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Assay Detail

CHEMBL617757

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

Binding
Binding affinity towards human cloned 5-hydroxytryptamine 2C receptor of HEK293 cells by displacement of [3H]mesulergine
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.
Bromidge SM, Dabbs S, Davies S, Duckworth DM, Forbes IT, Jones GE, Jones J, King FD, Saunders DV, Blackburn TP, Holland V, Kennett GA, Lightowler S, Middlemiss DN, Riley GJ, Trail B, Wood MD.
Bioorg Med Chem Lett (2000) 10 : 1863 -1866
PubMed 10969986 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 8.49 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54560 1 9.40
CHEMBL55207 1 9.30
CHEMBL14374 1 9.20
CHEMBL301012 1 9.20
CHEMBL59584 1 9.10
CHEMBL55079 1 9.00
CHEMBL14460 SB-243213 1 9.00
CHEMBL14563 SB-242084 1 9.00
CHEMBL55331 1 9.00
CHEMBL292228 1 8.90
CHEMBL294030 1 8.90
CHEMBL53152 1 8.90
CHEMBL55292 1 8.90
CHEMBL56508 1 8.80
CHEMBL55472 1 8.80
CHEMBL54775 1 8.80
CHEMBL55964 1 8.80
CHEMBL56336 1 8.80
CHEMBL55792 1 8.70
CHEMBL52308 1 8.70
CHEMBL53308 1 8.70
CHEMBL301784 1 8.70
CHEMBL299938 1 8.70
CHEMBL52919 1 8.60
CHEMBL53113 1 8.50
CHEMBL54769 1 8.50
CHEMBL433060 1 8.50
CHEMBL56050 1 8.50
CHEMBL58765 1 8.50
CHEMBL54610 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54560 Ki = 0.3981 nM 9.40
CHEMBL55207 Ki = 0.5012 nM 9.30
CHEMBL301012 Ki = 0.631 nM 9.20
CHEMBL14374 Ki = 0.631 nM 9.20
CHEMBL59584 Ki = 0.7943 nM 9.10
CHEMBL55079 Ki = 1.0 nM 9.00
CHEMBL14460 SB-243213 Ki = 1.0 nM 9.00
CHEMBL14563 SB-242084 Ki = 1.0 nM 9.00
CHEMBL55331 Ki = 1.0 nM 9.00
CHEMBL53152 Ki = 1.259 nM 8.90
CHEMBL55292 Ki = 1.259 nM 8.90
CHEMBL294030 Ki = 1.259 nM 8.90
CHEMBL292228 Ki = 1.259 nM 8.90
CHEMBL56336 Ki = 1.585 nM 8.80
CHEMBL55964 Ki = 1.585 nM 8.80
CHEMBL56508 Ki = 1.585 nM 8.80
CHEMBL54775 Ki = 1.585 nM 8.80
CHEMBL55472 Ki = 1.585 nM 8.80
CHEMBL299938 Ki = 1.995 nM 8.70
CHEMBL301784 Ki = 1.995 nM 8.70
CHEMBL53308 Ki = 1.995 nM 8.70
CHEMBL55792 Ki = 1.995 nM 8.70
CHEMBL52308 Ki = 1.995 nM 8.70
CHEMBL52919 Ki = 2.512 nM 8.60
CHEMBL53113 Ki = 3.162 nM 8.50
CHEMBL54769 Ki = 3.162 nM 8.50
CHEMBL433060 Ki = 3.162 nM 8.50
CHEMBL56050 Ki = 3.162 nM 8.50
CHEMBL58765 Ki = 3.162 nM 8.50
CHEMBL54610 Ki = 3.981 nM 8.40
CHEMBL299726 Ki = 3.981 nM 8.40
CHEMBL291510 Ki = 5.012 nM 8.30
CHEMBL59097 Ki = 6.31 nM 8.20
CHEMBL299530 Ki = 6.31 nM 8.20
CHEMBL298696 Ki = 15.85 nM 7.80
CHEMBL53053 Ki = 15.85 nM 7.80
CHEMBL55958 Ki = 39.81 nM 7.40
CHEMBL56232 Ki = 100.0 nM 7.00
CHEMBL53793 Ki = 125.89 nM 6.90
CHEMBL299506 Ki = 199.53 nM 6.70
CHEMBL300232 Ki = 199.53 nM 6.70