nM 7.80
CHEMBL1202288 Ki = 15.85 nM 7.80
CHEMBL160607 Ki = 19.95 nM 7.70
CHEMBL1203631 Ki = 19.95 nM 7.70
CHEMBL1202289 Ki = 25.12 nM 7.60
CHEMBL1203625 Ki = 25.12 nM 7.60
CHEMBL1203603 Ki = 25.12 nM 7.60
CHEMBL156229 Ki = 25.12 nM 7.60
CHEMBL1202291 Ki = 31.62 nM 7.50
CHEMBL348058 Ki = 31.62 nM 7.50
CHEMBL1203624 Ki = 31.62 nM 7.50
CHEMBL1203595 Ki = 39.81 nM 7.40
CHEMBL346276 Ki = 50.12 nM 7.30
CHEMBL1203600 Ki = 50.12 nM 7.30
CHEMBL1203623 Ki = 50.12 nM 7.30
CHEMBL1203598 Ki = 50.12 nM 7.30
CHEMBL1203644 Ki = 63.1 nM 7.20
CHEMBL348273 Ki = 79.43 nM 7.10
CHEMBL158505 Ki = 79.43 nM 7.10
CHEMBL123349 Ki = 100.0 nM 7.00
CHEMBL1237145 Ki = 100.0 nM 7.00
CHEMBL1202290 Ki = 100.0 nM 7.00
CHEMBL160186 Ki = 125.89 nM 6.90
CHEMBL1203611 Ki = 199.53 nM 6.70
CHEMBL1203645 Ki = 199.53 nM 6.70
CHEMBL1203602 Ki = 316.23 nM 6.50
CHEMBL1203629 Ki = 398.11 nM 6.40
CHEMBL1203601 Ki = 630.96 nM 6.20
CHEMBL1203596 Ki = 794.33 nM 6.10
CHEMBL1203613 Ki = 1258.93 nM 5.90
CHEMBL1203614 Ki = 3162.28 nM 5.50
CHEMBL1202292 Ki = 5011.87 nM 5.30
CHEMBL1203612 Ki = 6309.57 nM 5.20