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Assay Detail

CHEMBL1051850

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Functional
Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
ChEMBL ↗
79
Total Activities
79
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

5-hydroxytryptamine receptor 4 (CHEMBL1875) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A multivalent approach to the design and discovery of orally efficacious 5-HT4 receptor agonists.
McKinnell RM, Armstrong SR, Beattie DT, Choi SK, Fatheree PR, Gendron RA, Goldblum A, Humphrey PP, Long DD, Marquess DG, Shaw JP, Smith JA, Turner SD, Vickery RG.
J Med Chem (2009) 52 : 5330 -5343
PubMed 19663444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 79 7.88 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL539713 — — 1 9.40
CHEMBL538635 — — 1 9.40
CHEMBL540981 — — 1 9.20
CHEMBL558163 — — 1 9.20
CHEMBL553404 — — 1 9.20
CHEMBL553405 — — 1 9.10
CHEMBL552484 — — 1 9.10
CHEMBL551013 — — 1 9.10
CHEMBL555222 — — 1 9.10
CHEMBL558719 — — 1 9.00
CHEMBL555210 — — 1 9.00
CHEMBL555223 — — 1 9.00
CHEMBL541968 — — 1 8.90
CHEMBL541223 — — 1 8.90
CHEMBL561278 — — 1 8.90
CHEMBL553685 — — 1 8.90
CHEMBL538706 — — 1 8.90
CHEMBL549449 — — 1 8.80
CHEMBL561398 — — 1 8.70
CHEMBL555693 — — 1 8.60
CHEMBL559322 — — 1 8.60
CHEMBL540980 — — 1 8.60
CHEMBL549650 — — 1 8.60
CHEMBL559548 — — 1 8.50
CHEMBL556326 — — 1 8.50
CHEMBL538956 — — 1 8.50
CHEMBL562636 — — 1 8.50
CHEMBL558855 — — 1 8.40
CHEMBL562902 — — 1 8.30
CHEMBL557867 — — 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL539713 — EC50 = 0.3981 nM 9.40
CHEMBL538635 — EC50 = 0.3981 nM 9.40
CHEMBL558163 — EC50 = 0.631 nM 9.20
CHEMBL553404 — EC50 = 0.631 nM 9.20
CHEMBL540981 — EC50 = 0.631 nM 9.20
CHEMBL553405 — EC50 = 0.7943 nM 9.10
CHEMBL552484 — EC50 = 0.7943 nM 9.10
CHEMBL551013 — EC50 = 0.7943 nM 9.10
CHEMBL555222 — EC50 = 0.7943 nM 9.10
CHEMBL558719 — EC50 = 1.0 nM 9.00
CHEMBL555210 — EC50 = 1.0 nM 9.00
CHEMBL555223 — EC50 = 1.0 nM 9.00
CHEMBL553685 — EC50 = 1.259 nM 8.90
CHEMBL541223 — EC50 = 1.259 nM 8.90
CHEMBL541968 — EC50 = 1.259 nM 8.90
CHEMBL561278 — EC50 = 1.259 nM 8.90
CHEMBL538706 — EC50 = 1.259 nM 8.90
CHEMBL549449 — EC50 = 1.585 nM 8.80
CHEMBL561398 — EC50 = 1.995 nM 8.70
CHEMBL555693 — EC50 = 2.512 nM 8.60
CHEMBL559322 — EC50 = 2.512 nM 8.60
CHEMBL540980 — EC50 = 2.512 nM 8.60
CHEMBL549650 — EC50 = 2.512 nM 8.60
CHEMBL562636 — EC50 = 3.162 nM 8.50
CHEMBL538956 — EC50 = 3.162 nM 8.50
CHEMBL559548 — EC50 = 3.162 nM 8.50
CHEMBL556326 — EC50 = 3.162 nM 8.50
CHEMBL558855 — EC50 = 3.981 nM 8.40
CHEMBL562902 — EC50 = 5.012 nM 8.30
CHEMBL557867 — EC50 = 5.012 nM 8.30
CHEMBL565146 — EC50 = 6.31 nM 8.20
CHEMBL552075 — EC50 = 6.31 nM 8.20
CHEMBL550459 — EC50 = 7.943 nM 8.10
CHEMBL539651 — EC50 = 7.943 nM 8.10
CHEMBL558259 — EC50 = 10.0 nM 8.00
CHEMBL559050 — EC50 = 10.0 nM 8.00
CHEMBL558924 — EC50 = 12.59 nM 7.90
CHEMBL559746 — EC50 = 12.59 nM 7.90
CHEMBL556235 — EC50 = 12.59 nM 7.90
CHEMBL551820 — EC50 = 15.85 nM 7.80
CHEMBL560940 — EC50 = 15.85 nM 7.80
CHEMBL560876 — EC50 = 15.85 nM 7.80
CHEMBL555447 — EC50 = 15.85 nM 7.80
CHEMBL552693 — EC50 = 15.85 nM 7.80
CHEMBL556595 — EC50 = 15.85 nM 7.80
CHEMBL550122 — EC50 = 19.95 nM 7.70
CHEMBL550530 — EC50 = 19.95 nM 7.70
CHEMBL563261 — EC50 = 25.12 nM 7.60
CHEMBL557053 — EC50 = 25.12 nM 7.60
CHEMBL559317 — EC50 = 25.12 nM 7.60