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Assay Detail

CHEMBL693824

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Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL ↗
65
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Histamine H1 receptor (CHEMBL3943) ↗
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis, biological evaluation, and quantitative structure-activity relationship analysis of [beta-(Aroylamino)ethyl]piperazines and -piperidines and [2-[(Arylamino)carbonyl]ethyl]piperazines, -pyrazinopyridoindoles, and -pyrazinoisoquinolines. A new class of potent H1 antagonists.
Saxena M, Agarwal SK, Patnaik GK, Saxena AK.
J Med Chem (1990) 33 : 2970 -2976
PubMed 1977909 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 6.13 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL657 DIPHENHYDRAMINE 4.0 2 9.00
CHEMBL100442 — — 1 6.69
CHEMBL321104 — — 1 6.55
CHEMBL100858 — — 2 6.46
CHEMBL101490 — — 1 6.44
CHEMBL97938 — — 1 6.43
CHEMBL319123 — — 2 6.38
CHEMBL101973 — — 2 6.32
CHEMBL421393 — — 2 6.28
CHEMBL101491 — — 1 6.27
CHEMBL100276 — — 2 6.25
CHEMBL101625 — — 2 6.20
CHEMBL100125 — — 2 6.18
CHEMBL319817 — — 2 6.17
CHEMBL321738 — — 2 6.16
CHEMBL101088 — — 2 6.11
CHEMBL101758 — — 2 6.10
CHEMBL101133 — — 2 6.08
CHEMBL101387 — — 2 6.08
CHEMBL327724 — — 1 6.03
CHEMBL101217 — — 2 6.01
CHEMBL101790 — — 2 5.97
CHEMBL101029 — — 2 5.89
CHEMBL100169 — — 2 5.88
CHEMBL101312 — — 2 5.88
CHEMBL100695 — — 2 5.88
CHEMBL100064 — — 2 5.87
CHEMBL103303 — — 2 5.82
CHEMBL101388 — — 2 5.81
CHEMBL100865 — — 2 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL657 DIPHENHYDRAMINE IC50 = 1.0 nM 9.00
CHEMBL100442 — IC50 = 206.0 nM 6.69
CHEMBL321104 — IC50 = 283.0 nM 6.55
CHEMBL100858 — IC50 = 345.0 nM 6.46
CHEMBL101490 — IC50 = 364.0 nM 6.44
CHEMBL97938 — IC50 = 375.0 nM 6.43
CHEMBL319123 — IC50 = 421.0 nM 6.38
CHEMBL101973 — IC50 = 477.0 nM 6.32
CHEMBL421393 — IC50 = 525.0 nM 6.28
CHEMBL101491 — IC50 = 535.0 nM 6.27
CHEMBL100276 — IC50 = 561.0 nM 6.25
CHEMBL101625 — IC50 = 634.0 nM 6.20
CHEMBL100125 — IC50 = 661.0 nM 6.18
CHEMBL319817 — IC50 = 677.0 nM 6.17
CHEMBL321738 — IC50 = 696.0 nM 6.16
CHEMBL101088 — IC50 = 778.0 nM 6.11
CHEMBL101758 — IC50 = 799.0 nM 6.10
CHEMBL101387 — IC50 = 836.0 nM 6.08
CHEMBL101133 — IC50 = 832.0 nM 6.08
CHEMBL327724 — IC50 = 925.0 nM 6.03
CHEMBL101217 — IC50 = 979.0 nM 6.01
CHEMBL101790 — IC50 = 1071.0 nM 5.97
CHEMBL101029 — IC50 = 1276.0 nM 5.89
CHEMBL100695 — IC50 = 1318.0 nM 5.88
CHEMBL101312 — IC50 = 1318.0 nM 5.88
CHEMBL100169 — IC50 = 1316.0 nM 5.88
CHEMBL100064 — IC50 = 1342.0 nM 5.87
CHEMBL103303 — IC50 = 1513.0 nM 5.82
CHEMBL101388 — IC50 = 1548.0 nM 5.81
CHEMBL100865 — IC50 = 1604.0 nM 5.79
CHEMBL101122 — IC50 = 1701.0 nM 5.77
CHEMBL100170 — IC50 = 1740.0 nM 5.76
CHEMBL316616 — IC50 = 2167.0 nM 5.66
CHEMBL101927 — IC50 = 6940.0 nM 5.16
CHEMBL328170 — IC50 = 7120.0 nM 5.15
CHEMBL328170 — IC50 = 2.4 ug.mL-1 -
CHEMBL101973 — IC50 = 0.17 ug.mL-1 -
CHEMBL101122 — IC50 = 0.75 ug.mL-1 -
CHEMBL103303 — IC50 = 0.49 ug.mL-1 -
CHEMBL100858 — IC50 = 0.18 ug.mL-1 -
CHEMBL101133 — IC50 = 0.28 ug.mL-1 -
CHEMBL100169 — IC50 = 0.5 ug.mL-1 -
CHEMBL101217 — IC50 = 0.4 ug.mL-1 -
CHEMBL100865 — IC50 = 0.6 ug.mL-1 -
CHEMBL316616 — IC50 = 0.71 ug.mL-1 -
CHEMBL101387 — IC50 = 0.36 ug.mL-1 -
CHEMBL657 DIPHENHYDRAMINE IC50 = 0.001 ug.mL-1 -
CHEMBL421393 — IC50 = 0.19 ug.mL-1 -
CHEMBL101927 — IC50 = 2.75 ug.mL-1 -
CHEMBL101088 — IC50 = 0.33 ug.mL-1 -