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Assay Detail

CHEMBL1036178

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Binding
Displacement of [3H]N-alpha methyl histamine from human cloned histamine H3 receptor expressed in C6 cells
ChEMBL ↗
73
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type C6
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships.
Zhao C, Sun M, Bennani YL, Miller TR, Witte DG, Esbenshade TA, Wetter J, Marsh KC, Hancock AA, Brioni JD, Cowart MD.
J Med Chem (2009) 52 : 4640 -4649
PubMed 19588934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 73 7.54 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL451821 — — 1 9.68
CHEMBL351231 — — 2 9.35
CHEMBL563998 — — 2 9.27
CHEMBL564405 — — 2 8.82
CHEMBL551355 — — 2 8.49
CHEMBL549470 — — 2 8.38
CHEMBL563976 — — 2 8.31
CHEMBL191703 CONESSINE 2.0 2 8.27
CHEMBL558084 — — 2 8.23
CHEMBL554495 — — 2 8.18
CHEMBL538429 — — 2 7.97
CHEMBL558085 — — 2 7.91
CHEMBL551289 — — 2 7.88
CHEMBL563392 — — 2 7.84
CHEMBL561028 — — 2 7.81
CHEMBL552506 — — 2 7.80
CHEMBL488891 — — 1 7.71
CHEMBL560958 — — 2 7.69
CHEMBL550017 — — 2 7.60
CHEMBL571448 — — 2 7.58
CHEMBL559446 — — 2 7.37
CHEMBL563409 — — 2 7.26
CHEMBL552505 — — 2 7.21
CHEMBL559447 — — 2 7.15
CHEMBL561420 — — 2 7.05
CHEMBL560358 — — 2 7.00
CHEMBL565206 — — 2 6.94
CHEMBL563014 — — 2 6.74
CHEMBL562100 — — 2 6.64
CHEMBL551896 — — 2 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL451821 — Ki = 0.21 nM 9.68
CHEMBL351231 — Ki = 0.45 nM 9.35
CHEMBL351231 — Ki = 0.4467 nM 9.35
CHEMBL563998 — Ki = 0.54 nM 9.27
CHEMBL563998 — Ki = 0.537 nM 9.27
CHEMBL564405 — Ki = 1.51 nM 8.82
CHEMBL564405 — Ki = 1.514 nM 8.82
CHEMBL551355 — Ki = 3.236 nM 8.49
CHEMBL551355 — Ki = 3.24 nM 8.49
CHEMBL549470 — Ki = 4.14 nM 8.38
CHEMBL549470 — Ki = 4.169 nM 8.38
CHEMBL563976 — Ki = 4.898 nM 8.31
CHEMBL563976 — Ki = 4.9 nM 8.31
CHEMBL191703 CONESSINE Ki = 5.37 nM 8.27
CHEMBL191703 CONESSINE Ki = 5.37 nM 8.27
CHEMBL558084 — Ki = 5.89 nM 8.23
CHEMBL558084 — Ki = 5.888 nM 8.23
CHEMBL554495 — Ki = 6.607 nM 8.18
CHEMBL554495 — Ki = 6.61 nM 8.18
CHEMBL538429 — Ki = 10.7 nM 7.97
CHEMBL538429 — Ki = 10.72 nM 7.97
CHEMBL558085 — Ki = 12.3 nM 7.91
CHEMBL558085 — Ki = 12.3 nM 7.91
CHEMBL551289 — Ki = 13.18 nM 7.88
CHEMBL551289 — Ki = 13.2 nM 7.88
CHEMBL563392 — Ki = 14.5 nM 7.84
CHEMBL563392 — Ki = 14.45 nM 7.84
CHEMBL561028 — Ki = 15.5 nM 7.81
CHEMBL561028 — Ki = 15.49 nM 7.81
CHEMBL552506 — Ki = 15.85 nM 7.80
CHEMBL552506 — Ki = 15.9 nM 7.80
CHEMBL488891 — Ki = 19.7 nM 7.71
CHEMBL560958 — Ki = 20.42 nM 7.69
CHEMBL560958 — Ki = 20.4 nM 7.69
CHEMBL550017 — Ki = 25.12 nM 7.60
CHEMBL550017 — Ki = 25.1 nM 7.60
CHEMBL571448 — Ki = 26.3 nM 7.58
CHEMBL571448 — Ki = 26.3 nM 7.58
CHEMBL559446 — Ki = 42.66 nM 7.37
CHEMBL559446 — Ki = 42.7 nM 7.37
CHEMBL563409 — Ki = 55.0 nM 7.26
CHEMBL563409 — Ki = 54.95 nM 7.26
CHEMBL552505 — Ki = 61.7 nM 7.21
CHEMBL552505 — Ki = 61.66 nM 7.21
CHEMBL559447 — Ki = 70.79 nM 7.15
CHEMBL559447 — Ki = 70.8 nM 7.15
CHEMBL561420 — Ki = 89.13 nM 7.05
CHEMBL561420 — Ki = 89.1 nM 7.05
CHEMBL560358 — Ki = 100.0 nM 7.00
CHEMBL560358 — Ki = 100.0 nM 7.00