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Assay Detail

CHEMBL1052804

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

Binding
Displacement of [3H]Arg8-vasopressin from human vasopressin V1a receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Vasopressin V1a receptor (CHEMBL1889)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.
Scott JD, Miller MW, Li SW, Lin SI, Vaccaro HA, Hong L, Mullins DE, Guzzi M, Weinstein J, Hodgson RA, Varty GB, Stamford AW, Chan TY, McKittrick BA, Greenlee WJ, Priestley T, Parker EM.
Bioorg Med Chem Lett (2009) 19 : 6018 -6022
PubMed 19800231 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 5.93 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL582857 NELIVAPTAN 2.0 1 7.66
CHEMBL583082 1 7.48
CHEMBL572709 1 6.73
CHEMBL583083 1 6.72
CHEMBL1204126 1 6.50
CHEMBL572760 1 6.40
CHEMBL572984 1 6.31
CHEMBL572754 1 6.26
CHEMBL576341 1 6.15
CHEMBL583081 1 6.14
CHEMBL575796 1 6.02
CHEMBL1204403 1 5.95
CHEMBL575797 1 5.90
CHEMBL575987 1 5.90
CHEMBL572983 1 5.58
CHEMBL575359 1 5.44
CHEMBL567176 1 5.34
CHEMBL572835 1 5.32
CHEMBL583084 1 5.31
CHEMBL575986 1 5.30
CHEMBL575972 1 5.25
CHEMBL577816 1 5.21
CHEMBL575574 1 5.16
CHEMBL572921 1 5.06
CHEMBL574450 1 5.05
CHEMBL577599 1 -
CHEMBL576147 1 -
CHEMBL575773 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL582857 NELIVAPTAN Ki = 22.0 nM 7.66
CHEMBL583082 Ki = 33.0 nM 7.48
CHEMBL572709 Ki = 188.0 nM 6.73
CHEMBL583083 Ki = 192.0 nM 6.72
CHEMBL1204126 Ki = 314.0 nM 6.50
CHEMBL572760 Ki = 395.0 nM 6.40
CHEMBL572984 Ki = 486.0 nM 6.31
CHEMBL572754 Ki = 553.0 nM 6.26
CHEMBL576341 Ki = 709.0 nM 6.15
CHEMBL583081 Ki = 720.0 nM 6.14
CHEMBL575796 Ki = 947.0 nM 6.02
CHEMBL1204403 Ki = 1129.0 nM 5.95
CHEMBL575797 Ki = 1257.0 nM 5.90
CHEMBL575987 Ki = 1268.0 nM 5.90
CHEMBL572983 Ki = 2600.0 nM 5.58
CHEMBL575359 Ki = 3654.0 nM 5.44
CHEMBL567176 Ki = 4617.0 nM 5.34
CHEMBL572835 Ki = 4803.0 nM 5.32
CHEMBL583084 Ki = 4926.0 nM 5.31
CHEMBL575986 Ki = 4963.0 nM 5.30
CHEMBL575972 Ki = 5564.0 nM 5.25
CHEMBL577816 Ki = 6164.0 nM 5.21
CHEMBL575574 Ki = 6888.0 nM 5.16
CHEMBL572921 Ki = 8734.0 nM 5.06
CHEMBL574450 Ki = 8866.0 nM 5.05
CHEMBL577599 Ki > 10000.0 nM -
CHEMBL576147 Ki > 10000.0 nM -
CHEMBL575773 Ki > 8000.0 nM -