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Assay Detail

CHEMBL694998

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

Binding
Binding affinity against H2 receptor of Guinea pig atrium
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H2 receptor (CHEMBL2882)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Novel carbamates as potent histamine H3 receptor antagonists with high in vitro and oral in vivo activity.
Stark H, Purand K, Ligneau X, Rouleau A, Arrang JM, Garbarg M, Schwartz JC, Schunack W.
J Med Chem (1996) 39 : 1157 -1163
PubMed 8676353 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 4.62 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277537 1 6.00
CHEMBL263070 1 5.40
CHEMBL16874 1 5.30
CHEMBL16274 1 5.10
CHEMBL279617 1 4.90
CHEMBL16108 1 4.90
CHEMBL15883 1 4.90
CHEMBL16654 1 4.90
CHEMBL16338 1 4.80
CHEMBL16592 1 4.80
CHEMBL277989 1 4.80
CHEMBL15813 1 4.80
CHEMBL16496 1 4.50
CHEMBL16565 1 4.40
CHEMBL273549 1 4.40
CHEMBL16109 1 4.30
CHEMBL274989 1 4.20
CHEMBL16056 1 4.20
CHEMBL16231 1 4.10
CHEMBL16639 1 4.10
CHEMBL277149 1 4.10
CHEMBL16957 1 4.00
CHEMBL277285 1 4.00
CHEMBL16373 1 4.00
CHEMBL16407 1 -
CHEMBL415989 1 -
CHEMBL16404 1 -
CHEMBL16142 1 -
CHEMBL16331 1 -
CHEMBL16401 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277537 Ki = 1000.0 nM 6.00
CHEMBL263070 Ki = 3981.07 nM 5.40
CHEMBL16874 Ki = 5011.87 nM 5.30
CHEMBL16274 Ki = 7943.28 nM 5.10
CHEMBL279617 Ki = 12589.25 nM 4.90
CHEMBL16108 Ki = 12589.25 nM 4.90
CHEMBL15883 Ki = 12589.25 nM 4.90
CHEMBL16654 Ki = 12589.25 nM 4.90
CHEMBL16338 Ki = 15848.93 nM 4.80
CHEMBL16592 Ki = 15848.93 nM 4.80
CHEMBL277989 Ki = 15848.93 nM 4.80
CHEMBL15813 Ki = 15848.93 nM 4.80
CHEMBL16496 Ki = 31622.78 nM 4.50
CHEMBL16565 Ki = 39810.72 nM 4.40
CHEMBL273549 Ki = 39810.72 nM 4.40
CHEMBL16109 Ki = 50118.72 nM 4.30
CHEMBL274989 Ki = 63095.73 nM 4.20
CHEMBL16056 Ki = 63095.73 nM 4.20
CHEMBL16231 Ki = 79432.82 nM 4.10
CHEMBL16639 Ki = 79432.82 nM 4.10
CHEMBL277149 Ki = 79432.82 nM 4.10
CHEMBL16957 Ki = 100000.0 nM 4.00
CHEMBL277285 Ki = 100000.0 nM 4.00
CHEMBL16373 Ki = 100000.0 nM 4.00
CHEMBL16407 Ki > 100000.0 nM -
CHEMBL415989 Ki > 100000.0 nM -
CHEMBL16404 Ki > 100000.0 nM -
CHEMBL16142 Ki > 100000.0 nM -
CHEMBL16331 Ki > 100000.0 nM -
CHEMBL16401 Ki > 100000.0 nM -
CHEMBL274262 Ki > 100000.0 nM -