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Assay Detail

CHEMBL861820

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Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL ↗
61
Total Activities
32
Compounds Tested
4
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SK-N-MC
Confidence 9 — Direct single protein target
Curated By Expert

Target

Histamine H3 receptor (CHEMBL264) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: effect of various substitutions at the primary amino function.
Govoni M, Lim HD, El-Atmioui D, Menge WM, Timmerman H, Bakker RA, Leurs R, De Esch IJ.
J Med Chem (2006) 49 : 2549 -2557
PubMed 16610798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 32 - -
EC50 16 7.86 8.90
Log EC50 8 - -
IC50 5 8.06 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL206000 — — 2 8.90
CHEMBL203263 — — 2 8.90
CHEMBL90019 IMBUTAMINE — 2 8.30
CHEMBL417096 IMPENTAMINE — 2 8.30
CHEMBL206303 — — 2 8.30
CHEMBL203441 — — 2 8.30
CHEMBL205834 — — 2 8.10
CHEMBL205559 — — 2 8.10
CHEMBL381074 — — 2 8.00
CHEMBL377954 — — 2 8.00
CHEMBL206346 — — 2 7.90
CHEMBL205731 — — 2 7.80
CHEMBL203389 — — 2 7.70
CHEMBL204843 — — 2 7.60
CHEMBL205583 — — 2 7.50
CHEMBL203228 — — 2 7.50
CHEMBL206548 — — 2 7.50
CHEMBL204360 — — 2 7.40
CHEMBL206451 — — 2 7.40
CHEMBL205868 — — 2 7.30
CHEMBL203390 — — 2 7.30
CHEMBL202638 — — 2 -
CHEMBL205511 — — 2 -
CHEMBL379027 — — 1 -
CHEMBL383324 — — 1 -
CHEMBL379447 — — 1 -
CHEMBL205732 — — 2 -
CHEMBL202744 — — 2 -
CHEMBL377491 — — 2 -
CHEMBL202728 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203263 — IC50 = 1.259 nM 8.90
CHEMBL206000 — EC50 = 1.259 nM 8.90
CHEMBL90019 IMBUTAMINE EC50 = 5.012 nM 8.30
CHEMBL417096 IMPENTAMINE EC50 = 5.012 nM 8.30
CHEMBL203441 — EC50 = 5.012 nM 8.30
CHEMBL206303 — EC50 = 5.012 nM 8.30
CHEMBL205559 — IC50 = 7.943 nM 8.10
CHEMBL205834 — EC50 = 7.943 nM 8.10
CHEMBL381074 — EC50 = 10.0 nM 8.00
CHEMBL377954 — IC50 = 10.0 nM 8.00
CHEMBL206346 — IC50 = 12.59 nM 7.90
CHEMBL205731 — EC50 = 15.85 nM 7.80
CHEMBL203389 — EC50 = 19.95 nM 7.70
CHEMBL204843 — EC50 = 25.12 nM 7.60
CHEMBL203228 — EC50 = 31.62 nM 7.50
CHEMBL206548 — EC50 = 31.62 nM 7.50
CHEMBL205583 — EC50 = 31.62 nM 7.50
CHEMBL204360 — EC50 = 39.81 nM 7.40
CHEMBL206451 — IC50 = 39.81 nM 7.40
CHEMBL203390 — EC50 = 50.12 nM 7.30
CHEMBL205868 — EC50 = 50.12 nM 7.30
CHEMBL204360 — Activity = 0.47 — -
CHEMBL205583 — Activity = 0.64 — -
CHEMBL202744 — Log EC50 - — -
CHEMBL205868 — Activity = 0.35 — -
CHEMBL90019 IMBUTAMINE Activity = 0.98 — -
CHEMBL205732 — Activity = 0.1 — -
CHEMBL204843 — Activity = 0.73 — -
CHEMBL377491 — Log EC50 - — -
CHEMBL204615 — Log EC50 - — -
CHEMBL202728 — Log EC50 - — -
CHEMBL379447 — Activity - — -
CHEMBL383324 — Activity - — -
CHEMBL379027 — Activity - — -
CHEMBL205731 — Activity = 0.45 — -
CHEMBL204615 — Activity = 0.07 — -
CHEMBL206000 — Activity = 0.94 — -
CHEMBL202728 — Activity = - — -
CHEMBL377491 — Activity = 0.01 — -
CHEMBL203263 — Activity = -0.97 — -
CHEMBL204413 — Activity = 0.11 — -
CHEMBL381074 — Activity = 0.44 — -
CHEMBL206451 — Activity = -0.55 — -
CHEMBL203441 — Activity = 0.55 — -
CHEMBL205834 — Activity = 0.35 — -
CHEMBL202638 — Activity = 0.04 — -
CHEMBL202744 — Activity = 0.02 — -
CHEMBL206346 — Activity = -0.51 — -
CHEMBL377954 — Activity = -0.65 — -
CHEMBL204413 — Log EC50 - — -