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Assay Detail

CHEMBL620619

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

Binding
Binding affinity against 5-hydroxytryptamine 2C receptor using [125I]DOI radioligand.
38
Total Activities
32
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 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists.
Ennis MD, Hoffman RL, Ghazal NB, Olson RM, Knauer CS, Chio CL, Hyslop DK, Campbell JE, Fitzgerald LW, Nichols NF, Svensson KA, McCall RB, Haber CL, Kagey ML, Dinh DM.
Bioorg Med Chem Lett (2003) 13 : 2369 -2372
PubMed 12824036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 38 7.16 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76494 1 8.37
CHEMBL77234 1 8.33
CHEMBL312258 1 8.32
CHEMBL310620 1 8.21
CHEMBL312742 1 8.17
CHEMBL310473 1 7.92
CHEMBL312179 1 7.89
CHEMBL77701 2 7.85
CHEMBL6557 PNU-22394 1 7.72
CHEMBL311726 1 7.64
CHEMBL76645 2 7.52
CHEMBL312762 3 7.50
CHEMBL308958 1 7.42
CHEMBL310497 1 7.37
CHEMBL310090 1 7.27
CHEMBL310540 1 7.24
CHEMBL80603 1 7.19
CHEMBL312222 1 7.13
CHEMBL78164 1 7.07
CHEMBL76099 3 6.99
CHEMBL76153 1 6.95
CHEMBL79153 1 6.87
CHEMBL311614 1 6.80
CHEMBL310844 1 6.65
CHEMBL77418 1 6.58
CHEMBL80706 1 6.51
CHEMBL309570 1 6.41
CHEMBL75738 1 6.33
CHEMBL306540 1 6.14
CHEMBL310984 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76494 Ki = 4.3 nM 8.37
CHEMBL77234 Ki = 4.7 nM 8.33
CHEMBL312258 Ki = 4.8 nM 8.32
CHEMBL310620 Ki = 6.1 nM 8.21
CHEMBL312742 Ki = 6.8 nM 8.17
CHEMBL310473 Ki = 12.0 nM 7.92
CHEMBL312179 Ki = 13.0 nM 7.89
CHEMBL77701 Ki = 14.0 nM 7.85
CHEMBL6557 PNU-22394 Ki = 19.0 nM 7.72
CHEMBL311726 Ki = 23.0 nM 7.64
CHEMBL76645 Ki = 30.0 nM 7.52
CHEMBL312762 Ki = 32.0 nM 7.50
CHEMBL308958 Ki = 38.0 nM 7.42
CHEMBL76645 Ki = 39.0 nM 7.41
CHEMBL310497 Ki = 43.0 nM 7.37
CHEMBL310090 Ki = 54.0 nM 7.27
CHEMBL312762 Ki = 54.0 nM 7.27
CHEMBL310540 Ki = 57.0 nM 7.24
CHEMBL77701 Ki = 59.0 nM 7.23
CHEMBL80603 Ki = 64.0 nM 7.19
CHEMBL312222 Ki = 74.0 nM 7.13
CHEMBL78164 Ki = 85.0 nM 7.07
CHEMBL76099 Ki = 103.0 nM 6.99
CHEMBL76099 Ki = 110.0 nM 6.96
CHEMBL76153 Ki = 112.0 nM 6.95
CHEMBL79153 Ki = 136.0 nM 6.87
CHEMBL311614 Ki = 160.0 nM 6.80
CHEMBL312762 Ki = 178.0 nM 6.75
CHEMBL76099 Ki = 196.0 nM 6.71
CHEMBL310844 Ki = 223.0 nM 6.65
CHEMBL77418 Ki = 265.0 nM 6.58
CHEMBL80706 Ki = 310.0 nM 6.51
CHEMBL309570 Ki = 386.0 nM 6.41
CHEMBL75738 Ki = 472.0 nM 6.33
CHEMBL306540 Ki = 721.0 nM 6.14
CHEMBL310984 Ki = 793.0 nM 6.10
CHEMBL305655 Ki = 932.0 nM 6.03
CHEMBL310797 Ki = 4815.0 nM 5.32