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Assay Detail

CHEMBL1769656

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

Functional
Antagonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as inhibition of histamine-induced GTP-gammaS binding
ChEMBL ↗
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
Procopiou PA, Browning C, Buckley JM, Clark KL, Fechner L, Gore PM, Hancock AP, Hodgson ST, Holmes DS, Kranz M, Looker BE, Morriss KM, Parton DL, Russell LJ, Slack RJ, Sollis SL, Vile S, Watts CJ.
J Med Chem (2011) 54 : 2183 -2195
PubMed 21381763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 7.89 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1767160 — — 1 9.60
CHEMBL1767164 GSK-1004723 2.0 1 9.60
CHEMBL1767168 — — 1 9.60
CHEMBL1767165 — — 1 9.50
CHEMBL1767166 — — 1 9.40
CHEMBL1767162 — — 1 9.40
CHEMBL1767167 — — 1 9.40
CHEMBL1767159 — — 1 9.30
CHEMBL1767161 — — 1 8.70
CHEMBL1765111 — — 1 8.40
CHEMBL1767163 — — 1 8.10
CHEMBL1767137 — — 1 7.10
CHEMBL1767157 — — 1 7.10
CHEMBL1767135 — — 1 6.90
CHEMBL1767156 — — 1 6.90
CHEMBL639 AZELASTINE 4.0 1 6.80
CHEMBL1767151 — — 1 6.70
CHEMBL1767145 — — 1 6.70
CHEMBL1767138 — — 1 6.60
CHEMBL1767148 — — 1 6.60
CHEMBL1767139 — — 1 6.50
CHEMBL1767136 — — 1 6.40
CHEMBL1767147 — — 1 6.20
CHEMBL1767155 — — 1 -
CHEMBL1767154 — — 1 -
CHEMBL1767140 — — 1 -
CHEMBL1767158 — — 1 -
CHEMBL1767134 — — 1 -
CHEMBL1767153 — — 1 -
CHEMBL1767150 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1767160 — Ki = 0.2512 nM 9.60
CHEMBL1767168 — Ki = 0.2512 nM 9.60
CHEMBL1767164 GSK-1004723 Ki = 0.2512 nM 9.60
CHEMBL1767165 — Ki = 0.3162 nM 9.50
CHEMBL1767166 — Ki = 0.3981 nM 9.40
CHEMBL1767162 — Ki = 0.3981 nM 9.40
CHEMBL1767167 — Ki = 0.3981 nM 9.40
CHEMBL1767159 — Ki = 0.5012 nM 9.30
CHEMBL1767161 — Ki = 1.995 nM 8.70
CHEMBL1765111 — Ki = 3.981 nM 8.40
CHEMBL1767163 — Ki = 7.943 nM 8.10
CHEMBL1767137 — Ki = 79.43 nM 7.10
CHEMBL1767157 — Ki = 79.43 nM 7.10
CHEMBL1767135 — Ki = 125.89 nM 6.90
CHEMBL1767156 — Ki = 125.89 nM 6.90
CHEMBL639 AZELASTINE Ki = 158.49 nM 6.80
CHEMBL1767151 — Ki = 199.53 nM 6.70
CHEMBL1767145 — Ki = 199.53 nM 6.70
CHEMBL1767138 — Ki = 251.19 nM 6.60
CHEMBL1767148 — Ki = 251.19 nM 6.60
CHEMBL1767139 — Ki = 316.23 nM 6.50
CHEMBL1767136 — Ki = 398.11 nM 6.40
CHEMBL1767147 — Ki = 630.96 nM 6.20
CHEMBL1767152 — Ki > 1995.26 nM -
CHEMBL1767141 — Ki > 630.96 nM -
CHEMBL1767142 — Ki > 630.96 nM -
CHEMBL1767143 — Ki > 630.96 nM -
CHEMBL1767144 — Ki > 630.96 nM -
CHEMBL1767146 — Ki > 630.96 nM -
CHEMBL1767149 — Ki > 630.96 nM -
CHEMBL1767150 — Ki > 630.96 nM -
CHEMBL1767153 — Ki > 630.96 nM -
CHEMBL1767134 — Ki > 501.19 nM -
CHEMBL1767158 — Ki > 630.96 nM -
CHEMBL1767140 — Ki > 501.19 nM -
CHEMBL1767154 — Ki > 398.11 nM -
CHEMBL1767155 — Ki > 398.11 nM -