CCR2B receptor antagonists: Conversion of a weak HTS hit to a potent lead compound

Ian T. Forbes; David G. Cooper; Emma K. Dodds; Deirdre M. B. Hickey; Robert J. Ife; Malcolm Meeson; Martin Stockley; Theo Berkhout; Jayneeta Gohil; Pieter H. E. Groot; Kitty E. Moores

doi:10.1016/S0960-894X(00)00347-4

CCR2B receptor antagonists: Conversion of a weak HTS hit to a potent lead compound

Ian T. Forbes
, David G. Cooper
, Emma K. Dodds
, Deirdre M. B. Hickey
, Robert J. Ife
, Malcolm Meeson
, Martin Stockley
, Theo Berkhout
, Jayneeta Gohil
, Pieter H. E. Groot
, Kitty E. Moores

Research output: Contribution to journal › Article › peer-review

56 Citations (Scopus)

Abstract

A weak HTS hit at the CCR2B receptor has been converted into a potent antagonist by array SAR studies. Selectivity over the closely related CCR5 receptor is also achieved. (C) 2000 Elsevier Science Ltd. All rights reserved.

Original language	English
Pages (from-to)	1803-1806
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	10
Issue number	16
DOIs	https://doi.org/10.1016/S0960-894X(00)00347-4
Publication status	Published - 21 Aug 2000

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title = "CCR2B receptor antagonists: Conversion of a weak HTS hit to a potent lead compound",

abstract = "A weak HTS hit at the CCR2B receptor has been converted into a potent antagonist by array SAR studies. Selectivity over the closely related CCR5 receptor is also achieved. (C) 2000 Elsevier Science Ltd. All rights reserved.",

author = "Forbes, \{Ian T.\} and Cooper, \{David G.\} and Dodds, \{Emma K.\} and Hickey, \{Deirdre M. B.\} and Ife, \{Robert J.\} and Malcolm Meeson and Martin Stockley and Theo Berkhout and Jayneeta Gohil and Groot, \{Pieter H. E.\} and Moores, \{Kitty E.\}",

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language = "English",

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T1 - CCR2B receptor antagonists

T2 - Conversion of a weak HTS hit to a potent lead compound

AU - Forbes, Ian T.

AU - Cooper, David G.

AU - Dodds, Emma K.

AU - Hickey, Deirdre M. B.

AU - Ife, Robert J.

AU - Meeson, Malcolm

AU - Stockley, Martin

AU - Berkhout, Theo

AU - Gohil, Jayneeta

AU - Groot, Pieter H. E.

AU - Moores, Kitty E.

PY - 2000/8/21

Y1 - 2000/8/21

N2 - A weak HTS hit at the CCR2B receptor has been converted into a potent antagonist by array SAR studies. Selectivity over the closely related CCR5 receptor is also achieved. (C) 2000 Elsevier Science Ltd. All rights reserved.

AB - A weak HTS hit at the CCR2B receptor has been converted into a potent antagonist by array SAR studies. Selectivity over the closely related CCR5 receptor is also achieved. (C) 2000 Elsevier Science Ltd. All rights reserved.

U2 - 10.1016/S0960-894X(00)00347-4

DO - 10.1016/S0960-894X(00)00347-4

M3 - Article

C2 - 10969972

AN - SCOPUS:0034698896

SN - 0960-894X

VL - 10

SP - 1803

EP - 1806

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 16

ER -

CCR2B receptor antagonists: Conversion of a weak HTS hit to a potent lead compound

Abstract

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